Targeting STAT proteins via computational analysis in colorectal cancer

التفاصيل البيبلوغرافية
العنوان: Targeting STAT proteins via computational analysis in colorectal cancer
المؤلفون: Saimila Momin, Santoshi Muppala, Gowru Srivani, Afroz Alam, Begum Dariya, Madhu Sudhana Saddala
المصدر: Molecular and Cellular Biochemistry. 476:165-174
بيانات النشر: Springer Science and Business Media LLC, 2020.
سنة النشر: 2020
مصطلحات موضوعية: STAT3 Transcription Factor, 0301 basic medicine, Magnetic Resonance Spectroscopy, Clinical Biochemistry, Genistein, SH2 domain, stat, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Protein Domains, Humans, STAT1, STAT2, STAT3, Molecular Biology, Transcription factor, Cell Proliferation, Inflammation, Binding Sites, biology, Chemistry, Computational Biology, STAT2 Transcription Factor, Cell Biology, General Medicine, HCT116 Cells, Molecular Docking Simulation, STAT1 Transcription Factor, 030104 developmental biology, 030220 oncology & carcinogenesis, Mutagenesis, Site-Directed, STAT protein, Cancer research, biology.protein, Colorectal Neoplasms, HT29 Cells, Protein Processing, Post-Translational, Signal Transduction
الوصف: Colorectal cancer (CRC) is the third most common cancer diagnosed worldwide making it a serious global challenge. CRC progression results from dysregulated cytoplasmic transcription factors, including signal transducer and activator of transcription (STAT) proteins that are involved in JAK-STAT pathway. The STAT proteins contain a conserved SH2 domain that facilitates the initiation of STAT activation via binding to tyrosine motifs followed by STAT dimerization. The STAT proteins include STAT1, STAT2 and STAT3 which all facilitate therapeutic targets for many drugs, since they are associated with pathogenesis in various cancers such as CRC. Genistein is an efficient chemopreventive phytochemical drug against CRC. The current investigation presents a computational study performed to investigate the molecular interaction between STAT1, STAT2 and STAT3 proteins with genistein. The molecular dynamic simulation was conducted for STAT2 protein. The studies from molecular docking revealed that the interaction of STAT proteins and genistein is predicted to be effective with better binding energies. Furthermore, targeting STAT3 could be an efficient therapeutic target and understanding the interaction between STAT3 and genistein can help to contribute to a better inhibition process for CRC progression. Treatment with genistein led to significant suppression of cell proliferation and STAT3 protein expression in both CRC (HCT 116 and HT-29) cell lines. This further provides development of efficient STAT inhibitors with better potency and bioavailability.
تدمد: 1573-4919
0300-8177
الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49d27bd1b7252e5e4163649a6a4a5a1bTest
https://doi.org/10.1007/s11010-020-03893-6Test
حقوق: CLOSED
رقم الانضمام: edsair.doi.dedup.....49d27bd1b7252e5e4163649a6a4a5a1b
قاعدة البيانات: OpenAIRE