bluuebunny/crossref_metadata_2025 huggingface dataset:
Figure S1-S11 and Table S1-S4 from Identification of the Novel Role of CD24 as an Oncogenesis Regulator and Therapeutic Target for Triple-Negative Breast Cancer
Authors: Chan Shih-Hsuan , Tsai Kuo-Wang , Chiu Shu-Yi , Kuo Wen-Hung , Chen Heng-Yi , Jiang Shih Sheng , Chang King-Jen , Hung Wen-Chun , Wang Lu-Hai
Published: April 2023

Establishment of breast cancer cells derived from the long-term lung metastatic nodules in a xenograft mouse model (Figure S1). LC cells display strong lymph node-tropic metastasis and tumorigenicity in an orthotopic mouse model (Figure S2). Inhibition of CD24 impairs the ability of in vitro anchorage-independent growth and cell proliferation in CD24-expressing TNBC cell lines (Figure S3). Effect of inhibition of CD24 on luminal breast cancer cell line MCF-7 (Figure S4). CD24-depleted IV2 cells failed to colonize in the lung of SCID mice (Figure S5). CD24 depletion did not alter initial lung targeting of IV2 cells (Figure S6). Ectopic expression of CD24 in 231 cells promotes primary tumor growth and lymphangiogensis/angiogenesis (Figure S7). Depletion of CD24 impairs lymphangiogenesis and angiogenesis via downregulation of VEGF-C and -A (Figure S8). HGF- and EGF-induced VEGF-A and -C expression in TNBC cell lines (Figure S9). Treatment of CD24 mAb reduced lung colonization of MDA-MB-468 in a tail vein injection mouse model (Figure S10). Analysis of clinical correlation between CD24 and EGFR/Met protein expression in 133 TNBC specimens using IHC staining (Figure S11) Cox proportional regression analysis of the influence of CD24 level on 5-year survival of breast cancer patients with different subtypes (Table S1). Cox proportional regression analysis of the influence of CD24 level on recurrence of BC patients in Ma dataset (Table S2). All antibodies and reagents used in this study (Table S3). Primers, oligos and plasmids used in this study (Table S4).
Table S4 from Theranostic Radiolabeled Anti-CD20 sdAb for Targeted Radionuclide Therapy of Non-Hodgkin Lymphoma
Authors: Krasniqi Ahmet , D'Huyvetter Matthias , Xavier Catarina , Van der Jeught Kevin , Muyldermans Serge , Van Der Heyden José , Lahoutte Tony , Tavernier Jan , Devoogdt Nick
Published: April 2023

Ex vivo biodistribution of 177Lu-DTPA-sdAb 9077, 9079 and non-target control sdAb (177Lu-DTPA-ctrl sdAb) at 1.5 h p.i., co-infused with 150 mg/kg Gelofusin, in hCD20 B16 tumor mouse model. Results are presented as mean % IA/g {plus minus} SD (n = 3 per sdAb). T/M: Tumor-to-Muscle ratio; T/B: Tumor- to-Blood ratio.
Figure S6 from ALK Inhibitor Response in Melanomas Expressing EML4-ALK Fusions and Alternate ALK Isoforms
Authors: Couts Kasey L. , Bemis Judson , Turner Jacqueline A. , Bagby Stacey M. , Murphy Danielle , Christiansen Jason , Hintzsche Jennifer D. , Le Anh , Pitts Todd M. , Wells Keith , Applegate Allison , Amato Carol , Multani Pratik , Chow-Maneval Edna , Tentler John J. , Shellman Yiqun G. , Rioth Matthew J. , Tan Aik-Choon , Gonzalez Rene , Medina Theresa , Doebele Robert C. , Robinson William A.
Published: April 2023

siRNA knockdown of ALKATI
Figure S2 from ALK Inhibitor Response in Melanomas Expressing EML4-ALK Fusions and Alternate ALK Isoforms
Authors: Couts Kasey L. , Bemis Judson , Turner Jacqueline A. , Bagby Stacey M. , Murphy Danielle , Christiansen Jason , Hintzsche Jennifer D. , Le Anh , Pitts Todd M. , Wells Keith , Applegate Allison , Amato Carol , Multani Pratik , Chow-Maneval Edna , Tentler John J. , Shellman Yiqun G. , Rioth Matthew J. , Tan Aik-Choon , Gonzalez Rene , Medina Theresa , Doebele Robert C. , Robinson William A.
Published: April 2023

Characterization of EML4-ALK fusion variants in MB 2141
Supplementary Table S5 from Combinatorial Screening of Pancreatic Adenocarcinoma Reveals Sensitivity to Drug Combinations Including Bromodomain Inhibitor Plus Neddylation Inhibitor
Authors: Langdon Casey G. , Platt James T. , Means Robert E. , Iyidogan Pinar , Mamillapalli Ramanaiah , Klein Michael , Held Matthew A. , Lee Jong Woo , Koo Ja Seok , Hatzis Christos , Hochster Howard S. , Stern David F.
Published: April 2023

Isobologram synergy analysis
Supplementary Table S3 from Combinatorial Screening of Pancreatic Adenocarcinoma Reveals Sensitivity to Drug Combinations Including Bromodomain Inhibitor Plus Neddylation Inhibitor
Authors: Langdon Casey G. , Platt James T. , Means Robert E. , Iyidogan Pinar , Mamillapalli Ramanaiah , Klein Michael , Held Matthew A. , Lee Jong Woo , Koo Ja Seok , Hatzis Christos , Hochster Howard S. , Stern David F.
Published: April 2023

Average AUC by target category
Supplemental Data from PPARγ Ligand–induced Annexin A1 Expression Determines Chemotherapy Response via Deubiquitination of Death Domain Kinase RIP in Triple-negative Breast Cancers
Authors: Chen Luxi , Yuan Yi , Kar Shreya , Kanchi Madhu M. , Arora Suruchi , Kim Ji E. , Koh Pei F. , Yousef Einas , Samy Ramar P. , Shanmugam Muthu K. , Tan Tuan Z. , Shin Sung W. , Arfuso Frank , Shen Han M. , Yang Henry , Goh Boon C. , Park Joo I. , Gaboury Louis , Lobie Peter E. , Sethi Gautam , Lim Lina H.K. , Kumar Alan P.
Published: April 2023

Supplementary methods and supplementary figure legends
Supplementary Data from Covalent Targeting of Fibroblast Growth Factor Receptor Inhibits Metastatic Breast Cancer
Authors: Brown Wells S. , Tan Li , Smith Andrew , Gray Nathanael S. , Wendt Michael K.
Published: April 2023

This file includes supplementary figures S1-S8 and supplementary tables S1-S3.
Supplemental Figure 1 from Clinical Dosing Regimen of Selinexor Maintains Normal Immune Homeostasis and T-cell Effector Function in Mice: Implications for Combination with Immunotherapy
Authors: Tyler Paul M. , Servos Mariah M. , de Vries Romy C. , Klebanov Boris , Kashyap Trinayan , Sacham Sharon , Landesman Yosef , Dougan Michael , Dougan Stephanie K.
Published: April 2023

