bluuebunny/crossref_metadata_2025_split huggingface dataset:
Azoheteroarene and Diazocine Molecular Photoswitches: Self‐Assembly, Responsive Materials and Photopharmacology
Authors: Mukherjee Anurag , Seyfried Maximilian D. , Ravoo Bart Jan 
Published: May 2023

AbstractAromatic units tethered with an azo (−N=N−) functionality comprise a unique class of compounds, known as molecular photoswitches, exhibiting a reversible transformation between their E‐ and Z‐isomers in response to photo‐irradiation. Photoswitches have been explored extensively in the recent past to prepare dynamic self‐assembled materials, optoelectronic devices, responsive biomaterials, and more. Most of such materials involve azobenzenes as the molecular photoswitch and to date, SciFinder lists more than 7000 articles and 1000 patents. Subsequently, a great deal of effort has been invested to improve the photo‐isomerization efficiency and related mesoscopic properties of azobenzenes. Recently, azoheteroarenes and cyclic azobenzenes, such as arylazopyrazoles, arylazoisoxazoles, arylazopyridines, and diazocines, have emerged as second generation molecular photoswitches beyond conventional azobenzenes. These photoswitches offer distinct photoswitching behavior and responsive properties which make them highly promising candidates for multifaceted applications ranging from photoresponsive materials to photopharmacophores. In this minireview, we introduce the structural refinement and photoresponsive properties of azoheteroarenes and diazocines and summarize the state‐of‐the‐art on utilizing these photoswitches as responsive building blocks in supramolecular assembly, material science and photopharmacology, highlighting their versatile photochemical behavior, enhanced functionality, and latest applications.
First report on the utility of pupal case for early determination of CRISPR/Cas9 ribonucleoprotein mediated genomic edits in the oriental fruit fly, Bactrocera dorsalis (Hendel) (Tephritidae: Diptera)
Authors: Ashok Karuppannasamy , Bhargava Chikmagalur Nagaraja , Asokan Ramasamy , Pradeep Chalapathi , Kennedy John Samuel , Rai Anil , Manamohan Maligeppagol 
Published: May 2023

AbstractThe Oriental fruit fly, Bactrocera dorsalis (Hendel), is a highly invasive pest of quarantine importance affecting the global fruit trade. In managing B. dorsalis, methods like cultural, biological, chemical, sterile insect technique (SIT), and semiochemical‐mediated attract‐and‐kill are in use with varying success. The SIT approach is the method of choice for a chemical‐free, long‐term suppression of B. dorsalis, followed in many countries across the globe. The nonspecific mutations caused by irradiation affect the overall fitness of flies, thus requiring a more precise method for a heritable, fitness‐not‐compromising approach. In this regard, CRISPR/Cas9‐mediated genome editing enables the creation of mutations at the precise genomic location/s through RNA‐guided dsDNA cleavage. Of late, DNA‐free editing employing ribonucleoprotein complex (RNP) is preferred to validate the target genes at G0 stage embryos in insects. It requires characterizing genomic edits from adults after completing their life cycle, which may entail a few days to months, depending on longevity. Additionally, edit characterization is required from each individual, as edits are unique. Therefore, all RNP‐microinjected individuals must be maintained until the end of their life cycle, irrespective of editing. To overcome this impediment, we predetermine the genomic edits from the shed tissues, such as pupal cases, to maintain only edited individuals. In this study, we have shown the utility of pupal cases from five males and females of B. dorsalis to predetermine the genomic edits, which corroborated the edits from the respective adults.
Current progress in the targeted therapy of breast cancer: Structure–activity correlation and docking studies (2015–2021)
Authors: Pandey Shivanshu , Mondal Sitanshu , Kajal Kumari , Kurmi Balak Das , Verma Sant Kumar , Patel Preeti 
Published: May 2023

