Armando G. Villaseñor

TL;DR: The first structure of a mammalian 15-lipoxygenase is reported, comprising a catalytic domain and a previously unrecognized β-barrel domain, which provides a unifying hypothesis for the positional specificity of mammalian lipoxygenases.

TL;DR: The development of a new core structure of p38 inhibitors, 3-(4-fluorophenyl)-2-(pyridin-4-yl)-1H-pyrrolo[3,2-b] pyridine, is described, which identified 42c as a potent inhibitor of p 38, which also possessed the required physical properties worthy of advanced studies.

TL;DR: Structural-based optimization of diaryl ether inhibitors led to the discovery of a new series of pyrazolo[3,4-c]pyridazine NNRTIs that bind the reverse transcriptase enzyme of human immunodeficiency virus-1 (HIV-RT) in an expanded volume relative to most other inhibitors in this class.

TL;DR: An analysis of the binding motifs of known HIV-1 non-nucleoside reverse transcriptase inhibitors has led to discovery of novel piperidine-linked aminopyrimidine derivatives with broad activity against wild-type as well as drug-resistant mutant viruses.

TL;DR: The crystal structures of the apo and ligand-bound forms of human IRAK4 kinase domain reveal several features that provide opportunities for the design of selective IRAK 4 inhibitors and provide insights into the regulation of its activity.