Supplemental Figure 1: Response to immunization is only modestly affected by selinexor.
Supplementary Data from Synergy between EphA2-ILs-DTXp, a Novel EphA2-Targeted Nanoliposomal Taxane, and PD-1 Inhibitors in Preclinical Tumor Models
Authors: Kamoun Walid S. , Dugast Anne-Sophie , Suchy James J. , Grabow Stephanie , Fulton Ross B. , Sampson James F. , Luus Lia , Santiago Michael , Koshkaryev Alexander , Sun Gang , Askoxylakis Vasileios , Tam Eric , Huang Zhaohua Richard , Drummond Daryl C. , Sawyer Andrew J.
Published: April 2023

Supplemental figures 1, 2, and 3 and supplemental tables 1 and 2, showing the antitumor activity of EphA2-ILS-DTXp and the pharmacokinetics in multiple murine tumor models.
Supplementary Figure 2 from Inhibition of the Replication Stress Response Is a Synthetic Vulnerability in SCLC That Acts Synergistically in Combination with Cisplatin
Authors: Nagel Remco , Avelar Ana Teresa , Aben Nanne , Proost Natalie , van de Ven Marieke , van der Vliet Jan , Cozijnsen Miranda , de Vries Hilda , Wessels Lodewyk F. A. , Berns Anton
Published: April 2023

Supplementary figure 2. Graphs showing the correlation between all three replicates of the genomeâ€�wide CRISPRâ€�Cas9 screen at the start of the experiment (t=0) and at the final time point (t=14).
Supplementary figures from The FA/BRCA Pathway Identified as the Major Predictor of Cisplatin Response in Head and Neck Cancer by Functional Genomics
Authors: Martens-de Kemp Sanne R. , Brink Arjen , van der Meulen Ida H. , de Menezes Renée X. , te Beest Dennis E. , Leemans C. René , van Beusechem Victor W. , Braakhuis Boudewijn J.M. , Brakenhoff Ruud H.
Published: April 2023

Supplementary figures S1-S4
Supplementary Tables from Carbonic Anhydrase XII Inhibitors Overcome P-Glycoprotein–Mediated Resistance to Temozolomide in Glioblastoma
Authors: Salaroglio Iris C. , Mujumdar Prashant , Annovazzi Laura , Kopecka Joanna , Mellai Marta , Schiffer Davide , Poulsen Sally-Ann , Riganti Chiara
Published: April 2023

The file contains Supplementary Tables S1-S5. Table S1 reports cell phenotypic characterization; Table S2 reports CA Ki of compounds; Table S3 reports plasma and microsomal stability of compound 1; Table S4 reports cytochrome metabolism activity on compound 1; Table S5 reports the hematochemical parameters of the treated animals.
Supplementary Figure S1 from Highly Potent, Anthracycline-based Antibody–Drug Conjugates Generated by Enzymatic, Site-specific Conjugation
Authors: Stefan Nikolas , Gébleux Rémy , Waldmeier Lorenz , Hell Tamara , Escher Marie , Wolter Fabian I. , Grawunder Ulf , Beerli Roger R.
Published: April 2023

Effect of IgG pre-treatment on the in vivo half-life of ADCs in immunodeficient mice.
Supplemental Figure 1 from Therapeutic Impact of Nanoparticle Therapy Targeting Tumor-Associated Macrophages
Authors: Penn Courtney A. , Yang Kun , Zong Hong , Lim Jae-Young , Cole Alex , Yang Dongli , Baker James , Goonewardena Sascha N. , Buckanovich Ronald J.
Published: April 2023

NP synthesis QA
Supporting Video 03 from Is the Fate of Clinical Candidate Arry-520 Already Sealed? Predicting Resistance in Eg5–Inhibitor Complexes
Authors: Indorato Rose-Laure , Talapatra Sandeep K. , Lin Fangzhu , Haider Shozeb , Mackay Simon P. , Kozielski Frank , Skoufias Dimitrios A.
Published: April 2023

Time lapse imaging of U2OS-Eg5(D130A) expressing cells exposed to 10 nM Arry-520 and followed for 16 h. Cells divide uninhibited.
Figure S1 from CRISPR Genome-Wide Screening Identifies Dependence on the Proteasome Subunit PSMC6 for Bortezomib Sensitivity in Multiple Myeloma
Authors: Shi Chang-Xin , Kortüm K. Martin , Zhu Yuan Xiao , Bruins Laura A. , Jedlowski Patrick , Votruba Patrick G. , Luo Moulun , Stewart Robert A. , Ahmann Jonathan , Braggio Esteban , Stewart A. Keith
Published: April 2023

A. Cloned RPMI8226 cells with deleted PSMC6 also developed resistance to carfilzomib.B&C. Cloned KMS11 cells with deleted PSMC6 developed resistance to BTZ.
Supplementary Movie legend from Aggressive Progression in Glioblastoma Cells through Potentiated Activation of Integrin α5β1 by the Tenascin-C–Derived Peptide TNIIIA2
Authors: Fujita Motomichi , Yamamoto Tetsuya , Iyoda Takuya , Fujisawa Tatsuya , Sasada Manabu , Nagai Reo , Kudo Chikako , Otsuka Kazuki , Kamiya Sadahiro , Kodama Hiroaki , Fukai Fumio
Published: April 2023

This file shows the legends of Supplementary Movie S1-S3.
Supplementary Figure S2 from Eribulin Suppresses Clear Cell Sarcoma Growth by Inhibiting Cell Proliferation and Inducing Melanocytic Differentiation Both Directly and Via Vascular Remodeling
Authors: Nakai Sho , Tamiya Hironari , Imura Yoshinori , Nakai Takaaki , Yasuda Naohiro , Wakamatsu Toru , Tanaka Takaaki , Outani Hidetatsu , Takenaka Satoshi , Hamada Kenichiro , Myoui Akira , Araki Nobuhito , Ueda Takafumi , Yoshikawa Hideki , Naka Norifumi
Published: April 2023

Supplementary Figure S2 shows measurement of melanin content and WST-1 cell proliferation assay in Hewga-CCS and MP-CCS-SY cells treated with SCH772984.
Supplementary Figure 1 from Dimethyl Fumarate Controls the NRF2/DJ-1 Axis in Cancer Cells: Therapeutic Applications
Authors: Saidu Nathaniel Edward Bennett , Noé Gaëlle , Cerles Olivier , Cabel Luc , Kavian-Tessler Niloufar , Chouzenoux Sandrine , Bahuaud Mathilde , Chéreau Christiane , Nicco Carole , Leroy Karen , Borghese Bruno , Goldwasser François , Batteux Frédéric , Alexandre Jérôme
Published: April 2023

