Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors

Mark D Ericson; Anamika Singh; Srinivasa R Tala; Erica M Haslach; Marvin L Dirain; Jay W Schaub; Viktor Flores; Natalie Eick; Cody J Lensing; Katie T Freeman; Branden A Smeester; Danielle N Adank; Stacey L Wilber; Robert Speth; Carrie Haskell-Luevano

doi:10.1021/acs.jmedchem.8b00251

Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors

Mark D Ericson
, Anamika Singh
, Srinivasa R Tala
, Erica M Haslach
, Marvin L Dirain
, Jay W Schaub
, Viktor Flores
, Natalie Eick
, Cody J Lensing
, Katie T Freeman
, Branden A Smeester
, Danielle N Adank
, Stacey L Wilber
, Robert Speth
, Carrie Haskell-Luevano

Nova Southeastern University

Research output: Contribution to journal › Article › peer-review

6 Scopus citations

Abstract

β-Defensin 3 (BD3) was identified as a ligand for the melanocortin receptors (MCRs) in 2007, although the pharmacology activity of BD3 has not been clearly elucidated. Herein, it is demonstrated that human BD3 and mouse BD3 are full micromolar agonists at the MCRs. Furthermore, mouse β-defensin 1 (BD1) and human BD1 are also MCR micromolar agonists. This work identifies BD1 as an endogenous MCR ligand and clarifies the controversial role of BD3 as a micromolar agonist.

Original language	American English
Pages (from-to)	3738-3744
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	61
Issue number	8
DOIs	https://doi.org/10.1021/acs.jmedchem.8b00251
State	Published - Mar 26 2018

Keywords

Amino Acid Sequence
Animals
Cyclic AMP/metabolism
Humans
Ligands
Male
Mice, Inbred C57BL
Receptors, Melanocortin/agonists
beta-Defensins/metabolism

Disciplines

Medicine and Health Sciences
Pharmacy and Pharmaceutical Sciences

Access to Document

10.1021/acs.jmedchem.8b00251License: Unspecified

Human -Defensin 1 and -Defensin 3 (Mouse Ortholog mBD14) FunctiFinal published version, 667 KBLicense: Unspecified

https://doi.org/10.1021/acs.jmedchem.8b00251

Cite this

Ericson, M. D., Singh, A., Tala, S. R., Haslach, E. M., Dirain, M. L., Schaub, J. W., Flores, V., Eick, N., Lensing, C. J., Freeman, K. T., Smeester, B. A., Adank, D. N., Wilber, S. L., Speth, R., & Haskell-Luevano, C. (2018). Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. Journal of Medicinal Chemistry, 61(8), 3738-3744. https://doi.org/10.1021/acs.jmedchem.8b00251

Ericson, MD, Singh, A, Tala, SR, Haslach, EM, Dirain, ML, Schaub, JW, Flores, V, Eick, N, Lensing, CJ, Freeman, KT, Smeester, BA, Adank, DN, Wilber, SL, Speth, R & Haskell-Luevano, C 2018, 'Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors', Journal of Medicinal Chemistry, vol. 61, no. 8, pp. 3738-3744. https://doi.org/10.1021/acs.jmedchem.8b00251

@article{abac62db80f64cb195d60879148a6cce,

title = "Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors",

abstract = " β-Defensin 3 (BD3) was identified as a ligand for the melanocortin receptors (MCRs) in 2007, although the pharmacology activity of BD3 has not been clearly elucidated. Herein, it is demonstrated that human BD3 and mouse BD3 are full micromolar agonists at the MCRs. Furthermore, mouse β-defensin 1 (BD1) and human BD1 are also MCR micromolar agonists. This work identifies BD1 as an endogenous MCR ligand and clarifies the controversial role of BD3 as a micromolar agonist.",

keywords = "Amino Acid Sequence, Animals, Cyclic AMP/metabolism, Humans, Ligands, Male, Mice, Inbred C57BL, Receptors, Melanocortin/agonists, beta-Defensins/metabolism",

author = "Ericson, \{Mark D\} and Anamika Singh and Tala, \{Srinivasa R\} and Haslach, \{Erica M\} and Dirain, \{Marvin L\} and Schaub, \{Jay W\} and Viktor Flores and Natalie Eick and Lensing, \{Cody J\} and Freeman, \{Katie T\} and Smeester, \{Branden A\} and Adank, \{Danielle N\} and Wilber, \{Stacey L\} and Robert Speth and Carrie Haskell-Luevano",

year = "2018",

month = mar,

day = "26",

doi = "10.1021/acs.jmedchem.8b00251",

language = "American English",

volume = "61",

pages = "3738--3744",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "8",

}

TY - JOUR

T1 - Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors

AU - Ericson, Mark D

AU - Singh, Anamika

AU - Tala, Srinivasa R

AU - Haslach, Erica M

AU - Dirain, Marvin L

AU - Schaub, Jay W

AU - Flores, Viktor

AU - Eick, Natalie

AU - Lensing, Cody J

AU - Freeman, Katie T

AU - Smeester, Branden A

AU - Adank, Danielle N

AU - Wilber, Stacey L

AU - Speth, Robert

AU - Haskell-Luevano, Carrie

PY - 2018/3/26

Y1 - 2018/3/26

N2 - β-Defensin 3 (BD3) was identified as a ligand for the melanocortin receptors (MCRs) in 2007, although the pharmacology activity of BD3 has not been clearly elucidated. Herein, it is demonstrated that human BD3 and mouse BD3 are full micromolar agonists at the MCRs. Furthermore, mouse β-defensin 1 (BD1) and human BD1 are also MCR micromolar agonists. This work identifies BD1 as an endogenous MCR ligand and clarifies the controversial role of BD3 as a micromolar agonist.

AB - β-Defensin 3 (BD3) was identified as a ligand for the melanocortin receptors (MCRs) in 2007, although the pharmacology activity of BD3 has not been clearly elucidated. Herein, it is demonstrated that human BD3 and mouse BD3 are full micromolar agonists at the MCRs. Furthermore, mouse β-defensin 1 (BD1) and human BD1 are also MCR micromolar agonists. This work identifies BD1 as an endogenous MCR ligand and clarifies the controversial role of BD3 as a micromolar agonist.

KW - Amino Acid Sequence

KW - Animals

KW - Cyclic AMP/metabolism

KW - Humans

KW - Ligands

KW - Male

KW - Mice, Inbred C57BL

KW - Receptors, Melanocortin/agonists

KW - beta-Defensins/metabolism

UR - https://nsuworks.nova.edu/hpd_facarticles/93

U2 - 10.1021/acs.jmedchem.8b00251

DO - 10.1021/acs.jmedchem.8b00251

M3 - Article

C2 - 29578343

SN - 0022-2623

VL - 61

SP - 3738

EP - 3744

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 8

ER -

Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors

Abstract

Keywords

Disciplines

Access to Document

Other files and links

Fingerprint

Cite this