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Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
Shirude PS, Madhavapeddi P, Naik M, Murugan K, Shinde V, Nandishaiah R, Bhat J, Kumar A, Hameed S, Holdgate G, Davies G, McMiken H, Hegde N, Ambady A, Venkatraman J, Panda M, Bandodkar B, Sambandamurthy VK, Read JA. Shirude PS, et al. Among authors: holdgate g. J Med Chem. 2013 Nov 14;56(21):8533-42. doi: 10.1021/jm4012033. Epub 2013 Oct 25. J Med Chem. 2013. PMID: 24107081
Thermal unfolding methods in drug discovery.
Llowarch P, Usselmann L, Ivanov D, Holdgate GA. Llowarch P, et al. Among authors: holdgate ga. Biophys Rev (Melville). 2023 May 16;4(2):021305. doi: 10.1063/5.0144141. eCollection 2023 Jun. Biophys Rev (Melville). 2023. PMID: 38510342 Free PMC article. Review.
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.
Ward RA, Brassington C, Breeze AL, Caputo A, Critchlow S, Davies G, Goodwin L, Hassall G, Greenwood R, Holdgate GA, Mrosek M, Norman RA, Pearson S, Tart J, Tucker JA, Vogtherr M, Whittaker D, Wingfield J, Winter J, Hudson K. Ward RA, et al. Among authors: holdgate ga. J Med Chem. 2012 Apr 12;55(7):3285-306. doi: 10.1021/jm201734r. Epub 2012 Mar 26. J Med Chem. 2012. PMID: 22417091
High-Throughput Mechanism of Inhibition.
Davies G, Semple H, McCandless M, Cairns J, Holdgate GA. Davies G, et al. Among authors: holdgate ga. SLAS Discov. 2021 Feb;26(2):248-256. doi: 10.1177/2472555220983809. SLAS Discov. 2021. PMID: 33482076 Free article.
Biophysical methods in early drug discovery.
Holdgate G, Embrey K, Milbradt A, Davies G. Holdgate G, et al. ADMET DMPK. 2019 Dec 11;7(4):222-241. doi: 10.5599/admet.733. eCollection 2019. ADMET DMPK. 2019. PMID: 35359617 Free PMC article. Review.
Prevention of MKK6-dependent activation by binding to p38alpha MAP kinase.
Sullivan JE, Holdgate GA, Campbell D, Timms D, Gerhardt S, Breed J, Breeze AL, Bermingham A, Pauptit RA, Norman RA, Embrey KJ, Read J, VanScyoc WS, Ward WH. Sullivan JE, et al. Biochemistry. 2005 Dec 20;44(50):16475-90. doi: 10.1021/bi051714v. Biochemistry. 2005. PMID: 16342939
54 results