bluuebunny/crossref_metadata_2025 huggingface dataset:
Table S2 from H4K20me3-Mediated Repression of Inflammatory Genes Is a Characteristic and Targetable Vulnerability of Persister Cancer Cells
Authors: Ramponi Valentina , Richart Laia , Kovatcheva Marta , Stephan-Otto Attolini Camille , Capellades Jordi , Lord Alice E. , Yanes Oscar , Ficz Gabriella , Serrano Manuel
Published: January 2025

Reagents for CUT&Tag
Table 1 from Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR–ABL–Positive Leukemia
Authors: Luo Ziwei , Lin Chencen , Yu Chuwei , Yuan Changxian , Wu Wenyong , Xu Xiaowei , Sun Renhong , Jia Yan , Wang Yafang , Shen Jie , Wang Dingyan , Wang Sinan , Jiang Hualiang , Jiang Biao , Yang Xiaobao , Xie Chengying
Published: January 2025

PK of SIAIS562055 after i.v., oral, or i.p. administration.
Figure 3 from Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR–ABL–Positive Leukemia
Authors: Luo Ziwei , Lin Chencen , Yu Chuwei , Yuan Changxian , Wu Wenyong , Xu Xiaowei , Sun Renhong , Jia Yan , Wang Yafang , Shen Jie , Wang Dingyan , Wang Sinan , Jiang Hualiang , Jiang Biao , Yang Xiaobao , Xie Chengying
Published: January 2025

SIAIS562055 alone or coadministered with KRAS inhibitors suppresses tumor growth of KRAS-mutant xenografts in vivo. A-C, MIA PaCa-2–xenografted mice received vehicle, SIAIS562055 (20 or 40 mg/kg/day), or BI-3406 [50 mg/kg, twice a day (bid)], then relative tumor volumes (A), tumor weights (B), and mouse body weights (C) were determined at indicated times. D, Western blot analysis of SOS1, pERK, and cleaved caspase-3 in MIA PaCa-2 tumor tissues after treatment with SIAI562055 or BI-3406. E and F, MIA PaCa-2 xenograft-bearing mice received vehicle, SIAIS562055, and MRTX849, alone or in combination; the relative tumor volumes (E) and photos of tumors (F) are shown. G and H, GP2d xenograft-bearing mice received vehicle, SIAIS562055, and MRTX1133, alone or in combination; the relative tumor volumes (G) and photos of tumors (H) are shown. Data are presented as mean ± SEM, n = 5. Statistical significance was assessed using two-tailed unpaired Student t test. *, P < 0.05; **, P < 0.01; ***, P < 0.001. qd, once a day.
Figure S2 from H4K20me3-Mediated Repression of Inflammatory Genes Is a Characteristic and Targetable Vulnerability of Persister Cancer Cells
Authors: Ramponi Valentina , Richart Laia , Kovatcheva Marta , Stephan-Otto Attolini Camille , Capellades Jordi , Lord Alice E. , Yanes Oscar , Ficz Gabriella , Serrano Manuel
Published: January 2025

Supplementary figure 2
Figure S1 from H4K20me3-Mediated Repression of Inflammatory Genes Is a Characteristic and Targetable Vulnerability of Persister Cancer Cells
Authors: Ramponi Valentina , Richart Laia , Kovatcheva Marta , Stephan-Otto Attolini Camille , Capellades Jordi , Lord Alice E. , Yanes Oscar , Ficz Gabriella , Serrano Manuel
Published: January 2025

Supplementary figure 1
Table S6 from TCTN1 Induces Fatty Acid Oxidation to Promote Melanoma Metastasis
Authors: Li Yinlam , Ming Ren , Zhang Tianyi , Gao Zixu , Wang Lu , Yang Yang , Shen Kangjie , Wei Chenlu , Zhu Yu , Li Jianrui , Zheng Shaoluan , Luo Zucheng , Ding Yiteng , Xuan Jiangying , Hu Qianrong , Yang Yanwen , Gu Jianying , Wei Chuanyuan
Published: January 2025

Table S6
Supplementary Figures from Stimulating Soluble Guanylyl Cyclase with the Clinical Agonist Riociguat Restrains the Development and Progression of Castration-Resistant Prostate Cancer
Authors: Zhang Ling , Troccoli Clara I. , Mateo-Victoriano Beatriz , Misiara Lincheta Laura , Jackson Erin , Shu Ping , Plastini Trisha , Tao Wensi , Kwon Deukwoo , Chen Xi Steven , Sharma Janaki , Jorda Merce , Kumar Surinder , Lombard David B. , Gulley James L. , Bilusic Marijo , Lockhart Albert C. , Beuve Annie , Rai Priyamvada
Published: January 2025

figures, legends and references associated with Supplementary figures
Table S4 from TCTN1 Induces Fatty Acid Oxidation to Promote Melanoma Metastasis
Authors: Li Yinlam , Ming Ren , Zhang Tianyi , Gao Zixu , Wang Lu , Yang Yang , Shen Kangjie , Wei Chenlu , Zhu Yu , Li Jianrui , Zheng Shaoluan , Luo Zucheng , Ding Yiteng , Xuan Jiangying , Hu Qianrong , Yang Yanwen , Gu Jianying , Wei Chuanyuan
Published: January 2025

