Murray McKinnon

TL;DR: It is demonstrated that siglec-10 is an immune system-restricted membrane-bound protein that is highly expressed in peripheral blood leukocytes as demonstrated by Northern, RT-PCR and flow cytometry and the genomic sequence was localized within the cluster of genes on chromosome 19q13.3-4 that encode other Siglec family members.

TL;DR: Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38alpha MAP kinase are described and the issue of metabolic instability associated with vicinal phenyl, benzo[d]thiazol-6-yl oxazoles/imidazoles was addressed by the replacement of the central oxazole or imidazole ring with an aminopyrazole system.

TL;DR: The synthesis and structure-activity relationships (SAR) of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds and x-ray co-crystallography of an oxalamide analog bound to unphosphorylated p37alpha led to the identification of compound (21) as a potent inhibitor of p 38alphaMAP kinase with good cellular potency toward the inhibition of TNF-alpha production.

TL;DR: The discovery and preliminary SAR of spirocyclic hydantoin based LFA-1 antagonists that culminated in the identification of analog 8 as a clinical candidate are described and the first example of the efficacy of a small molecule L FA-1 antagonist in combination with CTLA-4Ig in an animal model of transplant rejection is reported.