AbstractDespite cancer research and therapy, breast cancer remains a complicated health crisis in women and represents a top biomedical research priority. Nowadays, breast cancer is an extremely heterogeneous disease and is known as the leading cause of death among women worldwide. The incidence and mortality rates of breast cancer have been increasing gradually for the past decades. Nowadays, common treatments for breast cancer are chemotherapy, endocrine therapy, immunotherapy, radiotherapy, and surgery. The most common targets in breast cancer treatment are human epidermal growth factor receptor 2 (HER2) and estrogen receptors. The literature suggests that several targets/pathways are also involved in the development of breast cancer, that is, poly(ADP‐ribose) polymerase (PARP), bromodomain‐containing protein 4 (BRD4), cyclin‐dependent kinase 4/6 (CDK4/6), epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR), polo‐like kinase 1 (PLK1), phosphoinositide 3‐kinases/protein kinase B/mammalian target of rapamycin (PI3K/AKT/mTOR), histone deacetylase (HDAC), nuclear factor kappa B (NF‐κB), PD‐L1, and aromatase inhibitors. Meanwhile, the study of breast cancer is a hot topic in the current scenario of basic/clinical research. This review article provides information on different targets associated with breast cancer and summarizes the progress of current research on synthesized inhibitors as anti‐breast cancer agents from 2015 to 2021. The review aims to provide structure–activity relationship and docking studies for designing novel compounds for breast cancer therapy.
Tunable Luminescence of Nonaromatic Borate Esters
Authors: Yang Tianjia , Hou Wubeiwen , Yuan Wang Zhang 
Published: May 2023

AbstractWhile the majority of nonconventional luminophores consist of electron‐rich heteroatoms, an emerging category with electron‐deficient atoms (e. g. boron) have gained much attention. In this work, we focused on one of the most common boron‐containing substances, namely bis(pinacolato)diboron (BE1) and its analogue bis(2,4‐dimethylpentane‐2,4‐glycolato)diboron (BE2), whose empty p‐orbitals of boron atoms and p‐orbitals with lone pairs of oxygens form π frameworks. Both compounds are nonemissive in dilute solutions but depict remarkable photoluminescence (PL) at aggregate states, featuring aggregation‐induced emission characteristics. Additionally, their PL can be easily tuned by various external factors, such as excitation wavelength, compression, and oxygen. These photophysical properties could well be explained by the clustering‐triggered emission (CTE) mechanism.
Coordination‐Induced Migration of Aryl Groups in the Reactions of a Dialkylsilanone with a Series of Triarylboranes
Authors: Ishida Shintaro , Sakamoto Kengo , Kobayashi Ryo , Iwamoto Takeaki 
Published: May 2023

AbstractAlthough carbonyl compounds are activated by the coordination of a Lewis acid to the carbonyl oxygen atom, a similar activation process of R2Si=O species remains unclear. We report herein the reactions of a silanone (1, Scheme 1) with a series of triarylboranes to afford the corresponding boroxysilanes. Experimental results and computational studies indicate that the electrophilicity of the unsaturated silicon atom is enhanced by the complexation of 1 with triarylboranes, and the subsequent aryl migration from the boron atom to the electrophilic silicon atom proceeds.
Blossoming of Polyenamine Catalysis in Asymmetric Synthesis: Scope and Future Applications
Authors: Borah Biplob , Sivaprakash Murugesan , Sharma Samrita , Prasad Madavi S. , Raju Chowhan L. 
Published: May 2023

AbstractAfter the emergence of organocatalysis, the field of asymmetric synthesis has reached an exceptional level in this century. Asymmetric aminocatalysis, among other organocatalytic strategies, proceeded through LUMO‐lowering iminium ion and HOMO‐raising enamine ion activation has appeared as a powerful synthetic approach for realizing potential chiral building blocks from unmodified carbonyl compounds. Consequently, the concept of HOMO‐raising activation strategy for a plethora of asymmetric transformations based on enamine, dienamine, and most recently trienamine, tetraenamine, and pentaenamine catalysis has been devised. In this mini‐review article, we disclosed the recent progress accomplished in asymmetric aminocatalysis through polyenamine activation strategies for the functionalization of carbonyl compounds, and we covered the reports from 2014 to till date.
Preoperative denosumab treatment in patients with giant cell bone tumors in limbs: A retrospective study using propensity score matching
Authors: Huang Yongfu , Xu Mingxian , Wang Bo , Zhao Zhiqiang , Lin Tiao , Huang Gang , Yin Junqiang , Xie Xianbiao , Shen Jingnan , Zou Changye 
Published: May 2023

