Rational development of a high-affinity secretin receptor antagonist.
Dong M, Harikumar KG, Raval SR, Milburn JE, Clark C, Alcala-Torano R, Mobarec JC, Reynolds CA, Ghirlanda G, Christopoulos A, Wootten D, Sexton PM, Miller LJ.
Dong M, et al.
Biochem Pharmacol. 2020 Jul;177:113929. doi: 10.1016/j.bcp.2020.113929. Epub 2020 Mar 23.
Biochem Pharmacol. 2020.
PMID: 32217097
Free PMC article.
Alanine-replacement mutagenesis of these residues markedly affected ligand binding and biological activity. The optimal antagonist ligand, (Y(10),c[E(16),K(20)],I(17),Cha(22),R(25))sec(6-27), exhibited high binding affinity (4 nM), similar to natural secretin, and exhibite …
Alanine-replacement mutagenesis of these residues markedly affected ligand binding and biological activity. The optimal antagonist ligand, ( …