Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure–activity relationships and insurmountable antagonism

Releasing Hormone ◽

Structure Activity Relationships ◽

Structure Activity ◽

Antagonist Binding ◽

Gonadotropin Releasing Hormone Receptor ◽

Kinetics Of

Structure–activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2005.05.038 ◽

2005 ◽

Vol 15 (16) ◽

pp. 3685-3690 ◽

Cited By ~ 9

Author(s):

Zhiqiang Guo ◽

Dongpei Wu ◽

Yun-Fei Zhu ◽

Fabio C. Tucci ◽

Collin F. Regan ◽

...

Keyword(s):

Hormone Receptor ◽

Receptor Antagonists ◽

Releasing Hormone ◽

Structure Activity Relationships ◽

Structure Activity ◽

Synthesis and Structure−Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists

Journal of Medicinal Chemistry ◽

10.1021/jm030472z ◽

2004 ◽

Vol 47 (5) ◽

pp. 1259-1271 ◽

Cited By ~ 36

Author(s):

Zhiqiang Guo ◽

Yun-Fei Zhu ◽

Timothy D. Gross ◽

Fabio C. Tucci ◽

Yinghong Gao ◽

...

Keyword(s):

Hormone Receptor ◽

Receptor Antagonists ◽

Releasing Hormone ◽

Structure Activity Relationships ◽

Structure Activity ◽

Structure-Activity Relations of Successful Pharmacologic Chaperones for Rescue of Naturally Occurring and Manufactured Mutants of the Gonadotropin-Releasing Hormone Receptor

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.102.048454 ◽

2003 ◽

Vol 305 (2) ◽

pp. 608-614 ◽

Cited By ~ 94

Author(s):

Jo Ann Janovick ◽

Mark Goulet ◽

Eugene Bush ◽

Jonathan Greer ◽

David G. Wettlaufer ◽

...

Keyword(s):

Hormone Receptor ◽

Releasing Hormone ◽

Naturally Occurring ◽

Structure Activity ◽

Structure Activity Relations ◽

Determination of the Binding Mode of Thienopyrimidinedione Antagonists to the Human Gonadotropin Releasing Hormone Receptor Using Structure−Activity Relationships, Site-Directed Mutagenesis, and Homology Modeling

Journal of Medicinal Chemistry ◽

10.1021/jm060580w ◽

2006 ◽

Vol 49 (21) ◽

pp. 6170-6176 ◽

Cited By ~ 4

Author(s):

Stephen F. Betz ◽

Francisco M. Lio ◽

Yinghong Gao ◽

Greg J. Reinhart ◽

Zhiqiang Guo ◽

...

Keyword(s):

Homology Modeling ◽

Hormone Receptor ◽

Binding Mode ◽

Site Directed Mutagenesis ◽

Directed Mutagenesis ◽

Releasing Hormone ◽

Structure Activity ◽

Residues within Transmembrane Helices 2 and 5 of the Human Gonadotropin-Releasing Hormone Receptor Contribute to Agonist and Antagonist Binding

Molecular Endocrinology ◽

10.1210/mend.14.7.0483 ◽

2000 ◽

Vol 14 (7) ◽

pp. 1099-1115 ◽

Cited By ~ 27

Author(s):

Silke H. Hoffmann ◽

Ton ter Laak ◽

Ronald Kühne ◽

Helmut Reiländer ◽

Thomas Beckers

Keyword(s):

Hormone Receptor ◽

Transmembrane Helices ◽

Releasing Hormone ◽

Agonist And Antagonist ◽

Antagonist Binding ◽

Impact of Aromatic Residues within Transmembrane Helix 6 of the Human Gonadotropin-Releasing Hormone Receptor upon Agonist and Antagonist Binding†

Biochemistry ◽

10.1021/bi0113162 ◽

2002 ◽

Vol 41 (4) ◽

pp. 1129-1136 ◽

Cited By ~ 33

Author(s):

Sascha Hövelmann ◽

Silke H. Hoffmann ◽

Ronald Kühne ◽

Ton ter Laak ◽

Helmut Reiländer ◽

...

Keyword(s):

Hormone Receptor ◽

Transmembrane Helix ◽

Aromatic Residues ◽

Releasing Hormone ◽

Agonist And Antagonist ◽

Antagonist Binding ◽

A Locus of the Gonadotropin-releasing Hormone Receptor That Differentiates Agonist and Antagonist Binding Sites

Journal of Biological Chemistry ◽

10.1074/jbc.270.32.18853 ◽

1995 ◽

Vol 270 (32) ◽

pp. 18853-18857 ◽

Cited By ~ 76

Author(s):

Wei Zhou ◽

Vladimir Rodic ◽

Smiljka Kitanovic ◽

Colleen A. Flanagan ◽

Ling Chi ◽

...

Keyword(s):

Binding Sites ◽

Hormone Receptor ◽

Releasing Hormone ◽

Agonist And Antagonist ◽

Antagonist Binding ◽

Faculty Opinions recommendation of Suppression of serum luteinizing hormone in postmenopausal women by an orally administered nonpeptide antagonist of the gonadotropin-releasing hormone receptor (NBI-42902).

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1069755.522680 ◽

2007 ◽

Author(s):

Fernando Reis

Keyword(s):

Luteinizing Hormone ◽

Postmenopausal Women ◽

Hormone Receptor ◽

Releasing Hormone ◽

Serum Luteinizing Hormone ◽

Androgen Receptor Positively Regulates Gonadotropin-releasing Hormone Receptor in Pituitary Gonadotropes

Molecular and Cellular Endocrinology ◽

10.1016/j.mce.2021.111286 ◽

2021 ◽

pp. 111286

Author(s):

Genevieve E. Ryan ◽

Stephanie C. Bohaczuk ◽

Jessica Cassin ◽

Emily A. Witham ◽

Shadi Shojaei ◽

...

Keyword(s):

Androgen Receptor ◽

Hormone Receptor ◽

Releasing Hormone ◽

Proper receptor signalling in a mutant catfish gonadotropin-releasing hormone receptor lacking the highly conserved Asp90 residue

FEBS Letters ◽

10.1016/s0014-5793(01)02647-3 ◽

2001 ◽

Vol 501 (2-3) ◽

pp. 131-134 ◽

Cited By ~ 6

Author(s):

Marion Blomenröhr ◽

Ronald Kühne ◽

Eveline Hund ◽

Rob Leurs ◽

Jan Bogerd ◽

...

Keyword(s):

Hormone Receptor ◽

Releasing Hormone ◽

Receptor Signalling ◽