دورية أكاديمية
A library-derived peptide inhibitor of the BZLF1 transcription factor
| العنوان: | A library-derived peptide inhibitor of the BZLF1 transcription factor |
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| المؤلفون: | Madden, Sarah, Brennan, Andrew, Mason, Jody M. |
| المصدر: | Madden , S , Brennan , A & Mason , J M 2023 , ' A library-derived peptide inhibitor of the BZLF1 transcription factor ' , Journal of Peptide Science . https://doi.org/10.1002/psc.3557Test |
| سنة النشر: | 2023 |
| مصطلحات موضوعية: | BZLF1, PCA, ZEBRA, peptide antagonists, peptide screening, transcription factor, /dk/atira/pure/subjectarea/asjc/3000/3002, name=Drug Discovery, /dk/atira/pure/subjectarea/asjc/1300/1313, name=Molecular Medicine, /dk/atira/pure/subjectarea/asjc/1300/1312, name=Molecular Biology, /dk/atira/pure/subjectarea/asjc/1300/1315, name=Structural Biology, /dk/atira/pure/subjectarea/asjc/1300/1303, name=Biochemistry, /dk/atira/pure/subjectarea/asjc/3000/3004, name=Pharmacology, /dk/atira/pure/subjectarea/asjc/1600/1605, name=Organic Chemistry, /dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being, name=SDG 3 - Good Health and Well-being |
| الوصف: | Transcription factor dysregulation is associated with many diseases, including cancer. Peptide-based molecules are increasingly recognised as important modulators of difficult intracellular protein–protein interaction targets, with peptide library screening consequently proven to be a viable strategy in developing inhibitors against a wide range of transcription factors (TFs). However, current strategies simply select the highest affinity of binding to a target TF rather than the ability to inhibit TF function. Here, we utilise our Transcription Block Survival (TBS) screening platform to enable high-throughput identification of peptides that inhibit TFs from binding to cognate DNA sites, hence inhibiting functionality. In this study, we explore whether the TBS can be expanded to derive a potent and functional peptide inhibitor of the BZLF1 transcription factor. The library-derived peptide, AcidicW, is shown to form a more stable dimer with BZLF1 than the BZLF1 homodimer, with a thermal denaturation temperature exceeding 80°C. AcidicW can also functionally inhibit the BZLF1:TRE DNA interaction with high potency and an IC50 of 612 nM. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| العلاقة: | https://researchportal.bath.ac.uk/en/publications/79c74d26-cbdd-4383-90cf-586bb3f16450Test |
| DOI: | 10.1002/psc.3557 |
| الإتاحة: | https://doi.org/10.1002/psc.3557Test https://researchportal.bath.ac.uk/en/publications/79c74d26-cbdd-4383-90cf-586bb3f16450Test http://www.scopus.com/inward/record.url?scp=85178479901&partnerID=8YFLogxKTest |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.8EF670CF |
| قاعدة البيانات: | BASE |
| DOI: | 10.1002/psc.3557 |
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