Welcome to the Tesmer Lab

The structural basis of signal transduction

The structural basis of signal transduction

G protein-coupled receptors (GPCRs) are responsible for the sensations of sight and smell, for regulation of blood pressure and heart rate, and for many other cellular events. Signals impinging upon the exterior of the cell induce a conformational change in these GPCRs that allows them to activate heterotrimeric G proteins within the cell. The activated G proteins then bind to various effectors that initiate downstream cascades, leading to profound physiological change. In pathological settings, they contribute to maladaptive processes such as heart failure, hypertension, tumor growth and metastasis.

We study the molecular basis of GPCR-mediated signal transduction, principally via the technique of X-ray crystallography. By determining atomic structures of signaling proteins alone and in complex with their various targets, we can provide important insights into the molecular basis of signal transduction and how diseases result from dysfunctional regulation.

The lab is also interested in rational drug design and the development of biotherapeutic enzymes. We currently have a robust drug development program aimed at a family of GPCR kinases (GRKs) wherein we are seeking to identify potent and selective inhibitors of GRKs involved in cardiovascular disease. We also are investigating the structure and function of LCAT, a key enzyme in reverse cholesterol transport with the goal of understanding its activation by HDL particles and its design into a therapy for human somatic disease and acute coronary syndrome.

Lab news

December 2017:

January 2018:

Professor Tesmer and his lab students  Professor Tesmer and his lab group

March 2018:

April 2018:

Tesmer lab at the 5K Challenge run

May 2018:



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