Literature DB >> 15026056

Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis.

Tao Guo1, Anton E P Adang, Roland E Dolle, Guizhen Dong, Dan Fitzpatrick, Peng Geng, Koc-Kan Ho, Steven G Kultgen, Ruiyan Liu, Edward McDonald, Brian F McGuinness, Kurt W Saionz, Kenneth J Valenzano, Nicole C R van Straten, Dan Xie, Maria L Webb.   

Abstract

High-throughput screening of two million compounds in 37 distinct encoded combinatorial libraries using FSH receptor transfected cells provided small molecule agonists such as 1 (EC(50)=3 microM) and 2 (EC(50)=3.9 microM), based on which a focused combinatorial library with a total of 31372 compounds was designed, synthesized, and screened to reveal 72 novel biaryl FSH receptor agonists such as 8a-c as well as a unique combinatorial SAR.

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Year:  2004        PMID: 15026056     DOI: 10.1016/j.bmcl.2004.01.042

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  10 in total

1.  A negative allosteric modulator demonstrates biased antagonism of the follicle stimulating hormone receptor.

Authors:  James A Dias; Béatrice Bonnet; Barbara A Weaver; Julie Watts; Kerri Kluetzman; Richard M Thomas; Sonia Poli; Vincent Mutel; Brice Campo
Journal:  Mol Cell Endocrinol       Date:  2010-12-22       Impact factor: 4.102

Review 2.  Molecular pharmacology of gonadotropins.

Authors:  Robert K Campbell
Journal:  Endocrine       Date:  2005-04       Impact factor: 3.633

Review 3.  Novel pathways in gonadotropin receptor signaling and biased agonism.

Authors:  Alfredo Ulloa-Aguirre; Pascale Crépieux; Anne Poupon; Marie-Christine Maurel; Eric Reiter
Journal:  Rev Endocr Metab Disord       Date:  2011-12       Impact factor: 6.514

4.  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

5.  Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice.

Authors:  Susanne Neumann; Wenwei Huang; Steve Titus; Gerd Krause; Gunnar Kleinau; Anna Teresa Alberobello; Wei Zheng; Noel T Southall; James Inglese; Christopher P Austin; Francesco S Celi; Oksana Gavrilova; Craig J Thomas; Bruce M Raaka; Marvin C Gershengorn
Journal:  Proc Natl Acad Sci U S A       Date:  2009-07-10       Impact factor: 11.205

6.  Human TSH receptor ligands as pharmacological probes with potential clinical application.

Authors:  Susanne Neumann; Bruce M Raaka; Marvin C Gershengorn
Journal:  Expert Rev Endocrinol Metab       Date:  2009-11-01

Review 7.  Solid-phase and microwave-assisted syntheses of 2,5-diketopiperazines: small molecules with great potential.

Authors:  Jennifer C O'Neill; Helen E Blackwell
Journal:  Comb Chem High Throughput Screen       Date:  2007-12       Impact factor: 1.339

Review 8.  Small Molecule Follicle-Stimulating Hormone Receptor Agonists and Antagonists.

Authors:  Ross C Anderson; Claire L Newton; Robert P Millar
Journal:  Front Endocrinol (Lausanne)       Date:  2019-01-23       Impact factor: 5.555

Review 9.  Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold.

Authors:  Joanna Bojarska; Adam Mieczkowski; Zyta M Ziora; Mariusz Skwarczynski; Istvan Toth; Ahmed O Shalash; Keykavous Parang; Shaima A El-Mowafi; Eman H M Mohammed; Sherif Elnagdy; Maha AlKhazindar; Wojciech M Wolf
Journal:  Biomolecules       Date:  2021-10-14

Review 10.  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

  10 in total

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