Literature DB >> 24502334

Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).

Benjamin P Fauber1, Steven Magnuson.   

Abstract

As the biology surrounding the nuclear receptor retinoic acid receptor-related orphan receptor-gamma (RORγ or RORc) continues to evolve, significant effort has been invested in discovering modulators of this potentially important target for the treatment of metabolic and immunological diseases. Several major pharmaceutical and biotechnology companies have disclosed RORc inhibitors or partnered with other players in the field. In this perspective, we discuss both the biology and the underlying structural biology of RORc, and summarize the RORc modulators disclosed in the scientific and patent literature.

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Year:  2014        PMID： 24502334     DOI： 10.1021/jm401901d

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


  38 in total

1.  RORc Modulators for the Treatment of Autoimmune Diseases.

Authors:  Ahmed F Abdel-Magid
Journal:  ACS Med Chem Lett       Date:  2015-08-14       Impact factor: 4.345

2.  SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious RORγ Inhibitor.

Authors:  Kazuyuki Hirata; Masayuki Kotoku; Noriyoshi Seki; Takaki Maeba; Katsuya Maeda; Shintaro Hirashima; Takayuki Sakai; Shingo Obika; Akimi Hori; Yasunori Hase; Takayuki Yamaguchi; Yoshiaki Katsuda; Takahiro Hata; Naoki Miyagawa; Kojo Arita; Yukihiro Nomura; Kota Asahina; Yusuke Aratsu; Masafumi Kamada; Tsuyoshi Adachi; Masato Noguchi; Satoki Doi; Paul Crowe; Erin Bradley; Ruo Steensma; Haiyan Tao; Morgan Fenn; Robert Babine; Xiaolin Li; Scott Thacher; Hiromasa Hashimoto; Makoto Shiozaki
Journal:  ACS Med Chem Lett       Date:  2015-11-04       Impact factor: 4.345

3.  Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.

Authors:  Hongjun Zhang; Blair T Lapointe; Neville Anthony; Rita Azevedo; Jos Cals; Craig C Correll; Matthew Daniels; Sujal Deshmukh; Hans van Eenenaam; Heidi Ferguson; Laxminarayan G Hegde; Willem Jan Karstens; John Maclean; J Richard Miller; Lily Y Moy; Vladimir Simov; Sunil Nagpal; Arthur Oubrie; Rachel L Palte; Gopal Parthasarathy; Nunzio Sciammetta; Mario van der Stelt; Janice D Woodhouse; B Wesley Trotter; Kenneth Barr
Journal:  ACS Med Chem Lett       Date:  2020-01-09       Impact factor: 4.345

4.  ROR(GMMA)T Modulating Activity for the Treatment of Cancers.

Authors:  Robert B Kargbo
Journal:  ACS Med Chem Lett       Date:  2018-05-22       Impact factor: 4.345

5.  Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

Authors:  Olivier René; Benjamin P Fauber; Gladys de Leon Boenig; Brenda Burton; Céline Eidenschenk; Christine Everett; Alberto Gobbi; Sarah G Hymowitz; Adam R Johnson; James R Kiefer; Marya Liimatta; Peter Lockey; Maxine Norman; Wenjun Ouyang; Heidi A Wallweber; Harvey Wong
Journal:  ACS Med Chem Lett       Date:  2014-12-04       Impact factor: 4.345

6.  Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

Authors:  James J-W Duan; Zhonghui Lu; Bin Jiang; Sylwia Stachura; Carolyn A Weigelt; John S Sack; Javed Khan; Max Ruzanov; Michael A Galella; Dauh-Rurng Wu; Melissa Yarde; Ding-Ren Shen; David J Shuster; Virna Borowski; Jenny H Xie; Lisa Zhang; Sridhar Vanteru; Arun Kumar Gupta; Arvind Mathur; Qihong Zhao; William Foster; Luisa M Salter-Cid; Percy H Carter; T G Murali Dhar
Journal:  ACS Med Chem Lett       Date:  2019-02-26       Impact factor: 4.345

7.  N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor γ (RORγ) Agonists.

Authors:  Christelle Doebelin; Rémi Patouret; Ruben D Garcia-Ordonez; Mi Ra Chang; Venkatasubramanian Dharmarajan; Dana S Kuruvilla; Scott J Novick; Li Lin; Michael D Cameron; Patrick R Griffin; Theodore M Kamenecka
Journal:  ChemMedChem       Date:  2016-11-23       Impact factor: 3.466

8.  Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.

Authors:  Robert J Cherney; Lyndon A M Cornelius; Anurag Srivastava; Carolyn A Weigelt; David Marcoux; James J-W Duan; Qing Shi; Douglas G Batt; Qingjie Liu; Shiuhang Yip; Dauh-Rurng Wu; Max Ruzanov; John Sack; Javed Khan; Jinhong Wang; Melissa Yarde; Mary Ellen Cvijic; Arvind Mathur; Sha Li; David Shuster; Purnima Khandelwal; Virna Borowski; Jenny Xie; Mary Obermeier; Aberra Fura; Kevin Stefanski; Georgia Cornelius; Joseph A Tino; John E Macor; Luisa Salter-Cid; Rex Denton; Qihong Zhao; Percy H Carter; T G Murali Dhar
Journal:  ACS Med Chem Lett       Date:  2020-03-31       Impact factor: 4.345

9.  JQ1, a bromodomain inhibitor, suppresses Th17 effectors by blocking p300-mediated acetylation of RORγt.

Authors:  Xiunan Wang; Yan Yang; Dandan Ren; Yuanyuan Xia; Wenguang He; Qingsi Wu; Junling Zhang; Miao Liu; Yinan Du; Cuiping Ren; Bin Li; Jijia Shen; Yuxia Zhang
Journal:  Br J Pharmacol       Date:  2020-03-23       Impact factor: 8.739

Review 10.  Endogenously produced nonclassical vitamin D hydroxy-metabolites act as "biased" agonists on VDR and inverse agonists on RORα and RORγ.

Authors:  Andrzej T Slominski; Tae-Kang Kim; Judith V Hobrath; Allen S W Oak; Edith K Y Tang; Elaine W Tieu; Wei Li; Robert C Tuckey; Anton M Jetten
Journal:  J Steroid Biochem Mol Biol       Date:  2016-09-28       Impact factor: 4.292
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