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4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA. Liddle J, et al. Among authors: whitworth c. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5222-6. doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26. Bioorg Med Chem Lett. 2012. PMID: 22801646
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
Liddle J, Bamborough P, Barker MD, Campos S, Cousins RP, Cutler GJ, Hobbs H, Holmes DS, Ioannou C, Mellor GW, Morse MA, Payne JJ, Pritchard JM, Smith KJ, Tape DT, Whitworth C, Williamson RA. Liddle J, et al. Among authors: whitworth c. Bioorg Med Chem Lett. 2009 May 1;19(9):2504-8. doi: 10.1016/j.bmcl.2009.03.034. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19349179
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.
Chan C, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chaudry L, Chung CW, Convery MA, Hamblin JN, Johnstone L, Kelly HA, Kleanthous S, Patikis A, Patel C, Pateman AJ, Senger S, Shah GP, Toomey JR, Watson NS, Weston HE, Whitworth C, Young RJ, Zhou P. Chan C, et al. Among authors: whitworth c. J Med Chem. 2007 Apr 5;50(7):1546-57. doi: 10.1021/jm060870c. Epub 2007 Mar 6. J Med Chem. 2007. PMID: 17338508
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.
Watson NS, Brown D, Campbell M, Chan C, Chaudry L, Convery MA, Fenwick R, Hamblin JN, Haslam C, Kelly HA, King NP, Kurtis CL, Leach AR, Manchee GR, Mason AM, Mitchell C, Patel C, Patel VK, Senger S, Shah GP, Weston HE, Whitworth C, Young RJ. Watson NS, et al. Among authors: whitworth c. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. doi: 10.1016/j.bmcl.2006.04.053. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697194
P300 Modulates Endothelial Mechanotransduction of Fluid Shear Stress.
Whitworth CP, Aw WY, Doherty EL, Handler C, Ambekar Y, Sawhney A, Scarcelli G, Polacheck WJ. Whitworth CP, et al. Cell Mol Bioeng. 2024 Jun 11;17(5):507-523. doi: 10.1007/s12195-024-00805-2. eCollection 2024 Oct. Cell Mol Bioeng. 2024. PMID: 39513009
Targeting cancer with small-molecule pan-KRAS degraders.
Popow J, Farnaby W, Gollner A, Kofink C, Fischer G, Wurm M, Zollman D, Wijaya A, Mischerikow N, Hasenoehrl C, Prokofeva P, Arnhof H, Arce-Solano S, Bell S, Boeck G, Diers E, Frost AB, Goodwin-Tindall J, Karolyi-Oezguer J, Khan S, Klawatsch T, Koegl M, Kousek R, Kratochvil B, Kropatsch K, Lauber AA, McLennan R, Olt S, Peter D, Petermann O, Roessler V, Stolt-Bergner P, Strack P, Strauss E, Trainor N, Vetma V, Whitworth C, Zhong S, Quant J, Weinstabl H, Kuster B, Ettmayer P, Ciulli A. Popow J, et al. Among authors: whitworth c. Science. 2024 Sep 20;385(6715):1338-1347. doi: 10.1126/science.adm8684. Epub 2024 Sep 19. Science. 2024. PMID: 39298590
Confounding Factors in Targeted Degradation of Short-Lived Proteins.
Vetma V, Perez LC, Eliaš J, Stingu A, Kombara A, Gmaschitz T, Braun N, Ciftci T, Dahmann G, Diers E, Gerstberger T, Greb P, Kidd G, Kofink C, Puoti I, Spiteri V, Trainor N, Weinstabl H, Westermaier Y, Whitworth C, Ciulli A, Farnaby W, McAulay K, Frost AB, Chessum N, Koegl M. Vetma V, et al. Among authors: whitworth c. ACS Chem Biol. 2024 Jul 19;19(7):1484-1494. doi: 10.1021/acschembio.4c00152. Epub 2024 Jul 3. ACS Chem Biol. 2024. PMID: 38958654
175 results