Supplementary figure showing that high concentrations of DMF display cytotoxicity in several cancer cell lines
Tables and Methods from Preclinical Efficacy and Safety Comparison of CD3 Bispecific and ADC Modalities Targeting BCMA for the Treatment of Multiple Myeloma
Authors: Panowski Siler H. , Kuo Tracy C. , Zhang Yi , Chen Amy , Geng Tao , Aschenbrenner Laura , Kamperschroer Cris , Pascua Edward , Chen Wei , Delaria Kathy , Farias Santiago , Bateman Marjorie , Dushin Russell G. , Chin Sherman M. , Van Blarcom Thomas J. , Yeung Yik Andy , Lindquist Kevin C. , Chunyk Allison G. , Kuang Bing , Han Bora , Mirsky Michael , Pardo Ingrid , Buetow Bernard , Martin Thomas G. , Wolf Jeffrey L. , Shelton David , Rajpal Arvind , Strop Pavel , Chaparro-Riggers Javier , Sasu Barbra J.
Published: April 2023

Tables show PK kinetics, plasma cell numbers, and patient data. Methods include all supplemental methods.
Supplementary Figure S1 from Glibenclamide Targets Sulfonylurea Receptor 1 to Inhibit p70S6K Activity and Upregulate KLF4 Expression to Suppress Non-Small Cell Lung Carcinoma
Authors: Xu Kexin , Sun Geng , Li Min , Chen Hongling , Zhang Zuhao , Qian Xixi , Li Ping , Xu Lin , Huang Wenbin , Wang Xuerong
Published: April 2023

Supplementary Figure S1 shows the expression and survival correlation of Kir6.1 and Kir6.2 in NSCLC.
Supplemental Figure 7 from Nanoparticle-Based Celecoxib and Plumbagin for the Synergistic Treatment of Melanoma
Authors: Gowda Raghavendra , Kardos Gregory , Sharma Arati , Singh Sanjay , Robertson Gavin P.
Published: April 2023

Supplemental Figure 7. No significant change in TUNEL positive apoptotic cells occurred in CelePlum-777 treated tumors compared to controls.
Supplementary Tables 1-2 and Supplementary Figures 1-3 from MET Copy Number Gain Is Associated with Gefitinib Resistance in Leptomeningeal Carcinomatosis of EGFR-mutant Lung Cancer
Authors: Nanjo Shigeki , Arai Sachiko , Wang Wei , Takeuchi Shinji , Yamada Tadaaki , Hata Akito , Katakami Nobuyuki , Okada Yasunori , Yano Seiji
Published: April 2023

Supplementary Table 1: Patient characteristics; Supplementary Table 2: Primers for amplifying MET gene; Supplementary Figure 1: PC-9/LMC-GR did not express HGF or possess MET mutations; Supplementary Figure 2: Acquired gefitinib resistance of HCC827/luc cells in LMC model was associated with MET copy number gain; Supplementary Figure 3: Subcutaneous tumors with PC-9/LMC-GR cells are sensitive to gefitinib treatment.
Figure S2 from Itraconazole-Induced Inhibition on Human Esophageal Cancer Cell Growth Requires AMPK Activation
Authors: Chen Min-Bin , Liu Yuan-Yuan , Xing Zhao-Yu , Zhang Zhi-Qing , Jiang Qin , Lu Pei-Hua , Cao Cong
Published: April 2023

Figure S2. TE-1 cells, expressing AMPKÎ±1 shRNA ("sh-AMPKÎ±1") or scramble control shRNA ("shRNA-Ctrl"), as well as the parental control TE-1 cells ("No shRNA"), were treated with itraconazole ("Itra", 3.0 Î¼g/mL) for indicated time, and were tested by Western blot of listed proteins (A and B); Cell viability (MTT assay, C) and cell death (trypan blue staining assay, D) were tested. The primary human esophageal cancer cells ("Primary cancer cells") or HEEC esophageal epithelial cells were treated with/without itraconazole ("Itra", 3.0 Î¼g/mL) for applied time, and were tested of listed proteins (E-G). Notably, RTKs (EGFR, PDGFRÎ± and PDGFRÎ²) expression and Akt activation were low in HEEC cells. # P < 0.05 vs. group "shRNA-Ctrl".
Figure S7 from RAC1b Overexpression Confers Resistance to Chemotherapy Treatment in Colorectal Cancer
Authors: Goka Erik T. , Chaturvedi Pallavi , Lopez Dayrelis T. Mesa , Garza Adriana De La , Lippman Marc E.
Published: April 2023

Figure S7. HCT116 cells were treated with Oxaliplatin (5 Î¼M) and GYS32661 (25 Î¼M) and the combination of two, stimulated with TNFÎ± for 10 mins. 50 Î¼g of protein was resolved on SDS-PAGE gel, transferred on the nitrocellulose member. The membrane was probed with phosho IÎºÎ'Î±, total IÎºÎ'Î±, and phospho P65 antibodies
Figure S4 from RAC1b Overexpression Confers Resistance to Chemotherapy Treatment in Colorectal Cancer
Authors: Goka Erik T. , Chaturvedi Pallavi , Lopez Dayrelis T. Mesa , Garza Adriana De La , Lippman Marc E.
Published: April 2023

Figure S4. 1,000 HT29 NSC and shRac1b cells were plated in a 96-well plate and treated with different doses of 5FU for 10 days. On day 10, cell viability was analyzed using the PrestoBlue reagent according to the manufacturers instructions. Data was graphed using GraphPad software and IC50 values were generated using the log(inhibitor) vs. response - variable slope function. Data represents quadruplicates and the error bars represent the 95% confidence intervals.
Supplementary Data from Immunotherapy with Immunocytokines and PD-1 Blockade Enhances the Anticancer Activity of Small Molecule-Drug Conjugates Targeting Carbonic Anhydrase IX
Authors: Millul Jacopo , Krudewig Christiane , Zana Aureliano , Dakhel Plaza Sheila , Puca Emanuele , Villa Alessandra , Neri Dario , Cazzamalli Samuele
Published: April 2023

Supplementary material: chemical synthesis and biological characterisation
Supplementary Data Figure S1-S8 from A Genome-scale CRISPR Screen Identifies the ERBB and mTOR Signaling Networks as Key Determinants of Response to PI3K Inhibition in Pancreatic Cancer
Authors: Milton Charlotte K. , Self Annette J. , Clarke Paul A. , Banerji Udai , Piccioni Federica , Root David E. , Whittaker Steven R.
Published: April 2023

Figure S1. KRAS-dependency and effect of Cas9 expression on response to PI3K inhibition. Figure S2. Whole-genome CRISPR screen shows good replicate correlation and identifies enhancers and suppressors of GDC0941 antiproliferative activity. Figure S3. Expression of Cas9 does not alter response to BYL719 or GDC0941. Figure S4. Population doublings, replicate correlation and alternative analysis of the minipool screen. Figure S5. PI3K signalling is reduced following serum starvation. Figure S6. Combined inhibition of PI3K and mTOR results in potent antiproliferative activity in pancreatic cancer cell lines. Figure S7. Combined p110ï�¡ and mTOR or ERBB-family inhibition leads to sustained suppression of S6 phosphorylation. Figure S8. CRISPR and drug combination screens implicate the ERBB-PI3K-MTOR signalling axis as a key vulnerability of pancreatic cancer cells.
Supplementary Table S1 from A Pilot Study of Galunisertib plus Stereotactic Body Radiotherapy in Patients with Advanced Hepatocellular Carcinoma
Authors: Reiss Kim A. , Wattenberg Max M. , Damjanov Nevena , Prechtel Dunphy Elizabeth , Jacobs-Small Mona , Lubas M. Judy , Robinson James , Dicicco Lisa , Garcia-Marcano Luis , Giannone Michael A. , Karasic Thomas B. , Furth Emma E. , Carpenter Erica L. , Wojcieszynski Andrzej P. , Vonderheide Robert H. , Beatty Gregory L. , Ben-Josef Edgar
Published: April 2023