Table S4
Figure S6 from TCTN1 Induces Fatty Acid Oxidation to Promote Melanoma Metastasis
Authors: Li Yinlam , Ming Ren , Zhang Tianyi , Gao Zixu , Wang Lu , Yang Yang , Shen Kangjie , Wei Chenlu , Zhu Yu , Li Jianrui , Zheng Shaoluan , Luo Zucheng , Ding Yiteng , Xuan Jiangying , Hu Qianrong , Yang Yanwen , Gu Jianying , Wei Chuanyuan
Published: January 2025

Figure S6
Figure S3 from TCTN1 Induces Fatty Acid Oxidation to Promote Melanoma Metastasis
Authors: Li Yinlam , Ming Ren , Zhang Tianyi , Gao Zixu , Wang Lu , Yang Yang , Shen Kangjie , Wei Chenlu , Zhu Yu , Li Jianrui , Zheng Shaoluan , Luo Zucheng , Ding Yiteng , Xuan Jiangying , Hu Qianrong , Yang Yanwen , Gu Jianying , Wei Chuanyuan
Published: January 2025

Figure S3
Figure S2 from TCTN1 Induces Fatty Acid Oxidation to Promote Melanoma Metastasis
Authors: Li Yinlam , Ming Ren , Zhang Tianyi , Gao Zixu , Wang Lu , Yang Yang , Shen Kangjie , Wei Chenlu , Zhu Yu , Li Jianrui , Zheng Shaoluan , Luo Zucheng , Ding Yiteng , Xuan Jiangying , Hu Qianrong , Yang Yanwen , Gu Jianying , Wei Chuanyuan
Published: January 2025

Figure S2
Figure S1 from TCTN1 Induces Fatty Acid Oxidation to Promote Melanoma Metastasis
Authors: Li Yinlam , Ming Ren , Zhang Tianyi , Gao Zixu , Wang Lu , Yang Yang , Shen Kangjie , Wei Chenlu , Zhu Yu , Li Jianrui , Zheng Shaoluan , Luo Zucheng , Ding Yiteng , Xuan Jiangying , Hu Qianrong , Yang Yanwen , Gu Jianying , Wei Chuanyuan
Published: January 2025

Figure S1
Supplementary Table S4 from LSD1 and CoREST2 Potentiate STAT3 Activity to Promote Enteroendocrine Cell Differentiation in Mucinous Colorectal Cancer
Authors: Ladaika Christopher A. , Ghobashi Ahmed H. , Boulton William C. , Miller Samuel A. , O’Hagan Heather M.
Published: January 2025

CoREST2-FLAG CUT&RUN data.
Supplementary Table S3 from LSD1 and CoREST2 Potentiate STAT3 Activity to Promote Enteroendocrine Cell Differentiation in Mucinous Colorectal Cancer
Authors: Ladaika Christopher A. , Ghobashi Ahmed H. , Boulton William C. , Miller Samuel A. , O’Hagan Heather M.
Published: January 2025

STAT3 CUT&RUN data.
Supplementary Table S2 from LSD1 and CoREST2 Potentiate STAT3 Activity to Promote Enteroendocrine Cell Differentiation in Mucinous Colorectal Cancer
Authors: Ladaika Christopher A. , Ghobashi Ahmed H. , Boulton William C. , Miller Samuel A. , O’Hagan Heather M.
Published: January 2025

Single cell multi-omics differentially accessible peaks.
Supplementary Table S1 from LSD1 and CoREST2 Potentiate STAT3 Activity to Promote Enteroendocrine Cell Differentiation in Mucinous Colorectal Cancer
Authors: Ladaika Christopher A. , Ghobashi Ahmed H. , Boulton William C. , Miller Samuel A. , O’Hagan Heather M.
Published: January 2025

Single cell multi-omics cluster gene expression.
Figure S7 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

KRASG12C-mutated cell lines show universal G12Ci:SOS1i synergy in the absence of SOS2.
Figure S6 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

KRASG12C-mutated cell lines show universal G12Ci:SOS1i synergy in low-serum conditions.
Figure S4 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

KRASG12C-mutated cell lines show differential G12Ci:SOS1i synergy.
Figure S19 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

SOS1i shows dose-dependent inhibition of G12Ci acquired resistance.
Figure S17 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

SOSi prevents MEKi-induced TIC outgrowth.
Figure S15 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

SOS1i prevents G12Ci-induced TIC outgrowth.
Figure S14 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

SOS1 and SOS2 protein abundance is stable in G12Ci DTPs.
Figure S11 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

SOS1i synergizes with G12Ci or MEKi in ALDHhigh cells.
Figure S10 from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

G12Ci treatment increases aldehyde dehydrogenase activity in LUAD cells.
Supplementary Figures from Distant Metastases of Breast Cancer Resemble Primary Tumors in Cancer Cell Composition but Differ in Immune Cell Phenotypes
Authors: Kuett Laura , Bollhagen Alina , Tietscher Sandra , Sobottka Bettina , Eling Nils , Varga Zsuzsanna , Moch Holger , de Souza Natalie , Bodenmiller Bernd
Published: January 2025

Supplementary Figures 1-16
Figure 4 from Distant Metastases of Breast Cancer Resemble Primary Tumors in Cancer Cell Composition but Differ in Immune Cell Phenotypes
Authors: Kuett Laura , Bollhagen Alina , Tietscher Sandra , Sobottka Bettina , Eling Nils , Varga Zsuzsanna , Moch Holger , de Souza Natalie , Bodenmiller Bernd
Published: January 2025

