Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment?

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment? / Högberg, T.; Frimurer, T.M.; Sasmal, P.K.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 19, 01.10.2012, p. 6039-6047.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Högberg, T, Frimurer, TM & Sasmal, PK 2012, 'Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment?', Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 19, pp. 6039-6047. https://doi.org/10.1016/j.bmcl.2012.08.025

APA

Högberg, T., Frimurer, T. M., & Sasmal, P. K. (2012). Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment? Bioorganic & Medicinal Chemistry Letters, 22(19), 6039-6047. https://doi.org/10.1016/j.bmcl.2012.08.025

Vancouver

Högberg T, Frimurer TM, Sasmal PK. Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment? Bioorganic & Medicinal Chemistry Letters. 2012 Oct 1;22(19):6039-6047. https://doi.org/10.1016/j.bmcl.2012.08.025

Author

Högberg, T. ; Frimurer, T.M. ; Sasmal, P.K. / Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment?. In: Bioorganic & Medicinal Chemistry Letters. 2012 ; Vol. 22, No. 19. pp. 6039-6047.

Bibtex

@article{c06a02da2ecf4179b880df1758e75511,
title = "Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment?",
abstract = "Obesity is a global epidemic associated with multiple severe diseases. Several pharmacotherapies have been investigated including the melanin concentrating hormone (MCH) and its receptor 1. The development of MCHR1 antagonists are described with a specific perspective on different chemotypes investigated in efforts to overcome hERG liabilities while having orally active, potent and selective compounds with sufficient brain penetration. A chemometric comparison of ∼2000 diverse MCHR1 and ∼1000 diverse hERG ligands underline the structural similarities. A binding pocket analysis of a MCHR1 model and recent X-ray structures of GPCRs invoked in selectivity issues indicate a way to support future drug design.",
author = "T. H{\"o}gberg and T.M. Frimurer and P.K. Sasmal",
year = "2012",
month = oct,
day = "1",
doi = "10.1016/j.bmcl.2012.08.025",
language = "English",
volume = "22",
pages = "6039--6047",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "19",

}

RIS

TY - JOUR

T1 - Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment?

AU - Högberg, T.

AU - Frimurer, T.M.

AU - Sasmal, P.K.

PY - 2012/10/1

Y1 - 2012/10/1

N2 - Obesity is a global epidemic associated with multiple severe diseases. Several pharmacotherapies have been investigated including the melanin concentrating hormone (MCH) and its receptor 1. The development of MCHR1 antagonists are described with a specific perspective on different chemotypes investigated in efforts to overcome hERG liabilities while having orally active, potent and selective compounds with sufficient brain penetration. A chemometric comparison of ∼2000 diverse MCHR1 and ∼1000 diverse hERG ligands underline the structural similarities. A binding pocket analysis of a MCHR1 model and recent X-ray structures of GPCRs invoked in selectivity issues indicate a way to support future drug design.

AB - Obesity is a global epidemic associated with multiple severe diseases. Several pharmacotherapies have been investigated including the melanin concentrating hormone (MCH) and its receptor 1. The development of MCHR1 antagonists are described with a specific perspective on different chemotypes investigated in efforts to overcome hERG liabilities while having orally active, potent and selective compounds with sufficient brain penetration. A chemometric comparison of ∼2000 diverse MCHR1 and ∼1000 diverse hERG ligands underline the structural similarities. A binding pocket analysis of a MCHR1 model and recent X-ray structures of GPCRs invoked in selectivity issues indicate a way to support future drug design.

UR - http://www.scopus.com/inward/record.url?scp=84866384546&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2012.08.025

DO - 10.1016/j.bmcl.2012.08.025

M3 - Journal article

AN - SCOPUS:84866384546

VL - 22

SP - 6039

EP - 6047

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 19

ER -

ID: 47525846