Literature DB >> 19902448

Synthesis and pharmacological evaluation of dimeric follicle-stimulating hormone receptor antagonists.

Kimberly M Bonger1, Sascha Hoogendoorn, Chris J van Koppen, Cornelis M Timmers, Herman S Overkleeft, Gijsbert A van der Marel.   

Abstract

A series of homo- and heterodimeric compounds encompassing the follicle-stimulating hormone receptor (FSHR) antagonist (R)-1 and its inactive conformer (S)-1 connected through ethylene glycol spacers of various lengths is described. Evaluation of these compounds reveals that dimeric compounds, with a spacer of sufficient length, bearing two active copies of the antagonist are more potent relative to dimeric compounds in which one of the active pharmacophores is replaced by an inactive conformer. Interestingly, the opposite trend is observed if a short spacer is used, indicating that these compounds may be valuable tools to study FSHR dimerization in greater detail.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19902448     DOI： 10.1002/cmdc.200900344

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  6 in total

1.  Development of Selective LH Receptor Agonists by Heterodimerization with a FSH Receptor Antagonist.

Authors:  Kimberly M Bonger; Sascha Hoogendoorn; Chris J van Koppen; C Marco Timmers; Gijsbert A van der Marel; Herman S Overkleeft
Journal:  ACS Med Chem Lett       Date:  2010-11-08       Impact factor: 4.345

2.  Biological Significance of GPCR Heteromerization in the Neuro-Endocrine System.

Authors:  Maud Kamal; Ralf Jockers
Journal:  Front Endocrinol (Lausanne)       Date:  2011-02-01       Impact factor: 5.555

3.  Synthetic Development of New 3-(4-Arylmethylamino)butyl-5-arylidene-rhodanines under Microwave Irradiation and Their Effects on Tumor Cell Lines and against Protein Kinases.

Authors:  Camille Déliko Dago; Christelle N'ta Ambeu; Wacothon-Karime Coulibaly; Yves-Alain Békro; Janat Mamyrbékova; Audrey Defontaine; Blandine Baratte; Stéphane Bach; Sandrine Ruchaud; Rémy Le Guével; Myriam Ravache; Anne Corlu; Jean-Pierre Bazureau
Journal:  Molecules       Date:  2015-07-08       Impact factor: 4.411

4.  Discovery and Preclinical Development of Orally Active Small Molecules that Exhibit Highly Selective Follicle Stimulating Hormone Receptor Agonism.

Authors:  Selva Nataraja; Henry Yu; Joie Guner; Stephen Palmer
Journal:  Front Pharmacol       Date:  2021-01-14       Impact factor: 5.810

Review 5.  Discovery and Development of Small Molecule Allosteric Modulators of Glycoprotein Hormone Receptors.

Authors:  Selvaraj G Nataraja; Henry N Yu; Stephen S Palmer
Journal:  Front Endocrinol (Lausanne)       Date:  2015-09-14       Impact factor: 5.555

6.  Aminoluciferins extend firefly luciferase bioluminescence into the near-infrared and can be preferred substrates over D-luciferin.

Authors:  David M Mofford; Gadarla Randheer Reddy; Stephen C Miller
Journal:  J Am Chem Soc       Date:  2014-09-11       Impact factor: 15.419
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.