Immune cell phenotypes in PT and metastases. A, Uniform Manifold Approximation and Projection for Dimension Reduction (UMAP) visualization of all lymphoid cells from the T-cell panel dataset, colored by cell type (n = 87 patients). B, Heatmap showing the mean expression of T-cell–relevant markers across different T-cell phenotypic subtypes after graph-based clustering (n = 87 patients; n_cells = 91,000). Euclidean distance with average linkage was used for the hierarchical clustering of rows and columns. C, UMAP visualization of all myeloid cells from the myeloid cell panel dataset (n_cells = 161,000) excluding plasmacytoid dendritic cells (pDC), LAMP3+ DCs, and neutrophils, colored by phenotypic clusters (n = 87 patients). D, Heatmap showing the mean expression of myeloid-relevant markers across all myeloid cell phenotypic clusters resulting from graph-based clustering (n = 87 patients; n_cells = 161,000). Euclidean distance with average linkage was used for the hierarchical clustering of rows and columns. moDC, monocyte-derived DCs.
Supplementary Data from HIF1α Counteracts TGFβ1-Driven TSP1 Expression in Endothelial Cells to Stimulate Angiogenesis in the Hypoxic Tumor Microenvironment
Authors: Luo Yu-Wei , Fang Yang , Zeng Hui-Xian , Ji Yu-Chen , Wu Meng-Zhi , Li Hui , Chen Jie-Ying , Zheng Li-Min , Fang Jian-Hong , Zhuang Shi-Mei
Published: January 2025

Supplementary Data (marked with blue)
Data from TCTN1 Induces Fatty Acid Oxidation to Promote Melanoma Metastasis
Authors: Li Yinlam , Ming Ren , Zhang Tianyi , Gao Zixu , Wang Lu , Yang Yang , Shen Kangjie , Wei Chenlu , Zhu Yu , Li Jianrui , Zheng Shaoluan , Luo Zucheng , Ding Yiteng , Xuan Jiangying , Hu Qianrong , Yang Yanwen , Gu Jianying , Wei Chuanyuan
Published: January 2025

Abstract
Metabolic reprogramming promotes and sustains multiple steps of melanoma metastasis. Identification of key regulators of metabolic reprogramming could lead to the development of treatments for preventing and treating metastatic melanoma. In this study, we identified that tectonic family member 1 (TCTN1) promotes melanoma metastasis by increasing fatty acid oxidation (FAO). In clinical melanoma samples, high expression of TCTN1 correlated with increased metastasis and shorter patient survival. Functionally, TCTN1 promoted melanoma invasion and migration in vitro and distant metastasis in vivo and induced a mesenchymal-like phenotype switch. Mechanistically, TCTN1 acted as a protein scaffold to promote the binding of HADHA and HADHB, subunits of the mitochondrial trifunctional protein complex, thus leading to FAO activation. TCTN1-mediated FAO activated the p38/MAPK signaling pathway in melanoma cells, promoting tumor epithelial–mesenchymal transition and stemness. Molecular docking indicated that the prostaglandin F receptor agonist fluprostenol can block HADHA/HADHB binding, which was confirmed experimentally. Treatment with fluprostenol was able to inhibit TCTN1-induced melanoma invasion and metastasis. Taken together, these findings elucidate the mechanism of TCTN1-mediated promotion of melanoma metastasis and support the potential application of fluprostenol for targeted therapy of metastatic melanoma.

Significance: TCTN1 activates fatty acid oxidation to induce melanoma mesenchymal phenotype switching and invasion by promoting the binding of the subunits of MTP, which can be targeted with fluprostenol to inhibit melanoma metastasis.
Data from Replication Stress Is an Actionable Genetic Vulnerability in Desmoplastic Small Round Cell Tumors
Authors: Kawai-Kawachi Asuka , Lenormand Madison M. , Astier Clémence , Herbel Noé , Cutrona Meritxell B. , Ngo Carine , Garrido Marlène , Eychenne Thomas , Dorvault Nicolas , Bordelet Laetitia , Song Feifei , Bouyakoub Ryme , Loktev Anastasia , Romo-Morales Antonio , Henon Clémence , Colmet-Daage Léo , Vibert Julien , Drac Marjorie , Brough Rachel , Schwob Etienne , Martella Oliviano , Pinna Guillaume , Shipley Janet M. , Mittnacht Sibylle , Zimmermann Astrid , Gulati Aditi , Mir Olivier , Le Cesne Axel , Faron Matthieu , Honoré Charles , Lord Christopher J. , Chabanon Roman M. , Postel-Vinay Sophie
Published: January 2025

