Linear scaffolds for multivalent targeting of melanocortin receptors
Author:
Affiliation:
1. Department of Chemistry and Biochemistry
2. University of Arizona
3. Tucson
4. USA
5. Department of Physiology
6. The Bio5 Institute
Abstract
Short, efficient syntheses of multivalent molecules targeted to the human melanocortin 4 receptor based on ethylene glycol, glycerol, and d-mannitol are described.
Funder
National Cancer Institute
Publisher
Royal Society of Chemistry (RSC)
Subject
Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2015/OB/C5OB01779C
Reference38 articles.
1. Synthetic Multivalent Molecules–Concepts and Biomedical Applications, ed. S. K. Choi, Wiley Interscience, 2004, p. 1
2. Synthesis and Receptor Binding Analysis of Thirteen Oligomeric α-MSH Analogs
3. Increasing Burden of Melanoma in the United States
4. Melanotropin receptors demonstrated in situ in human melanoma.
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1. Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors;Journal of Medicinal Chemistry;2018-04-18
2. Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016;Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease;2017-10
3. A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NH2 versus the Bivalent Agonist Ac-His-DPhe-Arg-Trp-PEDG20-His-DPhe-Arg-Trp-NH2: A Bivalent Advantage;ACS Chemical Neuroscience;2017-02-16
4. An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers;Journal of Medicinal Chemistry;2016-03-29
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