Literature DB >> 27766861

An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.

Apirat Chaikuad1, Julien Diharce2, Martin Schröder3, Alicia Foucourt4, Bertrand Leblond5, Anne-Sophie Casagrande5, Laurent Désiré5, Pascal Bonnet2, Stefan Knapp1,3, Thierry Besson4.   

Abstract

Methyl 9-anilinothiazolo[5,4-f]quinazoline-2-carbimidates 1 (EHT 5372) and 2 (EHT 1610) are strong inhibitors of DYRK's family kinases. The crystal structures of the complex revealed a noncanonical binding mode of compounds 1 and 2 in DYRK2, explaining the remarkable selectivity and potency of these inhibitors. The structural data and comparison presented here provide therefore a template for further improvement of this inhibitor class and for the development of novel inhibitors selectively targeting DYRK kinases.

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Year:  2016        PMID： 27766861     DOI： 10.1021/acs.jmedchem.6b01083

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


  14 in total

1.  DYRK1A regulates B cell acute lymphoblastic leukemia through phosphorylation of FOXO1 and STAT3.

Authors:  Rahul S Bhansali; Malini Rammohan; Paul Lee; Anouchka P Laurent; Qiang Wen; Praveen Suraneni; Bon Ham Yip; Yi-Chien Tsai; Silvia Jenni; Beat Bornhauser; Aurélie Siret; Corinne Fruit; Alexandra Pacheco-Benichou; Ethan Harris; Thierry Besson; Benjamin J Thompson; Young Ah Goo; Nobuko Hijiya; Maria Vilenchik; Shai Izraeli; Jean-Pierre Bourquin; Sébastien Malinge; John D Crispino
Journal:  J Clin Invest       Date:  2021-01-04       Impact factor: 14.808

2.  Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.

Authors:  Tiantian Wei; Jue Wang; Ruqi Liang; Wendong Chen; Yilan Chen; Mingzhe Ma; An He; Yifei Du; Wenjing Zhou; Zhiying Zhang; Xin Zeng; Chu Wang; Jin Lu; Xing Guo; Xiao-Wei Chen; Youjun Wang; Ruijun Tian; Junyu Xiao; Xiaoguang Lei
Journal:  Elife       Date:  2022-04-19       Impact factor: 8.713

3.  Development of Kinase Inhibitors via Metal-Catalyzed C⁻H Arylation of 8-Alkyl-thiazolo[5,4-f]-quinazolin-9-ones Designed by Fragment-Growing Studies.

Authors:  Florence Couly; Marine Harari; Carole Dubouilh-Benard; Laetitia Bailly; Emilie Petit; Julien Diharce; Pascal Bonnet; Laurent Meijer; Corinne Fruit; Thierry Besson
Journal:  Molecules       Date:  2018-08-29       Impact factor: 4.411

4.  Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design.

Authors:  Rosanna Meine; Walter Becker; Hannes Falke; Lutz Preu; Nadège Loaëc; Laurent Meijer; Conrad Kunick
Journal:  Molecules       Date:  2018-01-24       Impact factor: 4.411

5.  [b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors.

Authors:  Christian Lechner; Maren Flaßhoff; Hannes Falke; Lutz Preu; Nadége Loaëc; Laurent Meijer; Stefan Knapp; Apirat Chaikuad; Conrad Kunick
Journal:  Molecules       Date:  2019-11-13       Impact factor: 4.411

6.  DYRK1a mediates BAFF-induced noncanonical NF-κB activation to promote autoimmunity and B-cell leukemogenesis.

Authors:  Yanchuan Li; Xiaoping Xie; Zuliang Jie; Lele Zhu; Jin-Young Yang; Chun-Jung Ko; Tianxiao Gao; Antrix Jain; Sung Yun Jung; Natalia Baran; Marina Y Konopleva; Xuhong Cheng; Shao-Cong Sun
Journal:  Blood       Date:  2021-12-09       Impact factor: 22.113

7.  Sulfur-containing therapeutics in the treatment of Alzheimer's disease.

Authors:  Haizhou Zhu; Venkateshwara Dronamraju; Wei Xie; Swati S More
Journal:  Med Chem Res       Date:  2021-01-15       Impact factor: 1.965

8.  Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A.

Authors:  Corinne Fruit; Florence Couly; Rahul Bhansali; Malini Rammohan; Mattias F Lindberg; John D Crispino; Laurent Meijer; Thierry Besson
Journal:  Pharmaceuticals (Basel)       Date:  2019-12-17

9.  Computational Analysis of Crystallization Additives for the Identification of New Allosteric Sites.

Authors:  Jade Fogha; Julien Diharce; Alan Obled; Samia Aci-Sèche; Pascal Bonnet
Journal:  ACS Omega       Date:  2020-02-03

10.  Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation.

Authors:  Jonathan Elie; Omid Feizbakhsh; Nathalie Desban; Béatrice Josselin; Blandine Baratte; Amandine Bescond; Julien Duez; Xavier Fant; Stéphane Bach; Dominique Marie; Matthieu Place; Sami Ben Salah; Agnes Chartier; Sabine Berteina-Raboin; Apirat Chaikuad; Stefan Knapp; Fabrice Carles; Pascal Bonnet; Frédéric Buron; Sylvain Routier; Sandrine Ruchaud
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
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