Abstract
Desmoplastic small round cell tumor (DSRCT) is an aggressive sarcoma subtype that is driven by the EWS–WT1 chimeric transcription factor. The prognosis for DSRCT is poor, and major advances in treating DSRCT have not occurred for over two decades. To identify effective therapeutic approaches to target DSRCT, we conducted a high-throughput drug sensitivity screen in a DSRCT cell line assessing chemosensitivity profiles for 79 small-molecule inhibitors. DSRCT cells were sensitive to PARP inhibitors (PARPi) and ataxia–telangiectasia and Rad3–related inhibitors (ATRi), as monotherapies and in combination. These effects were recapitulated using multiple clinical PARPi and ATRi in three biologically distinct, clinically relevant models of DSRCT, including cell lines, a patient-derived xenograft–derived organoid model, and a cell line–derived xenograft mouse model. Mechanistically, exposure to a combination of PARPi and ATRi caused increased DNA damage, G2–M checkpoint activation, micronuclei accumulation, replication stress, and R-loop formation. EWS–WT1 silencing abrogated these phenotypes and was epistatic with exogenous expression of the R-loop resolution enzyme RNase H1 in reversing sensitivity to PARPi and ATRi monotherapies. The combination of PARPi and ATRi also induced EWS–WT1–dependent cell-autonomous activation of the cyclic GMP–AMP synthase–stimulator of IFN genes innate immune pathway and cell-surface expression of PD-L1. Taken together, these findings point toward a role for EWS–WT1 in generating R-loop–dependent replication stress that leads to a targetable vulnerability, providing a rationale for the clinical assessment of PARPi and ATRi in DSRCT.

Significance: EWS–WT1, the unique oncogenic driver of desmoplastic small round cell tumors, confers sensitivity to PARP and ATR inhibitors, supporting the potential of these drugs in treating patients with this aggressive sarcoma subtype.
Data from SOS1 Inhibition Enhances the Efficacy of KRASG12C Inhibitors and Delays Resistance in Lung Adenocarcinoma
Authors: Daley Brianna R. , Sealover Nancy E. , Finniff Bridget A. , Hughes Jacob M. , Sheffels Erin , Gerlach Daniel , Hofmann Marco H. , Kostyrko Kaja , LaMorte Joseph P. , Linke Amanda J. , Beckley Zaria , Frank Andrew M. , Lewis Robert E. , Wilkerson Matthew D. , Dalgard Clifton L. , Kortum Robert L.
Published: January 2025

Abstract
The clinical effectiveness of KRASG12C inhibitors (G12Ci) is limited both by intrinsic and acquired resistance, necessitating the development of combination approaches. Here, we identified targeting proximal receptor tyrosine kinase signaling using the SOS1 inhibitor (SOS1i) BI-3406 as a strategy to improve responses to G12Ci treatment. SOS1i enhanced the efficacy of G12Ci and limited rebound receptor tyrosine kinase/ERK signaling to overcome intrinsic/adaptive resistance, but this effect was modulated by SOS2 protein levels. G12Ci drug-tolerant persister (DTP) cells showed up to a 3-fold enrichment of tumor-initiating cells (TIC), suggestive of a sanctuary population of G12Ci-resistant cells. SOS1i resensitized DTPs to G12Ci and inhibited G12C-induced TIC enrichment. Co-mutation of the tumor suppressor KEAP1 limited the clinical effectiveness of G12Ci, and KEAP1 and STK11 deletion increased TIC frequency and accelerated the development of acquired resistance to G12Ci, consistent with clinical G12Ci resistance seen with these co-mutations. Treatment with SOS1i both delayed acquired G12Ci resistance and limited the total number of resistant colonies regardless of KEAP1 and STK11 mutational status. Together, these data suggest that targeting SOS1 could be an effective strategy to both enhance G12Ci efficacy and prevent G12Ci resistance regardless of co-mutations.

Significance: The SOS1 inhibitor BI-3406 both inhibits intrinsic/adaptive resistance and targets drug tolerant persister cells to limit the development of acquired resistance to clinical KRASG12C inhibitors in lung adenocarcinoma cells.
Data from HIF1α Counteracts TGFβ1-Driven TSP1 Expression in Endothelial Cells to Stimulate Angiogenesis in the Hypoxic Tumor Microenvironment
Authors: Luo Yu-Wei , Fang Yang , Zeng Hui-Xian , Ji Yu-Chen , Wu Meng-Zhi , Li Hui , Chen Jie-Ying , Zheng Li-Min , Fang Jian-Hong , Zhuang Shi-Mei
Published: January 2025

Abstract
Emerging evidence suggests that TGFβ1 can inhibit angiogenesis, contradicting the coexistence of active angiogenesis and high abundance of TGFβ1 in the tumor microenvironment. Here, we investigated how tumors overcome the antiangiogenic effect of TGFβ1. TGFβ1 treatment suppressed physiologic angiogenesis in chick chorioallantoic membrane and zebrafish models but did not affect angiogenesis in mouse hepatoma xenografts. The suppressive effect of TGFβ1 on angiogenesis was recovered in mouse xenografts by a hypoxia-inducible factor 1α (HIF1α) inhibitor. In contrast, a HIF1α stabilizer abrogated angiogenesis in zebrafish, indicating that hypoxia may attenuate the antiangiogenic role of TGFβ1. Under normoxic conditions, TGFβ1 inhibited angiogenesis by upregulating antiangiogenic factor thrombospondin 1 (TSP1) in endothelial cells (EC) via TGFβ type I receptor (TGFβR1)–SMAD2/3 signaling. In a hypoxic microenvironment, HIF1α induced miR145 expression; miR145 abolished the inhibitory effect of TGFβ1 on angiogenesis by binding and repressing SMAD2/3 expression and subsequently reducing TSP1 levels in ECs. Primary ECs isolated from human hepatocellular carcinoma displayed increased miR145 and decreased SMAD3 and TSP1 compared with ECs from adjacent nontumor livers. The reduced SMAD3 or TSP1 in ECs was associated with increased angiogenesis in hepatocellular carcinoma tissues. Collectively, this study identified that TGFβ1–TGFβR1–SMAD2/3–TSP1 signaling in ECs inhibits angiogenesis. This inhibition can be circumvented by a hypoxia–HIF1α–miR145 axis, elucidating a mechanism by which hypoxia promotes angiogenesis.

