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: jazayeri a.
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
A series of novel allosteric antagonists of the GLP-1 receptor (GLP-1R), exemplified by HTL26119, are described. ...The region around residue C347(6.36b) of the GLP-1R receptor represents a key difference from GCGR and was targeted for selectivity for GLP-1R....
A series of novel allosteric antagonists of the GLP-1 receptor (GLP-1R), exemplified by HTL26119, are described. ...The region around …