Literature DB >> 20350806

Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta.

Nicole Höttecke1, Miriam Liebeck, Karlheinz Baumann, Robert Schubenel, Edith Winkler, Harald Steiner, Boris Schmidt.   

Abstract

CK1 and gamma-secretase are interesting targets for therapeutic intervention in the treatment of cancer and Alzheimer's disease. The CK1 inhibitor IC261 was reported to inhibit gamma-secretase activity. The question is: Does CK1 inhibition directly influence gamma-secretase activity? Therefore we analyzed the SAR of 15 analogues and their impact on gamma-secretase activity. The most active compounds were investigated on CK1delta activity. These findings exclude a direct influence of CK1delta on gamma-secretase, because any change in the substitution pattern of IC261 diminished CK1 inhibition, whereas gamma-secretase inhibition is still exerted by several analogues. 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20350806     DOI： 10.1016/j.bmcl.2010.02.110

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


  5 in total

Review 1.  The CK1 Family: Contribution to Cellular Stress Response and Its Role in Carcinogenesis.

Authors:  Uwe Knippschild; Marc Krüger; Julia Richter; Pengfei Xu; Balbina García-Reyes; Christian Peifer; Jakob Halekotte; Vasiliy Bakulev; Joachim Bischof
Journal:  Front Oncol       Date:  2014-05-19       Impact factor: 6.244

2.  A Rationale for Drug Design Provided by Co-Crystal Structure of IC261 in Complex with Tubulin.

Authors:  Jinghong Xian; Faqian Bu; Yuxi Wang; Fangyi Long; Zhixiong Zhang; Chengyong Wu; Yiran Tao; Ting Wang; Guan Wang
Journal:  Molecules       Date:  2021-02-10       Impact factor: 4.411

3.  Evaluation of Virtual Screening Strategies for the Identification of γ-Secretase Inhibitors and Modulators.

Authors:  Alicia Ioppolo; Melissa Eccles; David Groth; Giuseppe Verdile; Mark Agostino
Journal:  Molecules       Date:  2021-12-28       Impact factor: 4.411

4.  Synthesis and biological activity evaluation of 3-(hetero) arylideneindolin-2-ones as potential c-Src inhibitors.

Authors:  Salvatore Princiotto; Loana Musso; Fabrizio Manetti; Valentina Marcellini; Giovanni Maga; Emmanuele Crespan; Cecilia Perini; Nadia Zaffaroni; Giovanni Luca Beretta; Sabrina Dallavalle
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

5.  Microtubules depolymerization caused by the CK1 inhibitor IC261 may be not mediated by CK1 blockage.

Authors:  Martin Stöter; Marc Krüger; George Banting; Doris Henne-Bruns; Uwe Knippschild
Journal:  PLoS One       Date:  2014-06-17       Impact factor: 3.240
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.