Significance: Suppression of angiogenesis by TGFβ1 is mediated by TSP1 upregulation in endothelial cells and abrogated by HIF1α–miR145 activity in the hypoxic tumor microenvironment, providing potential targets to remodel the tumor vasculature.
Supplementary Figure 6 from PARP7 Inhibitors and AHR Agonists Act Synergistically across a Wide Range of Cancer Models
Authors: Chen Huadong , Gou Xuxu , Mao Ying , O’Leary Patrick C. , Diolaiti Morgan E. , Ashworth Alan
Published: January 2025

Supplementary Fig. 6 PARP7i and AHRa synergistically suppress the in vitro growth of hormone-resistant cancer cell lines and promote proteasomal turnover of hormone receptors
Supplementary Figure 2 from PARP7 Inhibitors and AHR Agonists Act Synergistically across a Wide Range of Cancer Models
Authors: Chen Huadong , Gou Xuxu , Mao Ying , O’Leary Patrick C. , Diolaiti Morgan E. , Ashworth Alan
Published: January 2025

Supplementary Fig. 2 The combination of PARP7i and AHRa induces cell cycle arrest, rather than apoptosis and reprograms transcriptional profiles
Supplementary Figure 1 from PARP7 Inhibitors and AHR Agonists Act Synergistically across a Wide Range of Cancer Models
Authors: Chen Huadong , Gou Xuxu , Mao Ying , O’Leary Patrick C. , Diolaiti Morgan E. , Ashworth Alan
Published: January 2025

Supplementary Fig. 1 Multiple AHRa are synergistically lethal with PARP7i in multiple cancer cells
Supplementary Table from A Small-Molecule BCL6 Inhibitor as an Anti-Proliferative Agent for Diffuse Large B-Cell Lymphoma
Authors: Xing Yajing , Guo Weikai , Wu Min , Xie Jiuqing , Huang Dongxia , Hu Pan , Zhou Miaoran , Zhang Lin , Zhong Yadong , Liu Mingyao , Chen Yihua , Yi Zhengfang
Published: January 2025

Supplementary Table 1. Main pharmacokinetic parameters of WK692 after oral administration or intravenous injection in rats (mean ± SD).
Supplementary Methods from A Small-Molecule BCL6 Inhibitor as an Anti-Proliferative Agent for Diffuse Large B-Cell Lymphoma
Authors: Xing Yajing , Guo Weikai , Wu Min , Xie Jiuqing , Huang Dongxia , Hu Pan , Zhou Miaoran , Zhang Lin , Zhong Yadong , Liu Mingyao , Chen Yihua , Yi Zhengfang
Published: January 2025

Supplementary Methods
Figure S6 from A Small-Molecule BCL6 Inhibitor as an Anti-Proliferative Agent for Diffuse Large B-Cell Lymphoma
Authors: Xing Yajing , Guo Weikai , Wu Min , Xie Jiuqing , Huang Dongxia , Hu Pan , Zhou Miaoran , Zhang Lin , Zhong Yadong , Liu Mingyao , Chen Yihua , Yi Zhengfang
Published: January 2025

Figure S6. WK692 targets BCL6-BTB domain. (A) Computer docking assay predicted that WK692 bound to the BCL6-BTB domain. (B) The binding affinities were measured by SPR assay. (C) SUDHL4 shBCL6-1/shBCL6-2 cells were infected with lentivirus for re-expression of BCL6 (vector, WT, C53A) and overexpression efficacy was examined by Western blots. (D) WK692 effectiveness against SUDHL4 shBCL6-1/shBCL6-2 cells that were infected with the indicated lentivirus expression vectors, and cell viability was determined by MTS assay.
Figure S4 from A Small-Molecule BCL6 Inhibitor as an Anti-Proliferative Agent for Diffuse Large B-Cell Lymphoma
Authors: Xing Yajing , Guo Weikai , Wu Min , Xie Jiuqing , Huang Dongxia , Hu Pan , Zhou Miaoran , Zhang Lin , Zhong Yadong , Liu Mingyao , Chen Yihua , Yi Zhengfang
Published: January 2025

Figure S4. Activation effect of BI3802, FX1 and WK692 on downstream gene of BCL6 at 10 µM. (*, P < 0.05; **, P < 0.01; ***, P < 0.001 versus control).
Figure S3 from A Small-Molecule BCL6 Inhibitor as an Anti-Proliferative Agent for Diffuse Large B-Cell Lymphoma
Authors: Xing Yajing , Guo Weikai , Wu Min , Xie Jiuqing , Huang Dongxia , Hu Pan , Zhou Miaoran , Zhang Lin , Zhong Yadong , Liu Mingyao , Chen Yihua , Yi Zhengfang
Published: January 2025

Figure S3. Quantitative ChIP assay was used to detect the enrichment of CDKN1A, CXCR4 and negative control region by NCOR in SUDHL4 cells exposed to 5 μM WK692 for 24 h. (*, P < 0.05 versus control)
Supplementary Data from Zelenirstat Inhibits N-Myristoyltransferases to Disrupt Src Family Kinase Signaling and Oxidative Phosphorylation, Killing Acute Myeloid Leukemia Cells
Authors: Gamma Jay M. , Liu Qiang , Beauchamp Erwan , Iyer Aishwarya , Yap Megan C. , Zak Zoulika , Ekstrom Cassidy , Pain Rony , Kostiuk Morris A. , Mackey John R. , Brandwein Joseph , Wang Jean C.Y. , Berthiaume Luc G.
Published: January 2025

