Pierre‐Luc Boudreault

Profiling crystal engineered ligands for targeting treatment resistant androgen receptors

This study develops and evaluates crystal-engineered ligands (CBs) for targeting treatment-resistant androgen receptors in prostate cancer, showing their potential as novel therapeutic agents.

TMPRSS6 Cleavage of β-Klotho Modulates FGF19 Signaling

The paper identifies β-Klotho as a novel substrate of TMPRSS6, showing that TMPRSS6 cleavage reduces KLB surface abundance and attenuates FGF19 signaling, linking TMPRSS6 to hepatic lipid metabolism.

A neurotensin receptor type 1-derived pepducin acts as a biased allosteric modulator to regulate target receptor function

This paper describes a pepducin derived from NTS1 that acts as a biased allosteric modulator, preferentially activating G proteins over β-arrestin and inhibiting receptor internalization.

In vitro and in vivo activity profiles of broad-spectrum bacterial ATP synthase inhibitors

The paper evaluates the antibacterial activity of tomatidine analogs against various bacterial strains, identifying TM-184 as effective against Gram-positive, Gram-negative, and multidrug-resistant bacteria, with in vivo efficacy in a mouse model.

Tunable Bias Signaling of the Angiotensin II Type 1 Receptor for Inotropy via C-Terminal Peptide Modifications and Allosteric Site Targeting

This study identifies AngII analogs with modified C-terminal peptides that selectively engage Gq or β-arrestin pathways, showing differential effects on cardiac function and blood pressure in rats.

Structural basis of TMPRSS11D specificity and autocleavage activation

The paper determines the structural basis of TMPRSS11D autocleavage activation and shows that nafamostat mesylate is cleaved by TMPRSS11D, reducing its efficacy as a protease inhibitor.

Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency

This study identifies low nanomolar TMPRSS13 inhibitors through chemical library screening and molecular modeling, showing their ability to block SARS-CoV-2 pseudovirus entry.