AbstractBackground and ObjectivesDenosumab is recommended for advanced giant cell tumor of bone (GCTB) that is unresectable or resectable with unacceptable morbidity. But the effect of preoperative denosumab treatment on the local control GCTB remains controversial.MethodsWe conducted a study of 49 patients with GCTB in the limbs treated with denosumab before surgery and 125 patients without in our hospital from 2010 to 2017. Propensity‐score matching (PSM) at a 1:1 ratio between the denosumab and control groups was performed to minimize possible selection bias, and compared the recurrence rate, limb function, and surgical degradation between the two groups.ResultsThe 3‐year recurrence rates in the denosumab group and the control group were 20.4% and 22.9% after PSM, respectively (p = 0.702). In the denosumab group, 75.5% (n = 37/49) of patients experienced surgical downgrading. Limb joint preservation rates were 92.1% (35) for 38 patients treated with denosumab and 60.2% (71) for 118 control subjects. (p ≺ 0.001). Postoperative MSTS were higher in patients in the denosumab group than in the control group (24.1 vs. 22.6, p = 0.034).ConclusionsPreoperative denosumab treatment did not result in an increased risk of local recurrence of GCTB. Patients with advanced GCTB may benefit from preoperative denosumab treatment for surgical downgrading and the preservation of the joint.
TRIM55 inhibits colorectal cancer development via enhancing protein degradation of c‐Myc
Authors: Lin Min , Fang Zejun , Lin Xuedan , Zhou Weihua , Wang Yizhang , Han Shanshan , Ye Ming , Zhu Fengjiao 
Published: May 2023

AbstractBackgroundColorectal cancer (CRC) is one of the most common and lethal malignancies which including colon and rectum cancer. Tripartite motif containing 55 (TRIM55) is an E3 ubiquitin ligase belonging to the TRIM family. Although the aberrant TRIM55 expression has been implicated in several tumors, its functional role, and molecular mechanisms in CRC remain unknown.MethodsImmunohistochemical studies, qRT‐PCR, and Western blot were performed to analyze the expression of TRIM55 in CRC patients and cell lines. TRIM55 expression and its relevance to clinical traits and prognosis were further explored in the TCGA database, and in our 87 clinical samples. Subsequently, we performed a series of functional assays to explore the effect of TRIM55 on CRC progression. Finally, the molecular mechanism of TRIM55 was investigated by immunoprecipitation and ubiquitination analyses.ResultsHere, we demonstrated that TRIM55 was markedly downregulated in CRC cell lines and tumors from CRC patients. Moreover, overexpression of TRIM55 could suppress CRC cell growth in vitro and inhibit CRC xenograft tumor development in vivo. Additionally, TRIM55 overexpression dampened CRC cell migration and invasion. Further bioinformatics analysis indicated that TRIM55 suppressed cyclin D1 and c‐Myc expression. Mechanistically, co‐immunoprecipitation assay revealed that TRIM55 directly interacted with c‐Myc and down‐regulated its protein expression level via protein ubiquitination. Intriguingly, c‐Myc overexpression partially antagonized the function of TRIM55 overexpression.ConclusionsTaken together, our findings suggest that TRIM55 inhibits CRC tumor development via, at least in part, enhancing protein degradation of c‐Myc. Targeting TRIM55 could provide a new therapeutic approach for CRC patients.
Reasons for truly negative cytology reports preceding the diagnoses of invasive cervical cancer—Results of a false‐negative cytology audit in Polish Cervical Cancer Screening Programme
Authors: Macios Anna , Komerska Katarzyna , Nowakowski Andrzej 
Published: May 2023

