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Development of allosteric and selective CDK2 inhibitors for contraception with negative cooperativity to cyclin binding.
Faber EB, Sun L, Tang J, Roberts E, Ganeshkumar S, Wang N, Rasmussen D, Majumdar A, Hirsch LE, John K, Yang A, Khalid H, Hawkinson JE, Levinson NM, Chennathukuzhi V, Harki DA, Schönbrunn E, Georg GI. Faber EB, et al. Among authors: harki da. Nat Commun. 2023 Jun 3;14(1):3213. doi: 10.1038/s41467-023-38732-x. Nat Commun. 2023. PMID: 37270540 Free PMC article.
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Divakaran A, Talluri SK, Ayoub AM, Mishra NK, Cui H, Widen JC, Berndt N, Zhu JY, Carlson AS, Topczewski JJ, Schonbrunn EK, Harki DA, Pomerantz WCK. Divakaran A, et al. Among authors: harki da. J Med Chem. 2018 Oct 25;61(20):9316-9334. doi: 10.1021/acs.jmedchem.8b01248. Epub 2018 Oct 16. J Med Chem. 2018. PMID: 30253095 Free PMC article.
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.
Cui H, Divakaran A, Hoell ZJ, Ellingson MO, Scholtz CR, Zahid H, Johnson JA, Griffith EC, Gee CT, Lee AL, Khanal S, Shi K, Aihara H, Shah VH, Lee RE, Harki DA, Pomerantz WCK. Cui H, et al. Among authors: harki da. J Med Chem. 2022 Feb 10;65(3):2342-2360. doi: 10.1021/acs.jmedchem.1c01779. Epub 2022 Jan 10. J Med Chem. 2022. PMID: 35007061 Free PMC article.
First-in-class small molecule inhibitors of the single-strand DNA cytosine deaminase APOBEC3G.
Li M, Shandilya SM, Carpenter MA, Rathore A, Brown WL, Perkins AL, Harki DA, Solberg J, Hook DJ, Pandey KK, Parniak MA, Johnson JR, Krogan NJ, Somasundaran M, Ali A, Schiffer CA, Harris RS. Li M, et al. Among authors: harki da. ACS Chem Biol. 2012 Mar 16;7(3):506-17. doi: 10.1021/cb200440y. Epub 2012 Jan 17. ACS Chem Biol. 2012. PMID: 22181350 Free PMC article.
4-Methyl-1,2,3-Triazoles as N-Acetyl-Lysine Mimics Afford Potent BET Bromodomain Inhibitors with Improved Selectivity.
Cui H, Carlson AS, Schleiff MA, Divakaran A, Johnson JA, Buchholz CR, Zahid H, Vail NR, Shi K, Aihara H, Harki DA, Miller GP, Topczewski JJ, Pomerantz WCK. Cui H, et al. Among authors: harki da. J Med Chem. 2021 Jul 22;64(14):10497-10511. doi: 10.1021/acs.jmedchem.1c00933. Epub 2021 Jul 8. J Med Chem. 2021. PMID: 34236185 Free PMC article.
70 results