Aminopyrrolidineamide inhibitors of site-1 protease.
The discovery and efficacy of a series of potent aminopyrrolidineamide-based inhibitors of sterol regulatory element binding protein site-1 protease is described.
Hay
Bruce A
BA
Pfizer Global Research and Development-Groton Laboratories, Groton, CT 06340, USA. burce_hay@sbcglobal.net
Abrams
Barbara
B
Zumbrunn
Allice Y
AY
Valentine
James J
JJ
Warren
Laurie C
LC
Petras
Stephen F
SF
Shelly
Lorraine D
LD
Xia
Angela
A
Varghese
Alison H
AH
Hawkins
Julie L
JL
Van Camp
Jennifer A
JA
Robbins
Michael D
MD
Landschulz
Katherine
K
Harwood
H James
HJ
D021581:Active Transport, Cell Nucleus / Q000187:drug effects; D000818:Animals; D020650:Combinatorial Chemistry Techniques; D005786:Gene Expression Regulation; D006801:Humans; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008297:Male; D051379:Mice; D015394:Molecular Structure; D043484:Proprotein Convertases / Q000037:antagonists & inhibitors*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D012697:Serine Endopeptidases; D051779:Sterol Regulatory Element Binding Proteins / Q000378:metabolism
D000960:Hypolipidemic Agents; D011758:Pyrroles; D051779:Sterol Regulatory Element Binding Proteins; D043484:Proprotein Convertases; D012697:Serine Endopeptidases; C115575:membrane-bound transcription factor peptidase, site 1