Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
Liu
J
J
Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
Underwood
D J
DJ
Cascieri
M A
MA
Rohrer
S P
SP
Cantin
L D
LD
Chicchi
G
G
Smith
A B
AB
Hirschmann
R
R
D000818:Animals; D016466:CHO Cells; D019556:COS Cells; D006224:Cricetinae; D005960:Glucosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D008565:Membrane Proteins; D018716:Molecular Mimicry; D064729:Neurokinin-1 Receptor Antagonists; D018040:Receptors, Neurokinin-1 / Q000378:metabolism; D017481:Receptors, Somatostatin / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013004:Somatostatin / Q000819:agonists / Q000737:chemistry*; D013373:Substance P / Q000037:antagonists & inhibitors*
D005960:Glucosides; D008565:Membrane Proteins; D064729:Neurokinin-1 Receptor Antagonists; D018040:Receptors, Neurokinin-1; D017481:Receptors, Somatostatin; C098681:somatostatin receptor subtype-4; D013373:Substance P; D013004:Somatostatin