AbstractBackgroundFalse‐negative (FN) results in cervical cancer (CC) screening pose significant risk for participants and should be audited. The aim of the study was to analyse the results of audit of FN slides collected in 2010–2013 in Polish Cervical Cancer Screening Program (CCSP) and to seek for risk factors of obtaining true‐negative result (TN; not containing abnormal cells as confirmed in audit) before CC diagnosis.MethodsScreening database was merged with National Cancer Registry to identify negative slides preceding histologically confirmed CC diagnosis up to 42 months. Two blinding slides were randomly assigned per each FN. The whole set was reassessed independently by three pathologists with 30 years of experience in cytology evaluation. Final audit result was established in the case of ≥2 coherent reports. Agreement rates and kappa (κ) coefficients were calculated. Logistic analysis of risk factors for obtaining TN result was performed.ResultsOf 374 included FNs, 204 were considered abnormal (54.6%) and 91 were confirmed negative for intraepithelial neoplasia (24.3%). Agreement between experts was moderate for FNs (κ = 0.266) and fair for blinding slides (κ = 0.142) when grouping abnormal slides. Adenocarcinoma diagnosis elevated the risk of TN result (OR = 3.83); detection of macroscopic changes on the cervix and smoking lowered the risk (OR = 0.39, OR = 0.40 respectively).ConclusionsMisinterpretation was the main reason for FN cytology in the CCSP which indicated the need of further personnel training to increase screening quality. Rather low agreement between auditors requires further insight. A standardised process of auditors' selection should be planned to increase audit quality.
PIK3R3 is upregulated in liver cancer and activates Akt signaling to control cancer growth by regulation of CDKN1C and SMC1A
Authors: Lin Weidong , Wang Kunpeng , Mo Jinggang , Wang Liezhi , Song Zhenshun , Jiang Hao , Wang Cong , Jin Chong 
Published: May 2023

AbstractBackgroundLiver cancer is a highly malignant disease and the third leading cause of cancer death worldwide. Abnormal activation of PI3K/Akt signaling is common in cancer, but whether phosphoinositide‐3‐kinase regulatory subunit 3 (PIK3R3) plays a role in liver cancer is largely unexplored.MethodsWe determined the expression of PIK3R3 in liver cancer by using TCGA data and our clinical samples and knocked it down by siRNA or overexpressing it by the lentivirus vector system. We also investigated the function of PIK3R3 by colony formation, 5‐Ethynyl‐2‐Deoxyuridine, flow cytometry assay, and subcutaneous xenograft model. The downstream of PIK3R3 was explored by RNA sequence and rescue assays.ResultsWe found that PIK3R3 was significantly upregulated in liver cancer and correlated with prognosis. PIK3R3 promoted liver cancer growth in vitro and in vivo by controlling cell proliferation and cell cycle. RNA sequence revealed that hundreds of genes were dysregulated upon PIK3R3 knockdown in liver cancer cells. CDKN1C, a cyclin‐dependent kinase inhibitor, was significantly upregulated by PIK3R3 knockdown, and CDKN1C siRNA rescued the impaired tumor cell growth. SMC1A was partially responsible for PIK3R3 regulated function, and SMC1A overexpression rescued the impaired tumor cell growth in liver cancer cells. Immunoprecipitation demonstrated there is indirect interaction between PIK3R3 and CNKN1C or SMC1A. Importantly, we verified that PIK3R3‐activated Akt signaling determined the expression of CDKN1C and SMC1A, two downstream of PIK3R3 in liver cancer cells.ConclusionPIK3R3 is upregulated in liver cancer and activates Akt signaling to control cancer growth by regulation of CDNK1C and SMC1A. Targeting PIK3R3 could be a promising treatment strategy for liver cancer that deserves further investigation.
Clinical characteristics and outcomes for children, adolescents and young adults with “CIC‐fused” or “BCOR‐rearranged” soft tissue sarcomas: A multi‐institutional European retrospective analysis
Authors: Sparber‐Sauer Monika , Corradini Nadège , Affinita Maria Carmen , Milano Giuseppe Maria , Pierron Gaelle , Carton Matthieu , Tirode Franck , Pissaloux Daniel , Alaggio Rita , Vokuhl Christian , Bisogno Gianni , Berlanga Pablo , Ferrari Andrea , Orbach Daniel 
Published: May 2023