Table of Materials
Supplemental Figure 1 from Tumor-Specific Antigen Delivery for T-cell Therapy via a pH-Sensitive Peptide Conjugate
Authors: Yurkevicz Annali M. , Liu Yanfeng , Katz Samuel G. , Glazer Peter M.
Published: January 2025

Cysteine addition to SIINFEKL does not impact T cell recognition, but S to E substitution abrogates recognition. Assay for engagement of OT1 T cells with B16-F10 melanoma cells electroporated with SIINFEKL-related peptides. Peptides were electroporated into B16-F10 cells which were subsequently co-cultured with far-red fluorescently dyed OT1 T cells at a 10:1 effector:target cell ratio for 2 h, followed by washing and visualization by fluorescent microscopy. B16-F10 cells were stained by DAPI. Peptides tested were the parental SIINFEKL (the naturally occurring sequence from ovalbumin), CSIINFEKL which contains the addition of an N-terminal cysteine, EIINFEKL, which has glutamic acid (E) substituted for serine (S), and CEIINFEKL with both an Nterminal cysteine and a glutamic acid substitution for serine.
Figure S14 from Zelenirstat Inhibits N-Myristoyltransferases to Disrupt Src Family Kinase Signaling and Oxidative Phosphorylation, Killing Acute Myeloid Leukemia Cells
Authors: Gamma Jay M. , Liu Qiang , Beauchamp Erwan , Iyer Aishwarya , Yap Megan C. , Zak Zoulika , Ekstrom Cassidy , Pain Rony , Kostiuk Morris A. , Mackey John R. , Brandwein Joseph , Wang Jean C.Y. , Berthiaume Luc G.
Published: January 2025

Supplementary Figure S14: Zelenirstat shows promising synergy with venetoclax. AML cell lines were screened for synergy between zelenirstat and venetoclax using Horizon’s Combination Profiling platform. Isobolograms of (A) MV-4-11 and (B) KG-1 cell lines of zelenirstat and venetoclax combination therapy. Trendlines below additivity line indicate synergy. (C) Synergy scores of AML cell lines in combination with venetoclax. Synergy scores indicate growth inhibition in excess of additive effects.
Figure S13 from Zelenirstat Inhibits N-Myristoyltransferases to Disrupt Src Family Kinase Signaling and Oxidative Phosphorylation, Killing Acute Myeloid Leukemia Cells
Authors: Gamma Jay M. , Liu Qiang , Beauchamp Erwan , Iyer Aishwarya , Yap Megan C. , Zak Zoulika , Ekstrom Cassidy , Pain Rony , Kostiuk Morris A. , Mackey John R. , Brandwein Joseph , Wang Jean C.Y. , Berthiaume Luc G.
Published: January 2025

Supplementary Figure S13: Zelenirstat reduces AMPKβ. AML cell lines were treated with zelenirstat for 48 hours, then stimulated with 100 nL/mL SCF & FL, then levels of AMPKβ analyzed by western blot. Band intensity was determined using Image Studio Lite, and each sample normalized to actin. Differences between treatment groups determined using one-way ANOVA.
Supplementary Figure 3 from Riluzole Enhancing Anti-PD-1 Efficacy by Activating cGAS/STING Signaling in Colorectal Cancer
Authors: Liang Beiyuan , Khan Misbah , Storts Hayden , Zhang Evan H. , Zheng Xinru , Xing Xuanxuan , Claybon Hazel , Wilson Jenna , Li Chunjie , Jin Ning , Fishel Richard , Miles Wayne O. , Wang Jing J.
Published: January 2025

Supplemental figure 3 and legend
Table S1 from Advances and Challenges in RAS Signaling Targeted Therapy in Leukemia
Authors: Chen Yu , Yin Zhenghao , Westover Kenneth D. , Zhou Zhiwei , Shu Liping
Published: January 2025

