T. P. Sakmar

Itch receptor MRGPRX4 interacts with the receptor activity-modifying proteins (RAMPs)

This study identifies that MRGPRX4 interacts with RAMP2, reducing its signaling and surface expression, and predicts the structure of the MRGPRX4-RAMP2 complex.

Multiplexed selectivity screening of anti-GPCR antibodies

The paper screens 400 anti-GPCR antibodies for selectivity using a multiplexed immunoassay against 215 solubilized GPCRs, finding 61% are selective, 11% bind off-target, and 28% bind none.

Entry Pathway for the Inverse Agonist Ligand in the G Protein-Coupled Receptor Rhodopsin

This study investigates the pathway for 11-cis-retinal entry into rhodopsin, finding that it enters through a transmembrane channel between TM5/6, controlled by dynamic allosteric mechanisms.

Frizzled BRET sensors based on bioorthogonal labeling of unnatural amino acids reveal WNT-induced dynamics of the cysteine-rich domain.

The paper develops BRET-based biosensors to study WNT-induced conformational changes in FZD CRD and shows CRD dynamics are not required for WNT/β-catenin signaling.

Uveal Melanoma Oncogene CYSLTR2 Encodes a Constitutively Active GPCR Highly Biased Toward Gq Signaling

Multiplexed Analysis of the Secretin-like GPCR-RAMP Interactome

This study identifies GPCR-RAMP interactions using a suspension bead array assay, revealing widespread interactions among secretin-like GPCRs and RAMPs.

High-Affinity Binding of Chemokine Analogs that Display Ligand Bias at the HIV-1 Co-receptor CCR5

The paper develops a fluorescence assay to study high-affinity chemokine analogs that show ligand bias at CCR5, finding they bind with subnanomolar affinities and occupy a site not accessible to native chemokines.

DNA-Encircled Lipid Bilayers

This paper introduces DNA-encircled bilayers (DEBs) as a novel membrane-mimetic system for studying lipid phases and membrane proteins with precise control over size and functionalization.