Metal Conjugated Antibodies for Mass Cytometry Analysis
Supplementary Figure S5 from A Pilot Study of Galunisertib plus Stereotactic Body Radiotherapy in Patients with Advanced Hepatocellular Carcinoma
Authors: Reiss Kim A. , Wattenberg Max M. , Damjanov Nevena , Prechtel Dunphy Elizabeth , Jacobs-Small Mona , Lubas M. Judy , Robinson James , Dicicco Lisa , Garcia-Marcano Luis , Giannone Michael A. , Karasic Thomas B. , Furth Emma E. , Carpenter Erica L. , Wojcieszynski Andrzej P. , Vonderheide Robert H. , Beatty Gregory L. , Ben-Josef Edgar
Published: April 2023

Gating strategy
Supplementary Methods from Single-Dose Anti–PD-L1/IL-15 Fusion Protein KD033 Generates Synergistic Antitumor Immunity with Robust Tumor-Immune Gene Signatures and Memory Responses
Authors: Martomo Stella A. , Lu Dan , Polonskaya Zhanna , Luna Xenia , Zhang Zhikai , Feldstein Sam , Lumban-Tobing Radovan , Almstead Danielle K. , Miyara Faical , Patel Jeegar
Published: April 2023

Detailed Methods for in vitro and in vivo Studies
Supplementary Figure 2 from Single-Dose Anti–PD-L1/IL-15 Fusion Protein KD033 Generates Synergistic Antitumor Immunity with Robust Tumor-Immune Gene Signatures and Memory Responses
Authors: Martomo Stella A. , Lu Dan , Polonskaya Zhanna , Luna Xenia , Zhang Zhikai , Feldstein Sam , Lumban-Tobing Radovan , Almstead Danielle K. , Miyara Faical , Patel Jeegar
Published: April 2023

Animal Study Designs and Additional Animal Study Data
Figure S4 from SLC7A11 Is a Superior Determinant of APR-246 (Eprenetapopt) Response than TP53 Mutation Status
Authors: Fujihara Kenji M. , Corrales Benitez Mariana , Cabalag Carlos S. , Zhang Bonnie Z. , Ko Hyun S. , Liu David S. , Simpson Kaylene J. , Haupt Ygal , Lipton Lara , Haupt Sue , Phillips Wayne A. , Clemons Nicholas J.
Published: April 2023

Figure S4 shows the effects of p53 overexpression and repression on SLC7A11 mRNA expression.
Figure S2 from SLC7A11 Is a Superior Determinant of APR-246 (Eprenetapopt) Response than TP53 Mutation Status
Authors: Fujihara Kenji M. , Corrales Benitez Mariana , Cabalag Carlos S. , Zhang Bonnie Z. , Ko Hyun S. , Liu David S. , Simpson Kaylene J. , Haupt Ygal , Lipton Lara , Haupt Sue , Phillips Wayne A. , Clemons Nicholas J.
Published: April 2023

Figure S2 shows APR-246 and PX-12 activity correlate in CTRPv2 and their impact on mutant-p53 thermostability.
Figure S1 from SLC7A11 Is a Superior Determinant of APR-246 (Eprenetapopt) Response than TP53 Mutation Status
Authors: Fujihara Kenji M. , Corrales Benitez Mariana , Cabalag Carlos S. , Zhang Bonnie Z. , Ko Hyun S. , Liu David S. , Simpson Kaylene J. , Haupt Ygal , Lipton Lara , Haupt Sue , Phillips Wayne A. , Clemons Nicholas J.
Published: April 2023

Figure S1 shows TP53 mutation alone is not predictive of cancer cell response to PRIMA-1.
Supplementary Figure S4 from Synthetic Lethality with Trifluridine/Tipiracil and Checkpoint Kinase 1 Inhibitor for Esophageal Squamous Cell Carcinoma
Authors: Ohashi Shinya , Kikuchi Osamu , Nakai Yukie , Ida Tomomi , Saito Tomoki , Kondo Yuki , Yamamoto Yoshihiro , Mitani Yosuke , Nguyen Vu Trang H. , Fukuyama Keita , Tsukihara Hiroshi , Suzuki Norihiko , Muto Manabu
Published: April 2023

DNA damage in TP53 wild-type cancer cells treated with FTD and CHK1 inhibitor.
Supplemental Table 4 from Role of Dimerized C16orf74 in Aggressive Pancreatic Cancer: A Novel Therapeutic Target
Authors: Kushibiki Toshihiro , Nakamura Toru , Tsuda Masumi , Tsuchikawa Takahiro , Hontani Koji , Inoko Kazuho , Takahashi Mizuna , Asano Toshimichi , Okamura Keisuke , Murakami Soichi , Kurashima Yo , Ebihara Yuma , Noji Takehiro , Nakanishi Yoshitsugu , Tanaka Kimitaka , Maishi Nako , Sasaki Katsunori , Park Woong-Ryeon , Shichinohe Toshiaki , Hida Kyoko , Tanaka Shinya , Hirano Satoshi
Published: April 2023

The antibodies and dilutions for Immunohistochemical staining
Supplementary Table 2 from Nonclinical Development of Next-generation Site-specific HER2-targeting Antibody–drug Conjugate (ARX788) for Breast Cancer Treatment
Authors: Nagaraja Shastri Prathap , Zhu Jingjing , Skidmore Lillian , Liang Xuejun , Ji Yanping , Gu Yi , Tian Feng , Yao Sulan , Xia Gang
Published: April 2023

Supplementary Table 2 describes Cynomolgus monkey tissue cross-reactivity study
Supplementary Table 1 from Nonclinical Development of Next-generation Site-specific HER2-targeting Antibody–drug Conjugate (ARX788) for Breast Cancer Treatment
Authors: Nagaraja Shastri Prathap , Zhu Jingjing , Skidmore Lillian , Liang Xuejun , Ji Yanping , Gu Yi , Tian Feng , Yao Sulan , Xia Gang
Published: April 2023

Supplementary Table 1 describes detection of pAF-AS269 metabolites after 120-minute incubation in cynomolgus or human hepatocytes
Supplementary Table S1 from Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR
Authors: Mao Shenlan , Chaerkady Raghothama , Yu Wen , D’Angelo Gina , Garcia Andrew , Chen Hong , Barrett Allison M. , Phipps Sandrina , Fleming Ryan , Hess Sonja , Koopmann Jens-Oliver , Dimasi Nazzareno , Wilson Susan , Pugh Kathryn , Cook Kimberly , Masterson Luke A. , Gao Changshou , Wu Herren , Herbst Ronald , Howard Philip W. , Tice David A. , Cobbold Mark , Harper Jay
Published: April 2023

