Literature DB >> 21106451

Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.

Vinay M Girijavallabhan1, Lei Chen, Chaoyang Dai, Robert J Feltz, Luke Firmansjah, Dansu Li, Seong Heon Kim, Joseph A Kozlowski, Brian J Lavey, Aneta Kosinski, John J Piwinski, Janeta Popovici-Muller, Razia Rizvi, Kristin E Rosner, Banderpalle B Shankar, Neng-Yang Shih, M Arshad Siddiqui, Ling Tong, Michael K C Wong, De-yi Yang, Liping Yang, Wensheng Yu, Guowei Zhou, Zhuyan Guo, Peter Orth, Vincent Madison, Hong Bian, Daniel Lundell, Xiaoda Niu, Himanshu Shah, Jing Sun, Shelby Umland.   

Abstract

Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors with good DMPK profiles. Published by Elsevier Ltd.

Entities:  

Mesh:

Substances:

Year:  2010        PMID: 21106451     DOI: 10.1016/j.bmcl.2010.10.081

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


  2 in total

1.  In Search of Selectivity in Inhibition of ADAM10.

Authors:  Kiran V Mahasenan; Derong Ding; Ming Gao; Trung T Nguyen; Mark A Suckow; Valerie A Schroeder; William R Wolter; Mayland Chang; Shahriar Mobashery
Journal:  ACS Med Chem Lett       Date:  2018-06-11       Impact factor: 4.345

Review 2.  Strategies to Target ADAM17 in Disease: From its Discovery to the iRhom Revolution.

Authors:  Matteo Calligaris; Doretta Cuffaro; Simone Bonelli; Donatella Pia Spanò; Armando Rossello; Elisa Nuti; Simone Dario Scilabra
Journal:  Molecules       Date:  2021-02-10       Impact factor: 4.411

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.