The Athan Kuliopulos Lab

Research Publications Biochemistry Cell Biology Genetics


Protease-Activated Receptors in Inflammation and Vascular Biology 

Protease-activated receptors (PARs) are a unique class of G protein-coupled receptors that play critical roles in thrombosis, inflammation, and vascular biologyThe PARs are cleaved by thrombin and other proteases at a specific peptide bond to expose a new N-terminus that binds to the body of the receptor in an unusual intramolecular mode. A major interest of our research group is to study the molecular mechanism of protease activation of the PARs and the subsequent signaling in vascular cells and in cancer.

Kuliopulos Fig 1

Figure 1. Interest in PARs and their role in physiology and disease has heightened in recent years.

PARs and Thrombosis

Thrombosis associated with the pathophysiological activation of platelets and vascular cells has brought thrombin and its receptors to the forefront of cardiovascular medicine. Protease signaling through the protease-activated receptors (PARs) has been shown to influence a wide range of physiological responses including platelet activation, intimal hyperplasia, inflammation, and maintenance of vascular tone and barrier function.

Kuliopulos Fig 1

Figure 2. The figure illustrates interactions with PARs and several of the physiological responses to the interaction.

Pepducins as Novel Cell-Penetrating Intracellular Agonists and Antagonists of G Protein-Coupled Receptors

We have established a new technology based on cell-penetrating peptides known as pepducins as a novel approach of activating or inhibiting signaling between selected receptors and G proteins. These cell-penetrating pepducins are powerful tools to evaluate PARs, chemokines, and other receptors as potential therapeutic targets in both in vitro and mouse model systems.

Kuliopulos Fig 2

Figure 3. A model of pepducin-mediated effects is shown.

Apply to the Sackler School


The priority application deadlines are as follows:

December 1: Basic Science Division PhD Programs

February 15: Building Diversity in Biomedical Sciences

March 31: Post-Baccalaureate Research Program

May 1: Clinical & Translational Science, MS in Pharmacology & Drug Development

June 15: Online Certificate in Fundamentals of Clinical Care Research