Abstract

ALLOSTERIC MODULATORS OF GPCR & THEIR POTENTIAL THERAPEUTIC APPLICATIONS

Dr. A. Avinash, Dr. Navin Patil*, Dr. Sushil Kiran Kunder, Dr. Anurag Pathak, Dr. Smita Shenoy, Dr. K.L.Bairy

Abstract

Paul Ehrlich brought in a revolution in the field of receptor biology, when he postulated that “Corpora non agunt nisi fixata”, which translates roughly into “Agents will not act unless they are bound”.[1] His postulate led on to the discovery of various regulatory proteins that are now targeted by most drugs in the market. Membrane receptors form a major chunk of these regulatory proteins. Membrane receptors are specialized integral membrane proteins to which external signaling molecules bind and trigger various functional changes. G-protein coupled receptors are the most widely distributed membrane receptors in the human body. The first G-protein coupled receptor (GPCR) was cloned way back in 1986, and this was the beta-adrenergic receptor.[2]

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