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- W3217012908 abstract "Future Medicinal ChemistryVol. 14, No. 3 EditorialSelective CDK9 degradation using a proteolysis-targeting chimera (PROTAC) strategyJayapal Reddy Mallareddy‡, Sarbjit Singh‡, Lidia Boghean & Amarnath NatarajanJayapal Reddy Mallareddy‡ https://orcid.org/0000-0003-0440-6617Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, NE 68198, USA‡Authors contributed equallySearch for more papers by this author, Sarbjit Singh‡Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, NE 68198, USA‡Authors contributed equallySearch for more papers by this author, Lidia Boghean https://orcid.org/0000-0003-3830-3560Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, NE 68198, USASearch for more papers by this author & Amarnath Natarajan *Author for correspondence: Tel.: +1 402 559 3793; E-mail Address: anatarajan@unmc.eduhttps://orcid.org/0000-0001-5067-0203Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, NE 68198, USADepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE 68198, USADepartment of Genetics, Cell Biology and Anatomy, University of Nebraska Medical Center, Omaha, NE 68198, USAFred and Pamela Buffett Cancer Center, University of Nebraska Medical Center, Omaha, NE 68198, USASearch for more papers by this authorPublished Online:24 Nov 2021https://doi.org/10.4155/fmc-2021-0220AboutSectionsView ArticleView Full TextPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinkedInReddit View articleKeywords: cancerCDK9degraderPROTACReferences1. 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Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat. Chem. Biol. 14(2), 163–170 (2018).Crossref, Medline, CAS, Google Scholar15. Bian J, Ren J, Li Y et al. Discovery of wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg. Chem. 81, 373–381 (2018).Crossref, Medline, CAS, Google Scholar16. Lu J, Qian Y, Altieri M et al. Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4. Chem. Biol. 22(6), 755–763 (2015).Crossref, Medline, CAS, Google Scholar17. Hu B, Zhou Y, Sun D et al. PROTACs: new method to degrade transcription regulating proteins. Eur. J. Med. Chem. 207, 112698 (2020).Crossref, Medline, CAS, Google Scholar18. Contreras JI, Robb CM, King HM et al. Chemical genetic screens identify kinase inhibitor combinations that target anti-apoptotic proteins for cancer therapy. ACS Chem. Biol. 13(5), 1148–1152 (2018).Crossref, Medline, CAS, Google Scholar19. Moreau K, Coen M, Zhang AX et al. Proteolysis-targeting chimeras in drug development: a safety perspective. Br. J. Pharmacol. 177(8), 1709–1718 (2020).Crossref, Medline, CAS, Google Scholar20. Qiu X, Li Y, Yu B et al. Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion. Eur. J. Med. Chem. 211, 113091 (2021).Crossref, Medline, CAS, Google ScholarFiguresReferencesRelatedDetails Vol. 14, No. 3 Follow us on social media for the latest updates Metrics Downloaded 325 times History Received 26 July 2021 Accepted 30 September 2021 Published online 24 November 2021 Published in print February 2022 Information© 2021 Newlands PressKeywordscancerCDK9degraderPROTACFinancial & competing interests disclosureL Boghean is supported by National Cancer Institute T32CA009476 training grant. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.No writing assistance was utilized in the production of this manuscript.PDF download" @default.
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