AbstractBackgroundIn certain rare undifferentiated small round cell sarcomas new specific molecular CIC‐DUX4/other partner, BCOR‐CCNB3/other partner, YWHAE fusions, or BCOR‐ITD (internal tandem duplication) were identified. These new “CIC fused” (CIC‐fused/ATXN1::NUTM1) and “BCOR rearranged” (BCOR fused/ITD/ YWHAE) soft tissue sarcomas (STS) are not well described.MethodsMulti‐institutional European retrospective analysis of young patients (0–24 years) with CIC‐fused and BCOR rearranged STS.ResultsOverall, out of the 60 patients selected, the fusion status was CIC‐fused (n = 29), ATXN1::NUTM1 (n = 2), BCOR::CCNB3 (n = 18), BCOR‐ITD (n = 7), and YWHAE (n = 3), MAML::BCOR STS (n = 1). The main primaries were abdomen‐pelvic (n = 23) and limbs (n = 18). Median age was 14 years (0.9–23.8) and 0.9 (0.1–19.1) for CIC‐fused and BCOR‐rearranged groups, respectively (n = 29; p < 0.001). IRS stages were I (n = 3), II (n = 7), III (n = 35), and IV (n = 15). Overall, 42 patients had large tumors (>5 cm) but only six had lymph node involvement. Patients received mainly chemotherapy (n = 57), local surgery (n = 50), and/or radiotherapy (n = 34). After a median follow‐up of 47.1 months (range, 3.4–230), 33 (52%) patients had an event and 23 patients died. Three‐year event‐free survivals were 44.0% (95% CI 28.7–67.5) and 41.2% (95% CI 25.4–67.0) for CIC and BCOR groups (p = 0.97), respectively. Three‐year overall survivals were 46.3% (95% CI 29.6–72.4) and 67.1% (95% CI 50.4–89.3; p = 0.24), respectively.ConclusionsPediatric patients often present with large tumors and metastatic disease, especially CIC sarcomas. Overall outcome is dismal. New treatment options are needed.
Associations of the 2018 World Cancer Research Fund/American Institute of Cancer Research (WCRF/AICR) cancer prevention recommendations with stages of colorectal carcinogenesis
Authors: Kværner Ane Sørlie , Andersen Astrid Riseth , Henriksen Hege Berg , Knudsen Markus Dines , Johansen Anne Marte Wetting , Hjartåker Anette , Bøhn Siv Kjølsrud , Paur Ingvild , Wiedswang Gro , Smeland Sigbjørn , Rounge Trine B. , Blomhoff Rune , Berstad Paula 
Published: May 2023

