Synthetic ACTH-Like Peptide GKVLKKRR, Corresponding to the Fragment 81–88 of Human Pro-Interleukin-1α, Acts as an Antagonist of ACTH Receptor

Navolotskaya, E. V.; Kovalitskaya, Yulia A.; Садовников, В. Б.; Zolotarev, Yu. A.; Kolobov, A. A.; Yurovsky, Vladimir V.; Липкин, В. М.

doi:10.1007/s10989-007-9091-2

Cited by 4 publications

(2 citation statements)

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“…Therefore, they concluded that the tetrapeptide KKRR (ACTH 15-18 ) is an antagonist for the ACTH receptor. The same research group has also found in a separate study that a synthetic peptide GKVLKKRR corresponding to the fragments 81 – 88 of human pro-IL-1α protein acts as an antagonist at the MC2R [32]. They chose this peptide because it has 80% sequence similarity with fragments 10 – 18 of ACTH.…”

Section: Human Mc2r Antagonistsmentioning

confidence: 99%

Approaches to the rational design of selective melanocortin receptor antagonists

Hruby¹,

Cai²,

Nyberg³

et al. 2011

Expert Opinion on Drug Discovery

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Introduction When establishing the physiological roles of specific receptors in normal and disease states, it is critical to have selective antagonist ligands for each receptor in a receptor system with several subtypes. The melanocortin receptors have five subtypes referred to as the melanocortin 1 receptor, melanocortin 2 receptor, melanocortin 3 receptor, melanocortin 4 receptor and melanocortin 5 receptor, and they are of critical importance for many aspects of human health and disease. Areas covered This article reviews the current efforts to design selective antagonistic ligands for the five human melanocortin receptors summarizing the currently published orthosteric and allosteric antagonists for each of these receptors. Expert opinion Though there has been progress, there are still few drugs available that address the many significant biological activities and diseases that are associated with these receptors, which is possibly due to the lack of receptor selectivity that these designed ligands are currently showing. The authors believe that further studies into the antagonists’ 3D conformational and topographical properties in addition to future mutagenesis studies will provide greater insight into these ligands which could play a role in the treatment of various diseases in the future.

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Section: Human Mc2r Antagonistsmentioning

confidence: 99%

Approaches to the rational design of selective melanocortin receptor antagonists

Hruby¹,

Cai²,

Nyberg³

et al. 2011

Expert Opinion on Drug Discovery

View full text Add to dashboard Cite

show abstract

“…[113][114][115] It has been shown that these uniformly tritium labeled peptides completely retain their biological activity. 116,117 The theoretical analysis of hydrogen exchange in the CtxG1 polypeptide revealed some important HSCIE features regarding the influence of peptide chain mobility on the reactivity of amino acids (Figure 20; Table 16). It is well-known that HSCIE reactions in free amino acids have comparable rates.…”

Section: Hscie Reaction With Peptides and Proteinsmentioning

confidence: 99%