ArticleBioorganic & medicinal chemistry letters2006
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
Article in Bioorganic & medicinal chemistry letters, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed, 39 citations in OpenAlex.
- Strategies for converting turn-motif and cyclic peptides to small molecules for targeting protein-protein interactions.RSC chemical biology · 2024Review
- Demonstration of a Common DPheJournal of medicinal chemistry · 2022Article
- ACTH(6-9)PGP Peptide Protects SH-SY5Y Cells from HMolecules (Basel, Switzerland) · 2021Article
- Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists.Journal of medicinal chemistry · 2020Article
- Adventures in peptides and science with students! The joys of research.Biopolymers · 2013Article
- Design of peptide and peptidomimetic ligands with novel pharmacological activity profiles.Annual review of pharmacology and toxicology · 2013Review
- Design of novel melanocortin receptor ligands: multiple receptors, complex pharmacology, the challenge.European journal of pharmacology · 2011Review
- Approaches to the rational design of selective melanocortin receptor antagonists.Expert opinion on drug discovery · 2011Article
- Article
- Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.Journal of medicinal chemistry · 2009Article
- Beta-turn secondary structure and melanocortin ligands.Bioorganic & medicinal chemistry · 2009Article
- Melanotropins as drugs for the treatment of obesity and other feeding disorders: potential and problems.Current topics in medicinal chemistry · 2009Review
- Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.Journal of medicinal chemistry · 2008Article
- The first preparative solution phase synthesis of melanotan II.Beilstein journal of organic chemistry · 2008Article
- Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor.Current topics in medicinal chemistry · 2007Review
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
A new bicyclic template has been developed for the synthesis of peptide mimetics. Straightforward synthetic steps, starting from amino acids, allow the facile construction of a wide range of analogs. This system was designed to target the melanocortin receptors (MCRs), with functional group selection based on a known pharmacophore and guidance from molecular modeling to rationally identify positional and stereochemical isomers likely to be active. The functions of hMCRs are critical to myriad biological activities, including pigmentation, steroidogenesis, energy homeostasis, erectile activity, and inflammation. These G-protein-coupled receptors (GPCRs) are targets for drug discovery in a number of areas, including cancer, pain, and obesity therapeutics. All compounds from this series tested to date are antagonists which bind with high affinity. Importantly, many are highly selective for a particular MCR subtype, including some of the first completely hMC5R-selective antagonists reported.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.