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Page 1
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Grimster NP, Gingipalli L, Balazs A, Barlaam B, Boiko S, Boyd S, Dry H, Goldberg FW, Ikeda T, Johnson T, Kawatkar S, Kemmitt P, Lamont S, Lorthioir O, Mfuh A, Patel J, Pike A, Read J, Romero R, Sarkar U, Sha L, Simpson I, Song K, Su Q, Wang H, Watson D, Wu A, Zehnder TE, Zheng X, Li S, Dong Z, Yang D, Song Y, Wang P, Liu X, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: kawatkar s. Bioorg Med Chem Lett. 2023 Jul 15;91:129352. doi: 10.1016/j.bmcl.2023.129352. Epub 2023 Jun 2. Bioorg Med Chem Lett. 2023. PMID: 37270074
Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.
Bagal SK, Gregson C, O' Donovan DH, Pike KG, Bloecher A, Barton P, Borodovsky A, Code E, Fillery SM, Hsu JH, Kawatkar SP, Li C, Longmire D, Nai Y, Nash SC, Pike A, Robinson J, Read JA, Rawlins PB, Shen M, Tang J, Wang P, Woods H, Williamson B. Bagal SK, et al. Among authors: kawatkar sp. J Med Chem. 2021 Dec 9;64(23):17146-17183. doi: 10.1021/acs.jmedchem.1c01161. Epub 2021 Nov 22. J Med Chem. 2021. PMID: 34807608
Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
O' Donovan DH, Gregson C, Packer MJ, Greenwood R, Pike KG, Kawatkar S, Bloecher A, Robinson J, Read J, Code E, Hsu JH, Shen M, Woods H, Barton P, Fillery S, Williamson B, Rawlins PB, Bagal SK. O' Donovan DH, et al. Among authors: kawatkar s. Bioorg Med Chem Lett. 2021 May 1;39:127904. doi: 10.1016/j.bmcl.2021.127904. Epub 2021 Mar 6. Bioorg Med Chem Lett. 2021. PMID: 33684441
Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors.
Barlaam B, Boiko S, Boyd S, Dry H, Gingipalli L, Ikeda T, Johnson T, Kawatkar S, Lorthioir O, Pike A, Pollard H, Read J, Su Q, Wang H, Wang H, Wang L, Wang P, Edmondson SD. Barlaam B, et al. Among authors: kawatkar s. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127523. doi: 10.1016/j.bmcl.2020.127523. Epub 2020 Aug 30. Bioorg Med Chem Lett. 2020. PMID: 32877741
Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.
Kawatkar SP, Barlaam B, Kemmitt P, Simpson I, Watson D, Wang P, Lamont S, Su Q, Boiko S, Ikeda T, Patel J, Pike A, Pollard H, Read J, Sarkar U, Wang H, Wen Q, Yan Z, Dowling JE, Dry H, Edmondson SD. Kawatkar SP, et al. Bioorg Med Chem Lett. 2020 Sep 15;30(18):127393. doi: 10.1016/j.bmcl.2020.127393. Epub 2020 Jul 10. Bioorg Med Chem Lett. 2020. PMID: 32721854
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP, Gingipalli L, Barlaam B, Su Q, Zheng X, Watson D, Wang H, Simpson I, Pike A, Balazs A, Boiko S, Ikeda TP, Impastato AC, Jones NH, Kawatkar S, Kemmitt P, Lamont S, Patel J, Read J, Sarkar U, Sha L, Tomlinson RC, Wang H, Wilson DM, Zehnder TE, Wang L, Wang P, Goldberg FW, Shao W, Fawell S, Dry H, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: kawatkar s. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127433. doi: 10.1016/j.bmcl.2020.127433. Epub 2020 Jul 24. Bioorg Med Chem Lett. 2020. PMID: 32717371
Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Su Q, Banks E, Bebernitz G, Bell K, Borenstein CF, Chen H, Chuaqui CE, Deng N, Ferguson AD, Kawatkar S, Grimster NP, Ruston L, Lyne PD, Read JA, Peng X, Pei X, Fawell S, Tang Z, Throner S, Vasbinder MM, Wang H, Winter-Holt J, Woessner R, Wu A, Yang W, Zinda M, Kettle JG. Su Q, et al. Among authors: kawatkar s. J Med Chem. 2020 May 14;63(9):4517-4527. doi: 10.1021/acs.jmedchem.9b01392. Epub 2020 Apr 28. J Med Chem. 2020. PMID: 32297743
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex.
Hsu JH, Rasmusson T, Robinson J, Pachl F, Read J, Kawatkar S, O' Donovan DH, Bagal S, Code E, Rawlins P, Argyrou A, Tomlinson R, Gao N, Zhu X, Chiarparin E, Jacques K, Shen M, Woods H, Bednarski E, Wilson DM, Drew L, Castaldi MP, Fawell S, Bloecher A. Hsu JH, et al. Among authors: kawatkar s. Cell Chem Biol. 2020 Jan 16;27(1):41-46.e17. doi: 10.1016/j.chembiol.2019.11.004. Epub 2019 Nov 27. Cell Chem Biol. 2020. PMID: 31786184 Free article.
Rapid Identification of Novel Allosteric PRC2 Inhibitors.
Read JA, Tart J, Rawlins PB, Gregson C, Jones K, Gao N, Zhu X, Tomlinson R, Code E, Cheung T, Chen H, Kawatkar SP, Bloecher A, Bagal S, O'Donovan DH, Robinson J. Read JA, et al. Among authors: kawatkar sp. ACS Chem Biol. 2019 Oct 18;14(10):2134-2140. doi: 10.1021/acschembio.9b00468. Epub 2019 Sep 23. ACS Chem Biol. 2019. PMID: 31525019
27 results