Gonzalo E. González-Páez

TL;DR: The preclinical profile for an optimized spiroindolone drug candidate, NITD609, shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model.

TL;DR: A quantitative analysis of cysteine-reactive small-molecule fragments screened against thousands of proteins in human proteomes and cells provides a greatly expanded portrait of the ligandable proteome and furnishes compounds that can illuminate protein functions in native biological systems.

TL;DR: The genomes of 14 Plasmodium falciparum patient isolates taken recently from the Iquitos region are fully characterized using genome scanning, a microarray-based technique that delineates the majority of single-base changes, indels, and copy number variants distinguishing the coding regions of two clones.

TL;DR: Fluorescent and biotinylated probes capable of selective detection of caspase-3 using key unnatural amino acids are identified and the X-ray crystal structures ofcaspases-3, -7, and -8 in complex with the authors' lead peptide inhibitor are determined to elucidate the binding mechanism and active site interactions that promote the selective recognition of casing-3 over other highly homologous caspases family members.

TL;DR: The ability to individually target wild-type active caspases-3 for detection and cell permeable inhibition is a valuable proof-of-concept methodology that can be readily employed to probe the significance of caspase-3 in apoptosis, neurological disorders, cardiovascular diseases, and sepsis.