Differentially expressed proteins identified in the 361-PBDr cell line
Supplementary Methods M2 from Nonclinical Development of Next-generation Site-specific HER2-targeting Antibody–drug Conjugate (ARX788) for Breast Cancer Treatment
Authors: Nagaraja Shastri Prathap , Zhu Jingjing , Skidmore Lillian , Liang Xuejun , Ji Yanping , Gu Yi , Tian Feng , Yao Sulan , Xia Gang
Published: April 2023

Supplementary Methods Section 2 describes tissue cross-reactivity study
Figure S5 from Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR
Authors: Mao Shenlan , Chaerkady Raghothama , Yu Wen , D’Angelo Gina , Garcia Andrew , Chen Hong , Barrett Allison M. , Phipps Sandrina , Fleming Ryan , Hess Sonja , Koopmann Jens-Oliver , Dimasi Nazzareno , Wilson Susan , Pugh Kathryn , Cook Kimberly , Masterson Luke A. , Gao Changshou , Wu Herren , Herbst Ronald , Howard Philip W. , Tice David A. , Cobbold Mark , Harper Jay
Published: April 2023

DNA damage checkpoint activation mediated by SLFN11 and ATR pathways in response to SG3199.
Figure S4 from Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR
Authors: Mao Shenlan , Chaerkady Raghothama , Yu Wen , D’Angelo Gina , Garcia Andrew , Chen Hong , Barrett Allison M. , Phipps Sandrina , Fleming Ryan , Hess Sonja , Koopmann Jens-Oliver , Dimasi Nazzareno , Wilson Susan , Pugh Kathryn , Cook Kimberly , Masterson Luke A. , Gao Changshou , Wu Herren , Herbst Ronald , Howard Philip W. , Tice David A. , Cobbold Mark , Harper Jay
Published: April 2023

Knockdown of 5T4 expression do not confer SG3199 resistance to parental MDA-MB-361 cells.
Supplementary Figure S3 from Nonclinical Development of Next-generation Site-specific HER2-targeting Antibody–drug Conjugate (ARX788) for Breast Cancer Treatment
Authors: Nagaraja Shastri Prathap , Zhu Jingjing , Skidmore Lillian , Liang Xuejun , Ji Yanping , Gu Yi , Tian Feng , Yao Sulan , Xia Gang
Published: April 2023

Supplementary Figure S3 illustrates body weights for male and female monkeys after repeat dose administration of ARX788. ARX788 was administered by intravenous infusion to cynomolgus monkeys at 3.3 mg/kg/dose (n=6 females and 6 males), 10 mg/kg/dose (n=6 females and 6 males), or 15 mg/kg/dose (n=7 females and 7 males) once every 3 weeks, for 4 total doses. The control group (n=6 females and 6 males) was administered placebo once every 3 weeks, for 4 total doses. Animals treated with 15 mg/kg/dose ARX788 did not receive the third and fourth doses due to unexpected mortality and toxicity observed after the second dose. Body weights for male (A) and female (B) monkeys were monitored once weekly for the duration of the study.
Figure S3 from Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR
Authors: Mao Shenlan , Chaerkady Raghothama , Yu Wen , D’Angelo Gina , Garcia Andrew , Chen Hong , Barrett Allison M. , Phipps Sandrina , Fleming Ryan , Hess Sonja , Koopmann Jens-Oliver , Dimasi Nazzareno , Wilson Susan , Pugh Kathryn , Cook Kimberly , Masterson Luke A. , Gao Changshou , Wu Herren , Herbst Ronald , Howard Philip W. , Tice David A. , Cobbold Mark , Harper Jay
Published: April 2023

The 361-ADCr, a MEDI0641 resistant line, has downregulated target 5T4
Supplementary Figure S2 from Nonclinical Development of Next-generation Site-specific HER2-targeting Antibody–drug Conjugate (ARX788) for Breast Cancer Treatment
Authors: Nagaraja Shastri Prathap , Zhu Jingjing , Skidmore Lillian , Liang Xuejun , Ji Yanping , Gu Yi , Tian Feng , Yao Sulan , Xia Gang
Published: April 2023

Supplementary Figure S2 illustrates biodistribution of 125I-anti-HER2 mAb in tumor-bearing mice. Tumor-bearing mice (n=6/group, 4 groups) were dosed intravenously with 125I-anti-HER2 mAb. At 2, 24, 72, or 168 hours post-dose, one group of treated mice were euthanized following blood and urine sample collection. Anti-HER2 mAb concentrations in tumor tissue remained relatively stable at approximately 10 µg Eq/mL from 2 hours through 72 hours post-dose, indicating HER2-targeted distribution into the tumor environment. In other tissues, anti-HER2 mAb peaked 2 hours post-dose followed by a gradual decrease in concentrations through 168 hours. The tissue biodistribution of 125I-ARX788 in tumor-bearing mice was similar to the biodistribution of 125I-anti-HER2 mAb .
Figure S2 from Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR
Authors: Mao Shenlan , Chaerkady Raghothama , Yu Wen , D’Angelo Gina , Garcia Andrew , Chen Hong , Barrett Allison M. , Phipps Sandrina , Fleming Ryan , Hess Sonja , Koopmann Jens-Oliver , Dimasi Nazzareno , Wilson Susan , Pugh Kathryn , Cook Kimberly , Masterson Luke A. , Gao Changshou , Wu Herren , Herbst Ronald , Howard Philip W. , Tice David A. , Cobbold Mark , Harper Jay
Published: April 2023

The addition of the ATR inhibitor, AZD6738, did not show synergistic cytotoxicity with SG3199 or ADCs in parental MDA-MB-361 cells
Supplementary Materials and Methods, Supplementary Figure S1, Supplementary Figure S2, Supplementary Figure S3, Supplementary Figure S4, Supplementary Figure S5 from Inhibition of Importin β1 Augments the Anticancer Effect of Agonistic Anti-Death Receptor 5 Antibody in TRAIL-resistant Tumor Cells
Authors: Kojima Yuko , Nishina Takashi , Nakano Hiroyasu , Okumura Ko , Takeda Kazuyoshi
Published: April 2023

Immunohistochemistry and image analysis, Apoptosis induction in shRNA-transduced importin β1 knockdown HeLa cells with administration of agonistic anti-hDR5 mAb (CS-1008) in vivo, Antitumor effect of importin β1 knockdown via atelocollagen delivery of shRNA in combination with CS-1008 on HeLa and HepG2 xenograft models, Effect of importazole on apoptosis induction by rTRAIL in HeLa and HepG2 cells in vitro, Body weights of the mice during the treatment importazole and/or CS-1008 in the experiments presented in Fig. 6, Importin β1 expression in the xenograft tumor tissues dissected from the mice treated with hIgG and doxycycline in the experiments presented in Fig. 3A and B.
Figure S5 from CRISPR Screening Identifies WEE1 as a Combination Target for Standard Chemotherapy in Malignant Pleural Mesothelioma
Authors: Xu Duo , Liang Shun-Qing , Yang Haitang , Bruggmann Rémy , Berezowska Sabina , Yang Zhang , Marti Thomas Michael , Hall Sean Ralph Robert , Gao Yanyun , Kocher Gregor J. , Schmid Ralph A. , Peng Ren-Wang
Published: April 2023