AbstractBackgroundWhile adherence to cancer prevention recommendations is linked to lower risk of colorectal cancer (CRC), few have studied associations across the entire spectrum of colorectal carcinogenesis. Here, we studied the relationship of the standardized 2018 World Cancer Research Fund/American Institute for Cancer Research (WCRF/AICR) Score for cancer prevention recommendations with detection of colorectal lesions in a screening setting. As a secondary objective, we examined to what extent the recommendations were being followed in an external cohort of CRC patients.MethodsAdherence to the seven‐point 2018 WCRF/AICR Score was measured in screening participants receiving a positive fecal immunochemical test and in CRC patients participating in an intervention study. Dietary intake, body fatness and physical activity were assessed using self‐administered questionnaires. Multinomial logistic regression was used to estimate odds ratios (ORs) and 95% confidence intervals (CIs) for screen‐detected lesions.ResultsOf 1486 screening participants, 548 were free from adenomas, 524 had non‐advanced adenomas, 349 had advanced lesions and 65 had CRC. Adherence to the 2018 WCRF/AICR Score was inversely associated with advanced lesions; OR 0.82 (95% CI 0.71, 0.94) per score point, but not with CRC. Of the seven individual components included in the score, alcohol, and BMI seemed to be the most influential. Of the 430 CRC patients included in the external cohort, the greatest potential for lifestyle improvement was seen for the recommendations concerning alcohol and red and processed meat, where 10% and 2% fully adhered, respectively.ConclusionsAdherence to the 2018 WCRF/AICR Score was associated with lower probability of screen‐detected advanced precancerous lesions, but not CRC. Although some components of the score seemed to be more influential than others (i.e., alcohol and BMI), taking a holistic approach to cancer prevention is likely the best way to prevent the occurrence of precancerous colorectal lesions.
An Efficient Approach for the Synthesis and Antitumor Evaluation of Novel Azo‐ and Anil‐Linked with 3‐Aminopyrazolo[3,4‐b]pyridine
Authors: El‐Bana Ghada G. , Hamama Wafaa S. , Zoorob Hanafi H. , Ibrahim Mona E. 
Published: May 2023

AbstractIn this project, an effective procedure for constructing a new combination of pyrazolo[3,4‐b]pyridine was depicted through the coupling of diazonium salt 2 of heterocyclic amine 1 with active methylene, enamine, and amidine moieties such as 3, 5, 7, and 9 at 0–5 °C in pyridine to afford hydrazinylhydrazonoyl derivatives 4, and diazenylheterocyclic derivatives 6, 8, and 10, respectively. Also, aminopyrazolo[3,4‐b]pyridine 1 condensed with different aryl or heteroaryl aldehydes in EtOH/AcOH gave the corresponding aldimine 14, 15, 16. Compound 15 was cyclized via refluxing in DMF for 6 h to afford 18, while the transformation of compound 16 with an alkyl halide afforded 19a, b. The synthesized compounds, explicated by spectral data and elemental analysis, were examined for their antitumor activities. The in vitro cytotoxic activity of new pyrazolo[3,4‐b]pyridines against the A2780CP, MCF‐7, and HepG‐2 cell lines was evaluated using the reference doxorubicin. Compounds 15 and 19a exhibited high reactivity against the A2780CP cell lines, with IC50 values of 35 and 17.9 μM, respectively. Also, compound 28 had the cytotoxic potential for A2780CP and MCF‐7 cell lines, with IC50 values of 14.5, and 27.8 μM, respectively.
Preparation of Acetylated Grapefruit Peel Polysaccharide
Authors: Yu Bingbing , Lin Bobo , Huang Gangliang 
Published: May 2023

AbstractGrapefruit peel polysaccharide has antioxidant, antitumor, hypoglycemic and other biological activities, and chemical modification can further improve the properties of the polysaccharide. Acetylation modification of polysaccharides has the advantages of simple operation, low cost and little pollution, and is widely used at present. Different degrees of acetylation modification have different effects on the properties of polysaccharides, so it is necessary to optimize the preparation technology of acetylated grapefruit peel polysaccharides. In this article, acetylated grapefruit peel polysaccharide was prepared by acetic anhydride method. With the degree of acetyl substitution as the evaluation index, combined with the analysis of sugar content and protein content in the polysaccharide before and after modification, the effects of three feeding ratios of 1:0.6, 1 : 1.2 and 1 : 1.8 (polysaccharide: acetic anhydride, mass/volume) on acetylation modification were explored through single factor experiments. The results showed that the optimum ratio of material to liquid for acetylation modification of grapefruit peel polysaccharide was 1:0.6. Under these conditions, the degree of substitution of acetylated grapefruit peel polysaccharide was 0.323, the sugar content was 59.50 % and the protein content was 1.038 %. The results provide some reference for the study of acetylated grapefruit peel polysaccharide.