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Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design.
O'Brien A, Andrews SP, Baig AH, Bortolato A, Brown AJH, Brown GA, Brown SH, Christopher JA, Congreve M, Cooke RM, De Graaf C, Errey JC, Fieldhouse C, Jazayeri A, Marshall FH, Mason JS, Mobarec JC, Okrasa K, Steele KN, Southall SM, Teobald I, Watson SP, Weir M. O'Brien A, et al. Among authors: Brown AJH, Brown GA, Brown SH. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126611. doi: 10.1016/j.bmcl.2019.08.015. Epub 2019 Aug 9. Bioorg Med Chem Lett. 2019. PMID: 31447084
Crystal structure of the GLP-1 receptor bound to a peptide agonist.
Jazayeri A, Rappas M, Brown AJH, Kean J, Errey JC, Robertson NJ, Fiez-Vandal C, Andrews SP, Congreve M, Bortolato A, Mason JS, Baig AH, Teobald I, Doré AS, Weir M, Cooke RM, Marshall FH. Jazayeri A, et al. Among authors: Brown AJH. Nature. 2017 Jun 8;546(7657):254-258. doi: 10.1038/nature22800. Epub 2017 May 31. Nature. 2017. PMID: 28562585
Extra-helical binding site of a glucagon receptor antagonist.
Jazayeri A, Doré AS, Lamb D, Krishnamurthy H, Southall SM, Baig AH, Bortolato A, Koglin M, Robertson NJ, Errey JC, Andrews SP, Teobald I, Brown AJ, Cooke RM, Weir M, Marshall FH. Jazayeri A, et al. Among authors: Brown AJ. Nature. 2016 May 12;533(7602):274-7. doi: 10.1038/nature17414. Epub 2016 Apr 25. Nature. 2016. PMID: 27111510
Cholinergic muscarinic M1 and M4 receptors as therapeutic targets for cognitive, behavioural, and psychological symptoms in psychiatric and neurological disorders.
Erskine D, Taylor JP, Bakker G, Brown AJH, Tasker T, Nathan PJ. Erskine D, et al. Among authors: Brown AJH. Drug Discov Today. 2019 Dec;24(12):2307-2314. doi: 10.1016/j.drudis.2019.08.009. Epub 2019 Sep 6. Drug Discov Today. 2019. PMID: 31499186 Review.
Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells.
Soave M, Stoddart LA, Brown A, Woolard J, Hill SJ. Soave M, et al. Version 2. Pharmacol Res Perspect. 2016 Aug 8;4(5):e00250. doi: 10.1002/prp2.250. eCollection 2016 Oct. Pharmacol Res Perspect. 2016. PMID: 27588207 Free PMC article.
Sustained wash-resistant receptor activation responses of GPR119 agonists.
Hothersall JD, Bussey CE, Brown AJ, Scott JS, Dale I, Rawlins P. Hothersall JD, et al. Eur J Pharmacol. 2015 Sep 5;762:430-42. doi: 10.1016/j.ejphar.2015.06.031. Epub 2015 Jun 20. Eur J Pharmacol. 2015. PMID: 26101059
Advances in therapeutic peptides targeting G protein-coupled receptors.
Davenport AP, Scully CCG, de Graaf C, Brown AJH, Maguire JJ. Davenport AP, et al. Among authors: Brown AJH. Nat Rev Drug Discov. 2020 Jun;19(6):389-413. doi: 10.1038/s41573-020-0062-z. Epub 2020 Mar 19. Nat Rev Drug Discov. 2020. PMID: 32494050 Review.
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