Supplementary Figure S5. Characterization of MPM cells that acquired resistance to chemotherapy.
Supplementary Data from Restoration of T-cell Effector Function, Depletion of Tregs, and Direct Killing of Tumor Cells: The Multiple Mechanisms of Action of a-TIGIT Antagonist Antibodies
Authors: Preillon Julie , Cuende Julia , Rabolli Virginie , Garnero Lucile , Mercier Marjorie , Wald Noémie , Pappalardo Angela , Denies Sofie , Jamart Diane , Michaux Anne-Catherine , Pirson Romain , Pitard Vincent , Bagot Martine , Prasad Shruthi , Houthuys Erica , Brouwer Margreet , Marillier Reece , Lambolez Florence , Marchante Joäo R. , Nyawouame Florence , Carter Mathew J. , Baron-Bodo Véronique , Marie-Cardine Anne , Cragg Mark , Déchanet-Merville Julie , Driessens Gregory , Hoofd Catherine
Published: April 2023

Supplementary material (Text)
Supp Figures from Restoration of T-cell Effector Function, Depletion of Tregs, and Direct Killing of Tumor Cells: The Multiple Mechanisms of Action of a-TIGIT Antagonist Antibodies
Authors: Preillon Julie , Cuende Julia , Rabolli Virginie , Garnero Lucile , Mercier Marjorie , Wald Noémie , Pappalardo Angela , Denies Sofie , Jamart Diane , Michaux Anne-Catherine , Pirson Romain , Pitard Vincent , Bagot Martine , Prasad Shruthi , Houthuys Erica , Brouwer Margreet , Marillier Reece , Lambolez Florence , Marchante Joäo R. , Nyawouame Florence , Carter Mathew J. , Baron-Bodo Véronique , Marie-Cardine Anne , Cragg Mark , Déchanet-Merville Julie , Driessens Gregory , Hoofd Catherine
Published: April 2023

Supplemental figures
Figure S2 from CRISPR Screening Identifies WEE1 as a Combination Target for Standard Chemotherapy in Malignant Pleural Mesothelioma
Authors: Xu Duo , Liang Shun-Qing , Yang Haitang , Bruggmann Rémy , Berezowska Sabina , Yang Zhang , Marti Thomas Michael , Hall Sean Ralph Robert , Gao Yanyun , Kocher Gregor J. , Schmid Ralph A. , Peng Ren-Wang
Published: April 2023

Supplementary Figure S2. Prognostic significance of G2-M related genes in MPM
Supplementary Data from HLA Polymorphisms Are Associated with Treatment-Free Remission Following Discontinuation of Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia
Authors: Ureshino Hiroshi , Shindo Takero , Tanaka Hidenori , Saji Hiroh , Kimura Shinya
Published: April 2023

Supplementary Data from HLA Polymorphisms Are Associated with Treatment-Free Remission Following Discontinuation of Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia
Figure S1 from CRISPR Screening Identifies WEE1 as a Combination Target for Standard Chemotherapy in Malignant Pleural Mesothelioma
Authors: Xu Duo , Liang Shun-Qing , Yang Haitang , Bruggmann Rémy , Berezowska Sabina , Yang Zhang , Marti Thomas Michael , Hall Sean Ralph Robert , Gao Yanyun , Kocher Gregor J. , Schmid Ralph A. , Peng Ren-Wang
Published: April 2023

Supplementary Figure S1. Genes regulating the G2-M cell cycle transition are deregulated in MPM.
Supplementary Materials and Methods from Blockade of Cell Volume Regulatory Protein NKCC1 Increases TMZ-Induced Glioma Apoptosis and Reduces Astrogliosis
Authors: Luo Lanxin , Guan Xiudong , Begum Gulnaz , Ding Dawei , Gayden Jenesis , Hasan Md Nabiul , Fiesler Victoria M. , Dodelson Jacob , Kohanbash Gary , Hu Baoli , Amankulor Nduka M. , Jia Wang , Castro Maria G. , Sun Baoshan , Sun Dandan
Published: April 2023

Supplementary Materials and Methods
Figure S3 from Blockade of Cell Volume Regulatory Protein NKCC1 Increases TMZ-Induced Glioma Apoptosis and Reduces Astrogliosis
Authors: Luo Lanxin , Guan Xiudong , Begum Gulnaz , Ding Dawei , Gayden Jenesis , Hasan Md Nabiul , Fiesler Victoria M. , Dodelson Jacob , Kohanbash Gary , Hu Baoli , Amankulor Nduka M. , Jia Wang , Castro Maria G. , Sun Baoshan , Sun Dandan
Published: April 2023

Fig. S3. Combining TMZ therapy with pharmacological inhibition of NKCC1 enhances apoptosis and reduces SB28-GFP glioma growth.
Supplementary Data from Rigosertib Induces Mitotic Arrest and Apoptosis in RAS-Mutated Rhabdomyosarcoma and Neuroblastoma
Authors: Kowalczyk Joshua T. , Wan Xiaolin , Hernandez Edjay R. , Luo Ruibai , Lyons Gaelyn C. , Wilson Kelli M. , Gallardo Devorah C. , Isanogle Kristine A. , Robinson Christina M. , Mendoza Arnulfo , Heske Christine M. , Chen Jinqui-Qiu , Luo Xiaoling , Kelly Alexander E. , Difilippantinio Simone , Robey Robert W. , Thomas Craig J. , Sackett Dan L. , Morrison Deborah K. , Randazzo Paul A. , Jenkins Lisa M. Miller , Yohe Marielle E.
Published: April 2023

Supplemental tables 1-3, supplemental figure legends, supplemental figures 1-4
Up-regulated Hypermethylated genes from Decitabine Response in Breast Cancer Requires Efficient Drug Processing and Is Not Limited by Multidrug Resistance
Authors: Dahn Margaret L. , Cruickshank Brianne M. , Jackson Ainsleigh J. , Dean Cheryl , Holloway Ryan W. , Hall Steven R. , Coyle Krysta M. , Maillet Hillary , Waisman David M. , Goralski Kerry B. , Giacomantonio Carman A. , Weaver Ian C.G. , Marcato Paola
Published: April 2023

Genes up-regulated by decitabine treatment in MDA-MB-468, MDA-MB-231, or SUM159 with hypermethylated promoters (TSS200)
Supplementary Figure S2 from Statins Reduce Intratumor Cholesterol Affecting Adrenocortical Cancer Growth
Authors: Trotta Francesca , Avena Paola , Chimento Adele , Rago Vittoria , De Luca Arianna , Sculco Sara , Nocito Marta C. , Malivindi Rocco , Fallo Francesco , Pezzani Raffaele , Pilon Catia , Lasorsa Francesco M. , Barile Simona N. , Palmieri Luigi , Lerario Antonio M. , Pezzi Vincenzo , Casaburi Ivan , Sirianni Rosa
Published: April 2023

