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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
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. Nature. 2017 Jun 8;546(7657):254-258. doi: 10.1038/nature22800. Epub 2017 May 31. Nature. 2017. PMID: 28562585
Corrigendum: 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. Nature. 2017 Aug 3;548(7665):122. doi: 10.1038/nature23311. Epub 2017 Jul 12. Nature. 2017. PMID: 28700581
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. 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
Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
Bucknell SJ, Ator MA, Brown AJH, Brown J, Cansfield AD, Cansfield JE, Christopher JA, Congreve M, Cseke G, Deflorian F, Jones CR, Mason JS, O'Brien MA, Ott GR, Pickworth M, Southall SM. Bucknell SJ, et al. J Med Chem. 2020 Jul 23;63(14):7906-7920. doi: 10.1021/acs.jmedchem.0c01003. Epub 2020 Jul 8. J Med Chem. 2020. PMID: 32558564
First-in-man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M1 -receptor partial agonist for the treatment of dementias.
Bakker C, Tasker T, Liptrot J, Hart EP, Klaassen ES, Prins S, van der Doef TF, Brown GA, Brown A, Congreve M, Weir M, Marshall FH, Cross DM, Groeneveld GJ, Nathan PJ. Bakker C, et al. Br J Clin Pharmacol. 2021 Jul;87(7):2945-2955. doi: 10.1111/bcp.14710. Epub 2021 Feb 5. Br J Clin Pharmacol. 2021. PMID: 33351971 Free PMC article. Clinical Trial.
Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study.
Bakker C, Tasker T, Liptrot J, Hart EP, Klaassen ES, Doll RJ, Brown GA, Brown A, Congreve M, Weir M, Marshall FH, Cross DM, Groeneveld GJ, Nathan PJ. Bakker C, et al. Alzheimers Res Ther. 2021 Apr 21;13(1):87. doi: 10.1186/s13195-021-00816-5. Alzheimers Res Ther. 2021. PMID: 33883008 Free PMC article. Clinical Trial.
1,118 results