Table S1. NRAS mutations in leukemia
Supplementary Table S9 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Table S9. Organ biodistribution analysis data in %ID/Organ tissue for 89Zr labeled nanocarriers at 96 h in mice model bearing CT26 subcutaneous tumors. (n = 5)
Supplementary Table S6 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Table S6. Organ biodistribution analysis data in %ID/g tissue for 89Zr labeled nanocarriers at 96 h in mice model bearing 22rv1 subcutaneous tumors. (n = 4)
Supplementary Table S3 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Table S3. Organ biodistribution data in %ID/Organ tissue for [89Zr]PEG-DFB1-TLZ3 at 72 h in mice model bearing different subcutaneous tumors. (n = 4)
Supplementary Table S11 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Table S11. Organ biodistribution analysis data in %ID/Organ tissue for 89Zr labeled nanocarriers at 96 h in mice model bearing LTL-545 subcutaneous tumors. (n = 4)
Supplementary Table S10 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Table S10. Organ biodistribution analysis data in %ID/g tissue for 89Zr labeled nanocarriers at 96 h in mice model bearing LTL-545 subcutaneous tumors. (n = 4)
Supplementary Figure S8 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S8. Organ biodistribution presented in (left) %ID/g, and (right) %ID/organ for 89Zr labeled nanocarriers in nude mice bearing 22rv1 subcutaneous tumors at 96 h postinjection. (n = 4, mean ± SD)
Supplementary Figure S5 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S5. Coronal μPET/CT fusion and MIP images obtained at 24 h, 48 h, 72 h, and 96 h following administration of 150-170 μCi of 89Zr labeled nanocarriers in nude mice bearing CT26 subcutaneous tumors over left flanks.
Supplementary Figure S22 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S22. BLI of all mice in the cohort inoculated with 22rv1-Luc cells in the left kidney capsule that demonstrate prominent signal of metastatic tumors at the neck and thigh region on the day of 89Zr labeled nanocarrier injection.
Supplementary Figure S2 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S2. Pilot PET/CT studies in prostate, pancreatic, and colorectal cancer models to measure the enhanced permeability retention effect using [89Zr]PEG-DFB1-TLZ3.
Supplementary Table 2 from Targeting Tumor Antigen 5T4 Using CAR T Cells for the Treatment of Acute Myeloid Leukemia
Authors: Harrop Richard , Blount Daniel G. , Khan Naeem , Soyombo Mayowa , Moyce Laura , Drayson Mark T. , Down Jenny , Lawson Michelle A. , O’Connor Deirdre , Nimmo Rachael , Lad Yatish , Souberbielle Bernard , Mitrophanous Kyriacos , Ettorre Anna
Published: January 2025

Supplementary Table 2: 5T4 Expression in AML Cell Lines
Supplementary Figure S15 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S15. Autoradiographic images of PDX LTL-610 tumor sections from day 1 to day 3 post injection of 89Zr labeled nanocarriers. H&E staining images of the respective timepoints are not available.
Supplementary Figure S14 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S14. Autoradiographic images and H&E staining images of PDX LTL-545 tumor sections from day 1 to day 4 post injection of 89Zr labeled nanocarriers.
Supplementary Figure S13 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S13. Autoradiographic images and H&E staining images of subcutaneous CT26 tumor sections from day 1 to day 4 post injection of 89Zr labeled nanocarriers. *Indicate the presence of necrosis.
Supplementary Figure 2 from Targeting Tumor Antigen 5T4 Using CAR T Cells for the Treatment of Acute Myeloid Leukemia
Authors: Harrop Richard , Blount Daniel G. , Khan Naeem , Soyombo Mayowa , Moyce Laura , Drayson Mark T. , Down Jenny , Lawson Michelle A. , O’Connor Deirdre , Nimmo Rachael , Lad Yatish , Souberbielle Bernard , Mitrophanous Kyriacos , Ettorre Anna
Published: January 2025

Supplementary Figure 2. Schematic representation and sequence of 5T4 construct
Supplementary Figure S11 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S11. Organ biodistribution presented in (left) %ID/g, and (right) %ID/organ for 89Zr labeled nanocarriers in nude mice bearing LTL-610 patient derived xenograft (PDX) of tumors at 96 h postinjection. (n = 4, mean ± SD)
Supplementary Figure S10 from PET Imaging Using 89Zr-Labeled StarPEG Nanocarriers Reveals Heterogeneous Enhanced Permeability and Retention in Prostate Cancer
Authors: Meher Niranjan , Bidkar Anil P. , Wadhwa Anju , Bobba Kondapa Naidu , Dhrona Suchi , Dasari Chandrashekhar , Mu Changhua , Fong Cyril O.Y. , Cámara Juan A. , Ali Umama , Basak Megha , Bulkley David , Steri Veronica , Fontaine Shaun D. , Zhu Jun , Oskowitz Adam , Aggarwal Rahul R. , Sriram Renuka , Chou Jonathan , Wilson David M. , Seo Youngho , Santi Daniel V. , Ashley Gary W. , VanBrocklin Henry F. , Flavell Robert R.
Published: January 2025

Supplementary Figure S10. Organ biodistribution presented in (left) %ID/g, and (right) %ID/organ for 89Zr labeled nanocarriers in nude mice bearing LTL-545 patient derived xenograft (PDX) of tumors at 96 h postinjection. (n = 4, mean ± SD)
Table S1 from Tumor Integrin-Targeted Glucose Oxidase Enzyme Promotes ROS-Mediated Cell Death that Combines with Interferon Alpha Therapy for Tumor Control
Authors: Stinson Jordan A. , Sheen Allison , Lax Brianna M. , Yang Grace N. , Duhamel Lauren , Santollani Luciano , Fink Elizabeth , Palmeri Joseph R. , Wittrup Karl Dane
Published: January 2025

Protein sequences
Figure S6 from Tumor Integrin-Targeted Glucose Oxidase Enzyme Promotes ROS-Mediated Cell Death that Combines with Interferon Alpha Therapy for Tumor Control
Authors: Stinson Jordan A. , Sheen Allison , Lax Brianna M. , Yang Grace N. , Duhamel Lauren , Santollani Luciano , Fink Elizabeth , Palmeri Joseph R. , Wittrup Karl Dane
Published: January 2025

Additional flow analysis of 2.5F-GOX dose escalation study
Figure S5 from Tumor Integrin-Targeted Glucose Oxidase Enzyme Promotes ROS-Mediated Cell Death that Combines with Interferon Alpha Therapy for Tumor Control
Authors: Stinson Jordan A. , Sheen Allison , Lax Brianna M. , Yang Grace N. , Duhamel Lauren , Santollani Luciano , Fink Elizabeth , Palmeri Joseph R. , Wittrup Karl Dane
Published: January 2025