Supplementary Fig. S2 shows Immunohistochemical staining of H295R xenograft samples.
Supplementary Data from AZD4625 is a Potent and Selective Inhibitor of KRASG12C
Authors: Chakraborty Atanu , Hanson Lyndsey , Robinson David , Lewis Hilary , Bickerton Sue , Davies Michael , Polanski Radoslaw , Whiteley Rebecca , Koers Alex , Atkinson James , Baker Tamara , del Barco Barrantes Ivan , Ciotta Giovanni , Kettle Jason G. , Magiera Lukasz , Martins Carla P. , Peter Alison , Wigmore Eleanor , Underwood Zoe , Cosulich Sabina , Niedbala Michael , Ross Sarah
Published: April 2023

Supplementary Data from AZD4625 is a Potent and Selective Inhibitor of KRASG12C
Supplementary Materials from Nifuroxazide Activates the Parthanatos to Overcome TMPRSS2:ERG Fusion-Positive Prostate Cancer
Authors: Li Chengxun , Zhang Jiale , Wu Qiming , Kumar Anuj , Pan Guihong , Kelvin David J.
Published: April 2023

Supplementary materials and methods, Supplementary Tables and Supplementary Figures 1S-10S
Supplementary Data 1 from Nifuroxazide Activates the Parthanatos to Overcome TMPRSS2:ERG Fusion-Positive Prostate Cancer
Authors: Li Chengxun , Zhang Jiale , Wu Qiming , Kumar Anuj , Pan Guihong , Kelvin David J.
Published: April 2023

Analysis of differentially expressed genes between untreated and NFZ-treated VCaP cells.
Supplementary figures S1-S10 from Near-Infrared Photoimmunotherapy Targeting Podoplanin-Expressing Cancer Cells and Cancer-Associated Fibroblasts
Authors: Kato Takuya , Furusawa Aki , Okada Ryuhei , Inagaki Fuyuki , Wakiyama Hiroaki , Furumoto Hideyuki , Fukushima Hiroshi , Okuyama Shuhei , Choyke Peter L. , Kobayashi Hisataka
Published: April 2023

Supplementary Fig. S1. Efficacy of PDPN-targeted NIR-PIT for BALB/c 3T3 cells in vitro.
Supplementary Fig. S2. Internalization of PDPN-IR700 in MOC1 and BALB/c 3T3 cells.
Supplementary Fig. S3. Distribution of PDPN-expressing cells in MOC2 tumors.
Supplementary Fig. S4. PDPN expression on hematopoietic cells.
Supplementary Fig. S5. In vivo 700 nm fluorescence imaging after the injection of PDPN-IR700.
Supplementary Fig. S6. Lymphogram after PDPN-targeted NIR-PIT.
Supplementary Fig. S7. The evaluation of lymphatic and blood vessels after PDPN-targeted NIR-PIT in a MOC1 tumor model by multiplex IHC.
Supplementary Fig. S8. Efficacy of in vitro PDPN-targeted NIR-PIT against MC38-luc tumors which has no PDPN expression.
Supplementary Fig. S9. The difference of MOC2 and MC38-luc tumors in multiplex IHC.
Supplementary Fig. S10. The distribution of DIG-labeled anti-PDPN (PDPN-DIG) in MOC1 tumors.
Supplementary Figure S5 from Ubiquitinated PCNA Drives USP1 Synthetic Lethality in Cancer
Authors: Simoneau Antoine , Engel Justin L. , Bandi Madhavi , Lazarides Katherine , Liu Shangtao , Meier Samuel R. , Choi Ashley H. , Zhang Hongxiang , Shen Binzhang , Martires Lauren , Gotur Deepali , Pham Truc V. , Li Fang , Gu Lina , Gong Shanzhong , Zhang Minjie , Wilker Erik , Pan Xuewen , Whittington Douglas A. , Throner Scott , Maxwell John P. , Chen Yingnan , Yu Yi , Huang Alan , Andersen Jannik N. , Feng Tianshu
Published: April 2023

CRISPR-UMI analysis of screens performed in NCI-H1693 cells - related to Figure 5
Supplementary Figure S4 from Ubiquitinated PCNA Drives USP1 Synthetic Lethality in Cancer
Authors: Simoneau Antoine , Engel Justin L. , Bandi Madhavi , Lazarides Katherine , Liu Shangtao , Meier Samuel R. , Choi Ashley H. , Zhang Hongxiang , Shen Binzhang , Martires Lauren , Gotur Deepali , Pham Truc V. , Li Fang , Gu Lina , Gong Shanzhong , Zhang Minjie , Wilker Erik , Pan Xuewen , Whittington Douglas A. , Throner Scott , Maxwell John P. , Chen Yingnan , Yu Yi , Huang Alan , Andersen Jannik N. , Feng Tianshu
Published: April 2023

USP1 and PARP inhibition are synergistic in a BRCA1/2-dependent manner - related to Figure 4
Supplementary Table from External Validation of Association of Baseline Circulating Tumor Cell Counts with Survival Outcomes in Men with Metastatic Castration-Sensitive Prostate Cancer
Authors: Swami Umang , Sayegh Nicolas , Jo Yeonjung , Haaland Benjamin , McFarland Taylor Ryan , Nussenzveig Roberto H. , Goel Divyam , Sirohi Deepika , Hahn Andrew W. , Maughan Benjamin L. , Goldkorn Amir , Agarwal Neeraj
Published: April 2023

Supplementary Table from External Validation of Association of Baseline Circulating Tumor Cell Counts with Survival Outcomes in Men with Metastatic Castration-Sensitive Prostate Cancer
Supplementary Table S3 from Emerging Developments in ETS-Positive Prostate Cancer Therapy
Authors: Bowling Gartrell C. , Rands Mitchell G. , Dobi Albert , Eldhose Binil
Published: April 2023

Supplementary Table S3
Fig S4 from A Bispecific METxMET Antibody–Drug Conjugate with Cleavable Linker Is Processed in Recycling and Late Endosomes
Authors: Perez Bay Andres E. , Faulkner Devon , DaSilva John O. , Young Tara M. , Yang Katie , Giurleo Jason T. , Ma Dangshe , Delfino Frank J. , Olson William C. , Thurston Gavin , Daly Christopher , Andreev Julian
Published: April 2023

Cathepsins
Figure S4 from Inhibition of LILRB2 by a Novel Blocking Antibody Designed to Reprogram Immunosuppressive Macrophages to Drive T-Cell Activation in Tumors
Authors: Umiker Ben , Hashambhoy-Ramsay Yasmin , Smith Jeff , Rahman Tanzila , Mueller Amy , Davidson Rachel , Meyer Christina , Patankar Gayatri , Alam Mohammad Murshid , Jaffe Sarah , Krukenberg Kristin , Goodman Allison , Spaulding Vikki , Priess Michelle , Dhaneshwar Abha , Wong Masie , Diiorio Alexa , O'Malley Kristin , McGrath Lara , Willer Margaret , Pepper Lauren , Gostissa Monica , Kis-Toth Katalin , Wiederschain Dmitri , Cohen Heather , Shaffer Donald R.
Published: April 2023

