Design and synthesis of potent and selective inhibitors of integrin VLA-4.
The synthesis and identification of a novel series of inhibitors of integrin VLA-4 are described. Their in vitro activity and selectivity against closely related integrins are also presented.
Wattanasin
S
S
Novartis Institute for Biomedical Research, Novartis Pharmaceuticals Corporation, 556 Morris Avenue, Summit, NJ 07901, USA. sompong.wattanasin@pharma.novartis.com
Weidmann
B
B
Roche
D
D
Myers
S
S
Xing
A
A
Guo
Q
Q
Sabio
M
M
von Matt
P
P
Hugo
R
R
Maida
S
S
Lake
P
P
Weetall
M
M
D018926:Anti-Allergic Agents / Q000037:antagonists & inhibitors*; D015195:Drug Design; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D016029:Receptors, Very Late Antigen / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014508:Urea / Q000737:chemistry
D018926:Anti-Allergic Agents; D039041:Integrin alpha4beta1; D016023:Integrins; D010455:Peptides; D016201:Receptors, Lymphocyte Homing; D016029:Receptors, Very Late Antigen; D014508:Urea