Literature DB >> 16250633

A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.

Conrad W Hummel1, Andrew G Geiser, Henry U Bryant, Ilene R Cohen, Robert D Dally, Kin Chiu Fong, Scott A Frank, Ronald Hinklin, Scott A Jones, George Lewis, Denis J McCann, Daniel G Rudmann, Timothy A Shepherd, Hongqi Tian, Owen B Wallace, Minmin Wang, Yong Wang, Jeffrey A Dodge.   

Abstract

The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors alpha and beta (ERalpha and ERbeta, respectively) and is a potent uterine antagonist with minimal effects on the ovaries as determined by serum biomarkers and histologic evaluation.

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Year:  2005        PMID： 16250633     DOI： 10.1021/jm050723z

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  14 in total

1.  The naphthol selective estrogen receptor modulator (SERM), LY2066948, is oxidized to an o-quinone analogous to the naphthol equine estrogen, equilenin.

Authors:  Teshome B Gherezghiher; Bradley Michalsen; R Esala P Chandrasena; Zhihui Qin; Johann Sohn; Gregory R J Thatcher; Judy L Bolton
Journal:  Chem Biol Interact       Date:  2012-01-28       Impact factor: 5.192

2.  Proceedings from the Third National Institutes of Health International Congress on Advances in Uterine Leiomyoma Research: comprehensive review, conference summary and future recommendations.

Authors:  James H Segars; Estella C Parrott; Joan D Nagel; Xiaoxiao Catherine Guo; Xiaohua Gao; Linda S Birnbaum; Vivian W Pinn; Darlene Dixon
Journal:  Hum Reprod Update       Date:  2014-01-08       Impact factor: 15.610

3.  GLL398, an oral selective estrogen receptor degrader (SERD), blocks tumor growth in xenograft breast cancer models.

Authors:  Shanchun Guo; Changde Zhang; Madhusoodanan Mottamal; Ahamed Hossain; Jiawang Liu; Guangdi Wang
Journal:  Breast Cancer Res Treat       Date:  2020-02-06       Impact factor: 4.872

4.  Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.

Authors:  Timothy I Richardson; Christian A Clarke; Kuo-Long Yu; Ying K Yee; Thomas J Bleisch; Jose E Lopez; Scott A Jones; Norman E Hughes; Brian S Muehl; Charles W Lugar; Terry L Moore; Pamela K Shetler; Richard W Zink; John J Osborne; Chahrzad Montrose-Rafizadeh; Nita Patel; Andrew G Geiser; Rachelle J Sells Galvin; Jeffrey A Dodge
Journal:  ACS Med Chem Lett       Date:  2010-12-09       Impact factor: 4.345

5.  Diverse methyl sulfone-containing benzo[b]thiophene library via iodocyclization and palladium-catalyzed coupling.

Authors:  Chul-Hee Cho; Benjamin Neuenswander; Richard C Larock
Journal:  J Comb Chem       Date:  2010-03-08

6.  4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors.

Authors:  Patrick T Weiser; Ching-Yi Chang; Donald P McDonnell; Robert N Hanson
Journal:  Bioorg Med Chem       Date:  2013-11-08       Impact factor: 3.641

7.  Structural modulation of oxidative metabolism in design of improved benzothiophene selective estrogen receptor modulators.

Authors:  Zhihui Qin; Irida Kastrati; Rezene T Ashgodom; Daniel D Lantvit; Cassia R Overk; Yongsoo Choi; Richard B van Breemen; Judy L Bolton; Gregory R J Thatcher
Journal:  Drug Metab Dispos       Date:  2008-10-20       Impact factor: 3.922

8.  Identification of xenoestrogens in food additives by an integrated in silico and in vitro approach.

Authors:  Alessio Amadasi; Andrea Mozzarelli; Clara Meda; Adriana Maggi; Pietro Cozzini
Journal:  Chem Res Toxicol       Date:  2009-01       Impact factor: 3.739

9.  Uterine peroxidase-catalyzed formation of diquinone methides from the selective estrogen receptor modulators raloxifene and desmethylated arzoxifene.

Authors:  Hong Liu; Zhihui Qin; Gregory R J Thatcher; Judy L Bolton
Journal:  Chem Res Toxicol       Date:  2007-07-13       Impact factor: 3.739

10.  Mitigating the Adverse Effects of Polychlorinated Biphenyl Derivatives on Estrogenic Activity via Molecular Modification Techniques.

Authors:  Wei He; Wenhui Zhang; Zhenhua Chu; Yu Li
Journal:  Int J Environ Res Public Health       Date:  2021-05-08       Impact factor: 3.390
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