Example gating strategy in vitro differentiated M-CSF macrophages
Figure S3 from Inhibition of LILRB2 by a Novel Blocking Antibody Designed to Reprogram Immunosuppressive Macrophages to Drive T-Cell Activation in Tumors
Authors: Umiker Ben , Hashambhoy-Ramsay Yasmin , Smith Jeff , Rahman Tanzila , Mueller Amy , Davidson Rachel , Meyer Christina , Patankar Gayatri , Alam Mohammad Murshid , Jaffe Sarah , Krukenberg Kristin , Goodman Allison , Spaulding Vikki , Priess Michelle , Dhaneshwar Abha , Wong Masie , Diiorio Alexa , O'Malley Kristin , McGrath Lara , Willer Margaret , Pepper Lauren , Gostissa Monica , Kis-Toth Katalin , Wiederschain Dmitri , Cohen Heather , Shaffer Donald R.
Published: April 2023

Example gating strategy for blood monocytes
Data from Inhibition of LILRB2 by a Novel Blocking Antibody Designed to Reprogram Immunosuppressive Macrophages to Drive T-Cell Activation in Tumors
Authors: Umiker Ben , Hashambhoy-Ramsay Yasmin , Smith Jeff , Rahman Tanzila , Mueller Amy , Davidson Rachel , Meyer Christina , Patankar Gayatri , Alam Mohammad Murshid , Jaffe Sarah , Krukenberg Kristin , Goodman Allison , Spaulding Vikki , Priess Michelle , Dhaneshwar Abha , Wong Masie , Diiorio Alexa , O'Malley Kristin , McGrath Lara , Willer Margaret , Pepper Lauren , Gostissa Monica , Kis-Toth Katalin , Wiederschain Dmitri , Cohen Heather , Shaffer Donald R.
Published: April 2023

Abstract
Tumor-associated macrophages (TAM) play an important role in maintaining the immunosuppressive state of the tumor microenvironment (TME). High levels of CD163+ TAMs specifically are associated with poor prognosis in many solid tumor types. Targeting TAMs may represent a key approach in development of the next generation of cancer immune therapeutics. Members of the leukocyte immunoglobulin-like receptor B (LILRB) family, including LILRB2 (ILT4), are known to transmit inhibitory signals in macrophages and other myeloid cells. Leveraging bulk and single cell RNA-sequencing datasets, as well as extensive immunophenotyping of human tumors, we found that LILRB2 is highly expressed on CD163+ CD11b+ cells in the TME and that LILRB2 expression correlates with CD163 expression across many tumor types. To target LILRB2, we have developed JTX-8064, a highly potent and selective antagonistic mAb. JTX-8064 blocks LILRB2 binding to its cognate ligands, including classical and nonclassical MHC molecules. In vitro, JTX-8064 drives the polarization of human macrophages and dendritic cells toward an immunostimulatory phenotype. As a result, human macrophages treated with a LILRB2 blocker are reprogrammed to increase the activation of autologous T cells in co-culture systems. Furthermore, JTX-8064 significantly potentiates the activity of anti-PD-1 in allogeneic mixed lymphocyte reaction. In a human tumor explant culture, pharmacodynamic activity of JTX-8064 was observed in monotherapy and in combination with anti-PD-1. Collectively, our work provides strong translational and preclinical rationale to target LILRB2 in cancer.
Data from The Secretome Engages STAT3 to Favor a Cytokine-rich Microenvironment in Mediating Acquired Resistance to FGFR Inhibitors
Authors: Wang Xinyi , Ai Jing , Liu Hongyan , Peng Xia , Chen Hui , Chen Yi , Su Yi , Shen Aijun , Huang Xun , Ding Jian , Geng Meiyu
Published: April 2023

Abstract
Acquired resistance severely hinders the application of small-molecule inhibitors. Our understanding of acquired resistance related to FGFRs is limited. Here, to explore the underlying mechanism of acquired resistance in FGFR-aberrant cancer cells, we generated cells resistant to multiple FGFR inhibitors (FGFRi) and investigated the potential mechanisms underlying acquired resistance. We discovered that reprogramming of the secretome is closely associated with acquired resistance to FGFRi. The secretome drives acquired resistance by activating the transcription factor STAT3 via its cognate receptors. Moreover, macrophages and fibroblasts could interact with cancer cells to enhance acquired resistance by promoting exaggerated and dynamic cytokine secretion, as well as STAT3 activation. We also found that Hsp90 and HDAC inhibitors could substantially and simultaneously suppress the proliferation of resistant cells, the secretion of multiple cytokines, and the activation of STAT3. Our study offers translational insights concerning the poor efficacy observed in patients with macrophage- and fibroblast-rich lung cancers and breast tumors after treatment with FGFRi in clinical trials.
Data from ATR Inhibition Is a Promising Radiosensitizing Strategy for Triple-Negative Breast Cancer
Authors: Tu Xinyi , Kahila Mohamed M. , Zhou Qin , Yu Jia , Kalari Krishna R. , Wang Liewei , Harmsen William S. , Yuan Jian , Boughey Judy C. , Goetz Matthew P. , Sarkaria Jann N. , Lou Zhenkun , Mutter Robert W.
Published: April 2023

Abstract
Triple-negative breast cancer (TNBC) is characterized by elevated locoregional recurrence risk despite aggressive local therapies. New tumor-specific radiosensitizers are needed. We hypothesized that the ATR inhibitor, VX-970 (now known as M6620), would preferentially radiosensitize TNBC. Noncancerous breast epithelial and TNBC cell lines were investigated in clonogenic survival, cell cycle, and DNA damage signaling and repair assays. In addition, patient-derived xenograft (PDX) models generated prospectively as part of a neoadjuvant chemotherapy study from either baseline tumor biopsies or surgical specimens with chemoresistant residual disease were assessed for sensitivity to fractionated radiotherapy, VX-970, or the combination. To explore potential response biomarkers, exome sequencing was assessed for germline and/or somatic alterations in homologous recombination (HR) genes and other alterations associated with ATR inhibitor sensitivity. VX-970 preferentially inhibited ATR-Chk1-CDC25a signaling, abrogated the radiotherapy-induced G2–M checkpoint, delayed resolution of DNA double-strand breaks, and reduced colony formation after radiotherapy in TNBC cells relative to normal-like breast epithelial cells. In vivo, VX-970 did not exhibit significant single-agent activity at the dose administered even in the context of genomic alterations predictive of ATR inhibitor responsiveness, but significantly sensitized TNBC PDXs to radiotherapy. Exome sequencing and functional testing demonstrated that combination therapy was effective in both HR-proficient and -deficient models. PDXs established from patients with chemoresistant TNBC were also highly radiosensitized. In conclusion, VX-970 is a tumor-specific radiosensitizer for TNBC. Patients with residual TNBC after neoadjuvant chemotherapy, a subset at particularly high risk of relapse, may be ideally suited for this treatment intensification strategy. Mol Cancer Ther; 17(11); 2462–72. ©2018 AACR.