TY - JOUR
AU - Lam, Kit S.
AB - α4β1 integrin is a therapeutic target for inflammation, autoimmune diseases, and lymphoid cancers. A series of peptidomimetic ligands based on the Nle‐D‐I motif have been synthesized and their binding affinities (IC50) to activated α4β1 integrin on Jurkat T‐leukemia cells have been determined using a cell adhesion assay. One of the 51 ligands, 18, has been determined to have an IC50 of 0.6 nM and has a more than twofold increase of binding affinity than the initial lead compound 1. Extensive SAR studies provide important information for further ligand optimization, which has served as a foundation for studies that ultimately led to identification of a potent ligand with an IC50 of 2 pM. © 2006 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 84: 595–604, 2006 This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com
TI - Structure–activity relationship studies of a series of peptidomimetic ligands for α 4 β 1 integrin on Jurkat T‐leukemia cells
JF - Biopolymers
DO - 10.1002/bip.20588
DA - 2006-01-01
UR - https://www.deepdyve.com/lp/wiley/structure-activity-relationship-studies-of-a-series-of-peptidomimetic-IUv8A70Amq
SP - 595
EP - 604
VL - 84
IS - 6
DP - DeepDyve
ER -