G protein-coupled receptors (GPCRs) constitute several membrane proteins that are turned on by hormones and
neurotransmitters to trigger cellular signaling pathways. GPCRs have been targeted in the development of several drugs
but the therapeutic potential of these proteins remains underutilized. Most drugs to date have targeted the class A, or the
rhodopsin family of GPCRs, but recently the Class B, i.e., the secretin family of G protein receptors has been targeted for
the treatment of metabolic diseases such as diabetes mellitus. Class B G protein-coupled receptors (GPCRs) have also
been targeted for managing several clinical conditions such as diabetes mellitus, bone disorders, malignancies,
neurodegeneration, cardiovascular diseases, neuropsychiatric disorders, etc. In this article, we review the medicinal
chemistry and potential clinical role of targeting GPCRs with a special emphasis on cardiovascular pharmacology.
Keywords: Beta-arrestin, cardiovascular diseases, diabetes, G protein-coupled receptor, glucagon, heart failure, hypertrophy,
ligand, rhodopsin, secretin.
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