Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors

Niyada Hin; Jesse Alt; Sarah C. Zimmermann; Greg Delahanty; Dana V. Ferraris; Camilo Rojas; Fengxian Li; Qin Liu; Xinzhong Dong; Barbara S. Slusher; Takashi Tsukamoto

doi:10.1016/j.bmc.2014.09.025

Peptidomimetics of Arg-Phe-NH₂ as small molecule agonists of Mas-related gene C (MrgC) receptors

Niyada Hin, Jesse Alt, Sarah C. Zimmermann, Greg Delahanty, Dana V. Ferraris, Camilo Rojas, Fengxian Li, Qin Liu, Xinzhong Dong, Barbara S. Slusher, Takashi Tsukamoto

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5 Scopus citations

Abstract

A series of Arg-Phe-NH₂ peptidomimetics containing an Arg mimetic were synthesized and tested as agonists of human MrgX1, rat MrgC, and mouse MrgC11 receptors. As predicted from the previously established species specificity, these peptidomimetics were found to be devoid of MrgX1 agonist activity. In contrast, these compounds acted as agonists of MrgC and/or MrgC11 with varying degrees of potency. These new peptidomimetics should complement the existing small molecule human MrgX1 agonists and enhance our ability to assess the therapeutic utility of targeting Mrg receptors in rodent models.

Original language	English
Pages (from-to)	5831-5837
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry
Volume	22
Issue number	21
DOIs	https://doi.org/10.1016/j.bmc.2014.09.025
State	Published - Nov 1 2014

Keywords

Agonist
Arginine mimetic
Mas-related gene
Mrg) receptors
Peptidomimetic

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10.1016/j.bmc.2014.09.025

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title = "Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors",

abstract = "A series of Arg-Phe-NH2 peptidomimetics containing an Arg mimetic were synthesized and tested as agonists of human MrgX1, rat MrgC, and mouse MrgC11 receptors. As predicted from the previously established species specificity, these peptidomimetics were found to be devoid of MrgX1 agonist activity. In contrast, these compounds acted as agonists of MrgC and/or MrgC11 with varying degrees of potency. These new peptidomimetics should complement the existing small molecule human MrgX1 agonists and enhance our ability to assess the therapeutic utility of targeting Mrg receptors in rodent models.",

keywords = "Agonist, Arginine mimetic, Mas-related gene, Mrg) receptors, Peptidomimetic",

author = "Niyada Hin and Jesse Alt and Zimmermann, {Sarah C.} and Greg Delahanty and Ferraris, {Dana V.} and Camilo Rojas and Fengxian Li and Qin Liu and Xinzhong Dong and Slusher, {Barbara S.} and Takashi Tsukamoto",

note = "Funding Information: This work was in part supported by National Institutes of Health ( 2R01NS054791 to X.D.) and a visiting scholar fellowship (to F.L.) from the Department of Anesthesiology, Zhujiang Hospital, Southern Medical University (Guangzhou, China). Publisher Copyright: {\textcopyright} 2014 Elsevier Ltd. All rights reserved.",

year = "2014",

month = nov,

day = "1",

doi = "10.1016/j.bmc.2014.09.025",

language = "English",

volume = "22",

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journal = "Bioorganic and Medicinal Chemistry",

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AU - Hin, Niyada

AU - Alt, Jesse

AU - Zimmermann, Sarah C.

AU - Delahanty, Greg

AU - Ferraris, Dana V.

AU - Rojas, Camilo

AU - Li, Fengxian

AU - Liu, Qin

AU - Dong, Xinzhong

AU - Slusher, Barbara S.

AU - Tsukamoto, Takashi

N1 - Funding Information: This work was in part supported by National Institutes of Health ( 2R01NS054791 to X.D.) and a visiting scholar fellowship (to F.L.) from the Department of Anesthesiology, Zhujiang Hospital, Southern Medical University (Guangzhou, China). Publisher Copyright: © 2014 Elsevier Ltd. All rights reserved.

PY - 2014/11/1

Y1 - 2014/11/1

N2 - A series of Arg-Phe-NH2 peptidomimetics containing an Arg mimetic were synthesized and tested as agonists of human MrgX1, rat MrgC, and mouse MrgC11 receptors. As predicted from the previously established species specificity, these peptidomimetics were found to be devoid of MrgX1 agonist activity. In contrast, these compounds acted as agonists of MrgC and/or MrgC11 with varying degrees of potency. These new peptidomimetics should complement the existing small molecule human MrgX1 agonists and enhance our ability to assess the therapeutic utility of targeting Mrg receptors in rodent models.

AB - A series of Arg-Phe-NH2 peptidomimetics containing an Arg mimetic were synthesized and tested as agonists of human MrgX1, rat MrgC, and mouse MrgC11 receptors. As predicted from the previously established species specificity, these peptidomimetics were found to be devoid of MrgX1 agonist activity. In contrast, these compounds acted as agonists of MrgC and/or MrgC11 with varying degrees of potency. These new peptidomimetics should complement the existing small molecule human MrgX1 agonists and enhance our ability to assess the therapeutic utility of targeting Mrg receptors in rodent models.

KW - Agonist

KW - Arginine mimetic

KW - Mas-related gene

KW - Mrg) receptors

KW - Peptidomimetic

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DO - 10.1016/j.bmc.2014.09.025

M3 - Article

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AN - SCOPUS:84908428881

SN - 0968-0896

VL - 22

SP - 5831

EP - 5837

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 21

ER -

Peptidomimetics of Arg-Phe-NH₂ as small molecule agonists of Mas-related gene C (MrgC) receptors

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Keywords

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