The Structure and Function of G Protein-Coupled Receptors

For those who may wish to understand my and my collaborator's work on the structure and function of G protein-coupled receptors, I’ve provided the following links to the papers that are most important for understanding this work. I like to bunch them into groups of three. First are:


Weber's Law Modeled by the Mathematical Description of a Beam Balance, Mathematical Biosciences 122: 89-94 (1994)

Method for determining drug compositions to prevent desensitization of cellular receptors, US Patent # 5,597,699 (1997)

Activation of G Protein-Coupled Receptors Entails Cysteine Modulation of Agonist Binding, J. Molecular Structure (Theochem), 430/1-3: 57-71 (1998)

The next three papers are:

Compositions to enhance the safety and efficacy of bio-pharmaceutical drugs. US Patent# 6,593,094 (2003)

Optimal Agonist/Antagonist Combinations Maintain Receptor Response by Preventing Rapid Beta-1 adrenergic Receptor Desensitization Intl. J. Pharmacol., 1(2): 122-131, (2005)

Molecular dynamics of a biophysical model for beta-2-adrenergic and G protein-coupled receptor activation Journal of Molecular Graphics and Modelling 25: 396-409 (2006)

Evidence for a free thiol necessary for GPCR activation

P2Y12, a G protein-coupled receptor that plays a central role in platelet activation is the receptor targeted by the antithrombotic drug, clopidogrel. The mechanism of action of clopidogrel involved cysteine 97 within the first extracellular loop of P2Y12. This provides supporting evidence for a free thiol or sulfhydryl group necessary for GPCR activation.

See - http://www.pnas.org/content/103/29/11069.full and http://www.bio-balance.com/Ref.htm