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Page 1
Selective non zinc binding inhibitors of MMP13.
De Savi C, Morley AD, Ting A, Nash I, Karabelas K, Wood CM, James M, Norris SJ, Karoutchi G, Rankine N, Hamlin G, Macfaul PA, Ryan D, Baker SV, Hargreaves D, Gerhardt S. De Savi C, et al. Among authors: hargreaves d. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4215-9. doi: 10.1016/j.bmcl.2011.05.075. Epub 2011 May 27. Bioorg Med Chem Lett. 2011. PMID: 21669521
Structure of IL-17A in complex with a potent, fully human neutralizing antibody.
Gerhardt S, Abbott WM, Hargreaves D, Pauptit RA, Davies RA, Needham MR, Langham C, Barker W, Aziz A, Snow MJ, Dawson S, Welsh F, Wilkinson T, Vaugan T, Beste G, Bishop S, Popovic B, Rees G, Sleeman M, Tuske SJ, Coales SJ, Hamuro Y, Russell C. Gerhardt S, et al. Among authors: hargreaves d. J Mol Biol. 2009 Dec 18;394(5):905-21. doi: 10.1016/j.jmb.2009.10.008. Epub 2009 Oct 14. J Mol Biol. 2009. PMID: 19835883
Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).
Scott JS, Bowker SS, Deschoolmeester J, Gerhardt S, Hargreaves D, Kilgour E, Lloyd A, Mayers RM, McCoull W, Newcombe NJ, Ogg D, Packer MJ, Rees A, Revill J, Schofield P, Selmi N, Swales JG, Whittamore PR. Scott JS, et al. Among authors: hargreaves d. J Med Chem. 2012 Jun 28;55(12):5951-64. doi: 10.1021/jm300592r. Epub 2012 Jun 19. J Med Chem. 2012. PMID: 22691057
Novel acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).
Scott JS, deSchoolmeester J, Kilgour E, Mayers RM, Packer MJ, Hargreaves D, Gerhardt S, Ogg DJ, Rees A, Selmi N, Stocker A, Swales JG, Whittamore PR. Scott JS, et al. Among authors: hargreaves d. J Med Chem. 2012 Nov 26;55(22):10136-47. doi: 10.1021/jm301252n. Epub 2012 Nov 7. J Med Chem. 2012. PMID: 23088558
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: hargreaves d. 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: hargreaves d. 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
Engineering a high-affinity anti-IL-15 antibody: crystal structure reveals an α-helix in VH CDR3 as key component of paratope.
Lowe DC, Gerhardt S, Ward A, Hargreaves D, Anderson M, Ferraro F, Pauptit RA, Pattison DV, Buchanan C, Popovic B, Finch DK, Wilkinson T, Sleeman M, Vaughan TJ, Mallinder PR. Lowe DC, et al. Among authors: hargreaves d. J Mol Biol. 2011 Feb 11;406(1):160-75. doi: 10.1016/j.jmb.2010.12.017. Epub 2010 Dec 16. J Mol Biol. 2011. PMID: 21167836
Discovery and optimization of covalent Bcl-xL antagonists.
Mukherjee H, Su N, Belmonte MA, Hargreaves D, Patel J, Tentarelli S, Aquila B, Grimster NP. Mukherjee H, et al. Among authors: hargreaves d. Bioorg Med Chem Lett. 2019 Dec 1;29(23):126682. doi: 10.1016/j.bmcl.2019.126682. Epub 2019 Sep 13. Bioorg Med Chem Lett. 2019. PMID: 31606346
Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.
Finlay MRV, Barton P, Bickerton S, Bista M, Colclough N, Cross DAE, Evans L, Floc'h N, Gregson C, Guérot CM, Hargreaves D, Kang X, Lenz EM, Li X, Liu Y, Lorthioir O, Martin MJ, McKerrecher D, McWhirter C, O'Neill D, Orme JP, Mosallanejad A, Rahi A, Smith PD, Talbot V, Ward RA, Wrigley G, Wylot M, Xue L, Yao T, Ye Y, Zhao X. Finlay MRV, et al. Among authors: hargreaves d. J Med Chem. 2021 Sep 23;64(18):13704-13718. doi: 10.1021/acs.jmedchem.1c01055. Epub 2021 Sep 7. J Med Chem. 2021. PMID: 34491761
250 results