Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor.

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Research Abstract Details 

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Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Abstract Text:

Victor J Hruby,Minying Cai,James P Cain,Alexander V Mayorov,Matthew M Dedek,Devendra Trivedi,Victor J Hruby,Minying Cai,James P Cain,Alexander V Mayorov,Matthew M Dedek,Devendra Trivedi,

The processed products of the proopiomelanocortin gene (ACTH, alpha-MSH, beta-MSH, gamma-MSH, etc.) interact with five melanocortin receptors, the MC1R, MC2R, MC3R, MC4R, and MC5R to modulate and control many important biological functions crucial for good health both peripherally (as hormones) and centrally (as neurotransmitters). Pivotal biological functions include pigmentation, adrenal function, response to stress, fear/flight, energy homeostasis, feeding behavior, sexual function and motivation, pain, immune response, and many others, and are believed to be involved in many disease states including pigmentary disorders, adrenal disorders, obesity, anorexia, prolonged and neuropathic pain, inflammatory response, etc. The melanocortin-3 receptor (MC3R) is found primarily in the brain and spinal cord and also in the periphery, and its biological functions are still not well understood. Here we review some of the biological functions attributed to the MC3R, and then examine in more detail efforts to design and synthesize ligands that are potent and selective for the MC3R, which might help resolve the many questions still remaining about its function. Though some progress has been made, there is still much to be done in this critical area.

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Publishing Authors By Initials

VJ Hruby,M Cai,JP Cain,AV Mayorov,MM Dedek,D Trivedi,VJ Hruby,M Cai,JP Cain,AV Mayorov,MM Dedek,D Trivedi,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: substrate specificity research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: substrate specificity research

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Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Journal Published:

PUBLICATION TYPE: Review

Journal: Current topics in medicinal chemistry

VOLUME: 7

Page Numbers: 1107-19

Journal Abbreviation:

ISSN: 1873-4294

DAY: 3

MONTH: 12

YEAR: 2007

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Information

Number of References: 111

LANGUAGE: eng

NlmUniqueID: 101119673

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Keywords Mesh Terms:

KEYWORDS: Substrate Specificity

MESH TERMS: metabolism

Chemical & Substance for Abstract: Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Information

Substance Name: Melanocyte-Stimulating Hormones

Registry Number: 9002-79-3

Grant and Affiliation Information for Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor.

AFFILIATION: Department of Chemistry, University of Arizona, Tucson, Arizona 85721, USA. hruby@u.arizona.edu

Country: Netherlands

AGENCY: United States NIDDK

GRANT: DK17420

ACRONYM: DK

MEDLINETA: Curr Top Med Chem

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