Literature DB >> 30010338

Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) Inhibitors: Hits and Misses.

Vrajesh B Pandya1, Sanjay Kumar1, Rajiv Sharma1, Ranjit C Desai1.   

Abstract

The nuclear receptor retinoic acid receptor-related orphan receptor gamma (RORγ or RORc) is a key transcription factor for the production of pro-inflammatory cytokines implicated in the pathogenesis of autoimmune diseases. Recently, small molecule inhibitors of RORc drew the enormous attention of the research community worldwide as a possible therapy for autoimmune diseases, mediated by the IL-17 cytokine. With the clinical proof-of-concept inferred from a small molecule inhibitor VTP-43742 for psoriasis and recent inflow of several RORc inhibitors into the clinic for therapeutic interventions in autoimmune diseases, this field continues to evolve. This review briefly summarizes the RORc inhibitors disclosed in the literature and discusses the progress made by these inhibitors in combating autoimmune diseases.

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Year:  2018        PMID： 30010338     DOI： 10.1021/acs.jmedchem.8b00588

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


  23 in total

1.  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

2.  Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.

Authors:  Stefan von Berg; Yafeng Xue; Mia Collins; Antonio Llinas; Roine I Olsson; Torbjörn Halvarsson; Maria Lindskog; Jesper Malmberg; Johan Jirholt; Nina Krutrök; Marie Ramnegård; Marie Brännström; Anders Lundqvist; Matti Lepistö; Anna Aagaard; Jane McPheat; Eva L Hansson; Rongfeng Chen; Yao Xiong; Thomas G Hansson; Frank Narjes
Journal:  ACS Med Chem Lett       Date:  2019-05-29       Impact factor: 4.345

3.  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

4.  Delineation of the molecular determinants of the unique allosteric binding site of the orphan nuclear receptor RORγt.

Authors:  Iris A Leijten-van de Gevel; Luc Brunsveld
Journal:  J Biol Chem       Date:  2020-05-20       Impact factor: 5.157

5.  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

6.  Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists.

Authors:  Ryota Nakajima; Hiroyuki Oono; Sakae Sugiyama; Yohei Matsueda; Tomohide Ida; Shinji Kakuda; Jun Hirata; Atsushi Baba; Akito Makino; Ryo Matsuyama; Ryan D White; Ryan Ρ Wurz; Youngsook Shin; Xiaoshan Min; Angel Guzman-Perez; Zhulun Wang; Antony Symons; Sanjay K Singh; Srinivasa Reddy Mothe; Sergei Belyakov; Anjan Chakrabarti; Satoshi Shuto
Journal:  ACS Med Chem Lett       Date:  2020-02-27       Impact factor: 4.345

7.  VPR-254: an inhibitor of ROR-gamma T with potential utility for the treatment of inflammatory bowel disease.

Authors:  Leo R Fitzpatrick; Jeff Small; Robert O'Connell; George Talbott; Gordon Alton; Jim Zapf
Journal:  Inflammopharmacology       Date:  2019-09-23       Impact factor: 4.473

8.  Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357.

Authors:  Christian Harcken; Johanna Csengery; Michael Turner; Lifen Wu; Shuang Liang; Robert Sibley; Steven Brunette; Mark Labadia; Kathleen Hoyt; Anita Wayne; Thomas Wieckowski; Gregg Davis; Mark Panzenbeck; Donald Souza; Stanley Kugler; Donna Terenzio; Delphine Collin; Dustin Smith; Ryan M Fryer; Yin-Chao Tseng; Jörg P Hehn; Kim Fletcher; Robert O Hughes
Journal:  ACS Med Chem Lett       Date:  2021-01-05       Impact factor: 4.345

9.  Structure-Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor γt.

Authors:  Femke A Meijer; Annet O W M Saris; Richard G Doveston; Guido J M Oerlemans; Rens M J M de Vries; Bente A Somsen; Anke Unger; Bert Klebl; Christian Ottmann; Peter J Cossar; Luc Brunsveld
Journal:  J Med Chem       Date:  2021-05-19       Impact factor: 7.446

10.  Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.

Authors:  Qingjie Liu; Hai-Yun Xiao; Douglas G Batt; Zili Xiao; Yeheng Zhu; Michael G Yang; Ning Li; Shiuhang Yip; Peng Li; Dawn Sun; Dauh-Rurng Wu; Max Ruzanov; John S Sack; Carolyn A Weigelt; Jinhong Wang; Sha Li; David J Shuster; Jenny H Xie; Yunling Song; Tara Sherry; Mary T Obermeier; Aberra Fura; Kevin Stefanski; Georgia Cornelius; Silvi Chacko; Purnima Khandelwal; Shailesh Dudhgaonkar; Anjuman Rudra; Jignesh Nagar; Venkata Murali; Arun Govindarajan; Rex Denton; Qihong Zhao; Nicholas A Meanwell; Robert Borzilleri; T G Murali Dhar
Journal:  ACS Med Chem Lett       Date:  2021-04-30       Impact factor: 4.345
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