Medicinal Chemistry-Fusion of Traditional and Western Medicine

Volume: 1

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Medicinal Chemistry - Fusion of Traditional and Western Medicine is a textbook intended for students taking courses in the various fields of medicinal chemistry, pharmacy, medical and dental ...
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Biology of Information Flow, Receptors and Signaling

Pp. 599-640 (42)

Robert E. Smith

Abstract

The most common second messenger is Ca2+, which is stored in the type of endoplasmic reticulum (ER). Some of the other important second messengers include IP3 and diacyl glycerol (produced by the hydrolysis of phosphoinositides), arachidonic acid (produced by the hydrolysis of phospholipids that have arachidonoyl on carbon number 2 of the glycerol backbone), ceramide, eicosanoids, lysophosphatidic acid, NO (nitric oxide), cAMP and cGMP. The most common type of receptor is the G proteincoupled receptor (GPCR). Protein kinases can catalyze the addition of a phosphate to another protein or even to themselves and affect signal transduction. Another class of G proteins is called the small GTPases. Nuclear receptors (NRs) play key roles in growth, development and homeostasis. Lipohilic natural hormones diffuse past the cell membrane and bind to receptors located in either the cytosol (type I NR) or the nucleus (type II NR). The IP3 receptor, or IP3R is a membrane-bound complex of glycoproteins. It is a Ca2+ channel that is activated by IP3, which is a secondary intra-cellular messenger. Inter-and intracellular communication can be considered as a network that contains many items (nodes) that have about one to thousands of connections. The most widely connected nodes are called hubs. Probably, the major genetic hub in human and many other mammalian cells is the gene TP53 which codes for the protein p53. About 50% of all human cancers have one or more mutations in p53 that alter DNA transcription.

Keywords:

Calcium, Ca2+, IP3, diacyl glycerol, arachidonic acid, ceramide, eicosanoids, lysophosphatidic acid, nitric oxide, cAMP, cGMP, GPCR.

Affiliation:

Adjunct Assistant Professor Park University and Consultant Science Advisor United States Food and Drug Administration (FDA) USA