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Page 1
Structural insight into allosteric modulation of protease-activated receptor 2.
Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N. Cheng RKY, et al. Among authors: brown ga, brown dg. Nature. 2017 May 4;545(7652):112-115. doi: 10.1038/nature22309. Epub 2017 Apr 26. Nature. 2017. PMID: 28445455
Agonists and Antagonists of Protease-Activated Receptor 2 Discovered within a DNA-Encoded Chemical Library Using Mutational Stabilization of the Target.
Brown DG, Brown GA, Centrella P, Certel K, Cooke RM, Cuozzo JW, Dekker N, Dumelin CE, Ferguson A, Fiez-Vandal C, Geschwindner S, Guié MA, Habeshian S, Keefe AD, Schlenker O, Sigel EA, Snijder A, Soutter HT, Sundström L, Troast DM, Wiggin G, Zhang J, Zhang Y, Clark MA. Brown DG, et al. Among authors: brown ga. SLAS Discov. 2018 Jun;23(5):429-436. doi: 10.1177/2472555217749847. Epub 2018 Jan 9. SLAS Discov. 2018. PMID: 29316408 Free article.
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 ga, brown sh, brown ajh. 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
Author Correction: Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits.
Palacios-Filardo J, Udakis M, Brown GA, Tehan BG, Congreve MS, Nathan PJ, Brown AJH, Mellor JR. Palacios-Filardo J, et al. Among authors: brown ga, brown ajh. Nat Commun. 2021 Dec 8;12(1):7265. doi: 10.1038/s41467-021-27351-z. Nat Commun. 2021. PMID: 34880229 Free PMC article. No abstract available.
Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity.
Borodovsky A, Barbon CM, Wang Y, Ye M, Prickett L, Chandra D, Shaw J, Deng N, Sachsenmeier K, Clarke JD, Linghu B, Brown GA, Brown J, Congreve M, Cheng RK, Dore AS, Hurrell E, Shao W, Woessner R, Reimer C, Drew L, Fawell S, Schuller AG, Mele DA. Borodovsky A, et al. Among authors: brown ga, brown j. J Immunother Cancer. 2020 Jul;8(2):e000417. doi: 10.1136/jitc-2019-000417. J Immunother Cancer. 2020. PMID: 32727810 Free PMC article.
From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD, Dwomoh L, Dias JM, Errey JC, Hurrell E, Liptrot J, Mattedi G, Molloy C, Nathan PJ, Okrasa K, Osborne G, Patel JC, Pickworth M, Robertson N, Shahabi S, Bundgaard C, Phillips K, Broad LM, Goonawardena AV, Morairty SR, Browning M, Perini F, Dawson GR, Deakin JFW, Smith RT, Sexton PM, Warneck J, Vinson M, Tasker T, Tehan BG, Teobald B, Christopoulos A, Langmead CJ, Jazayeri A, Cooke RM, Rucktooa P, Congreve MS, Weir M, Tobin AB. Brown AJH, et al. Among authors: brown ga, brown j. Cell. 2021 Nov 24;184(24):5886-5901.e22. doi: 10.1016/j.cell.2021.11.001. Cell. 2021. PMID: 34822784 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. Among authors: brown ga, brown a. 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.
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. Among authors: brown ga, brown a. 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.
279 results