Cross-presentation assay myeloid cell gating strategy
Figure S2 from Tumor Integrin-Targeted Glucose Oxidase Enzyme Promotes ROS-Mediated Cell Death that Combines with Interferon Alpha Therapy for Tumor Control
Authors: Stinson Jordan A. , Sheen Allison , Lax Brianna M. , Yang Grace N. , Duhamel Lauren , Santollani Luciano , Fink Elizabeth , Palmeri Joseph R. , Wittrup Karl Dane
Published: January 2025

Bolus hydrogen peroxide is cytotoxic but rapidly cleared by cancer cells
Figure S1 from Tumor Integrin-Targeted Glucose Oxidase Enzyme Promotes ROS-Mediated Cell Death that Combines with Interferon Alpha Therapy for Tumor Control
Authors: Stinson Jordan A. , Sheen Allison , Lax Brianna M. , Yang Grace N. , Duhamel Lauren , Santollani Luciano , Fink Elizabeth , Palmeri Joseph R. , Wittrup Karl Dane
Published: January 2025

Characterization of recombinant glucose oxidase fusions
Data from A Novel Lipid Nanoparticle NBF-006 Encapsulating Glutathione S-Transferase P siRNA for the Treatment of KRAS-Driven Non–small Cell Lung Cancer
Authors: Cina Cima , Majeti Bharat , O’Brien Zhihong , Wang Li , Clamme Jean Pierre , Adami Roger , Tsang Kwok Yin , Harborth Jens , Ying Wenbin , Zabludoff Sonya
Published: January 2025

Abstract
Non–small cell lung cancer (NSCLC) accounts for approximately 85% of lung cancers, and KRAS mutations occur in 25% to 30% of NSCLC. Our approach to developing a therapeutic with the potential to target KRAS-mutant NSCLC was to identify a new target involved in modulating signaling proteins in the RAS pathway. Glutathione S-transferase P (GSTP), known as a phase II detoxification enzyme, has more recently been identified as a modulator of MAPK-related cell signaling pathways. Therefore, developing a GSTP siRNA may be an effective therapeutic approach to treat KRAS-mutant NSCLC. The lead drug product candidate (NBF-006) is a proprietary siRNA-based lipid nanoparticle comprising GSTP siRNA (NDT-05-1040). Here, studies using a panel of KRAS-mutant NSCLC cell lines demonstrated that NDT-05-1040 is a very potent and selective GSTP siRNA inhibitor. Our Western blot analysis showed that NDT-05-1040 effectively decreased the phosphorylation of MAPK and PI3K pathway components while upregulating apoptotic signaling cascade. Our in vivo studies revealed statistically significant higher distribution of NBF-006 to the lungs and tumor as compared with the liver. In the subcutaneous and orthotopic tumor models, NBF-006 led to a statistically significant and dose-dependent antitumor growth inhibition. Furthermore, quantitative image analysis of proliferating cell nuclear antigen and PARP staining showed that NBF-006 decreased proliferation and induced apoptosis, respectively, in tumors. Additionally, in a surgically implanted orthotopic lung tumor model, the survival rate of the NBF-006 treatment group was significantly prolonged (P < 0.005) as compared with the vehicle control group. Together, these preclinical studies supported advancement of NBF-006 into clinical studies.
Data from Tumor-Specific Antigen Delivery for T-cell Therapy via a pH-Sensitive Peptide Conjugate
Authors: Yurkevicz Annali M. , Liu Yanfeng , Katz Samuel G. , Glazer Peter M.
Published: January 2025

Abstract
Identifying an optimal antigen for targeted cancer therapy is challenging as the antigen landscape on cancerous tissues mimics that of healthy tissues, with few unique tumor-specific antigens identified in individual patients. pH low insertion peptide (pHLIP) acts as a unique delivery platform that can specifically target the acidic microenvironment of tumors, sparing healthy tissue in the process. We developed a pHLIP-peptide conjugate to deliver the SIINFEKL peptide, an immunogenic fragment of ovalbumin (OVA), to tumor cells in vivo. When processed intracellularly, SIINFEKL is presented for immune recognition through the major histocompatibility complex (MHC) class I pathway. We observed selective delivery of pHLIP-SIINFEKL both in vitro and in vivo using fluorescently labeled constructs. In vitro, treatment of melanoma tumor cells with pHLIP-SIINFEKL resulted in recognition by SIINFEKL-specific T cells (OT1), leading to T-cell activation and effector function. Mechanistically, we show that this recognition by OT1 T cells was abrogated by siRNA/shRNA knockdown of multiple components within the MHC class I pathway in the target tumor cells, indicating that an intact antigen processing pathway in the cancer cells is necessary to mediate the effect of pHLIP-directed SIINFEKL delivery. In vivo, pHLIP-SIINFEKL treatment of tumor-bearing mice resulted in the recruitment of OT1 T cells and suppression of tumor growth in two syngeneic tumor models in immunocompetent mice, with no effect when mutating either the pHLIP or SIINFEKL components of the conjugate. These results suggest that pHLIP-mediated peptide delivery can be used to deliver novel artificial antigens that can be targeted by cell-based therapies.