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Page 1
Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.
McCoull W, Cheung T, Anderson E, Barton P, Burgess J, Byth K, Cao Q, Castaldi MP, Chen H, Chiarparin E, Carbajo RJ, Code E, Cowan S, Davey PR, Ferguson AD, Fillery S, Fuller NO, Gao N, Hargreaves D, Howard MR, Hu J, Kawatkar A, Kemmitt PD, Leo E, Molina DM, O'Connell N, Petteruti P, Rasmusson T, Raubo P, Rawlins PB, Ricchiuto P, Robb GR, Schenone M, Waring MJ, Zinda M, Fawell S, Wilson DM. McCoull W, et al. Among authors: rawlins pb. ACS Chem Biol. 2018 Nov 16;13(11):3131-3141. doi: 10.1021/acschembio.8b00698. Epub 2018 Oct 17. ACS Chem Biol. 2018. PMID: 30335946
Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.
Johannes JW, Bates S, Beigie C, Belmonte MA, Breen J, Cao S, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Ferguson AD, Habeshian S, Hargreaves D, Joubran C, Kazmirski S, Keefe AD, Lamb ML, Lan H, Li Y, Ma H, Mlynarski S, Packer MJ, Rawlins PB, Robbins DW, Shen H, Sigel EA, Soutter HH, Su N, Troast DM, Wang H, Wickson KF, Wu C, Zhang Y, Zhao Q, Zheng X, Hird AW. Johannes JW, et al. Among authors: rawlins pb. ACS Med Chem Lett. 2016 Dec 27;8(2):239-244. doi: 10.1021/acsmedchemlett.6b00464. eCollection 2017 Feb 9. ACS Med Chem Lett. 2016. PMID: 28197319 Free PMC article.
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: rawlins pb. J Med Chem. 2017 May 25;60(10):4386-4402. doi: 10.1021/acs.jmedchem.7b00359. Epub 2017 May 9. J Med Chem. 2017. PMID: 28485934
Correction to Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: rawlins pb. J Med Chem. 2017 Jul 27;60(14):6459. doi: 10.1021/acs.jmedchem.7b00962. Epub 2017 Jul 17. J Med Chem. 2017. PMID: 28714680 No abstract available.
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.
Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD, Gregory GP, Hargreaves D, Hendricks JA, Johannes JW, Johnstone RW, Kazmirski SL, Kettle JG, Lamb ML, Matulis SM, Nooka AK, Packer MJ, Peng B, Rawlins PB, Robbins DW, Schuller AG, Su N, Yang W, Ye Q, Zheng X, Secrist JP, Clark EA, Wilson DM, Fawell SE, Hird AW. Tron AE, et al. Among authors: rawlins pb. Nat Commun. 2018 Dec 17;9(1):5341. doi: 10.1038/s41467-018-07551-w. Nat Commun. 2018. PMID: 30559424 Free PMC 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: rawlins pb. 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
Antibody fragments structurally enable a drug-discovery campaign on the cancer target Mcl-1.
Luptak J, Bista M, Fisher D, Flavell L, Gao N, Wickson K, Kazmirski SL, Howard T, Rawlins PB, Hargreaves D. Luptak J, et al. Among authors: rawlins pb. Acta Crystallogr D Struct Biol. 2019 Nov 1;75(Pt 11):1003-1014. doi: 10.1107/S2059798319014116. Epub 2019 Oct 31. Acta Crystallogr D Struct Biol. 2019. PMID: 31692474 Free PMC article.
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. 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.
34 results