Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor-Reference-Cited by-同舟云学术

Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

Published:2022-02-15 Issue:4 Volume:65 Page:3173-3192
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

M. Serafim Ricardo A.¹²³,da Silva Santiago André²³,Schwalm Martin P.⁴⁵,Hu Zexi⁶⁷,dos Reis Caio V.²³,Takarada Jessica E.²³,Mezzomo Priscila²³,Massirer Katlin B.²³,Kudolo Mark¹,Gerstenecker Stefan¹,Chaikuad Apirat⁴⁵^ORCID,Zender Lars⁶⁷⁸,Knapp Stefan⁴⁵⁹^ORCID,Laufer Stefan¹⁷¹⁰^ORCID,Couñago Rafael M.²³^ORCID,Gehringer Matthias¹⁷^ORCID

Affiliation:

1. Department of Pharmaceutical/Medicinal Chemistry, Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany

2. Centro de Química Medicinal (CQMED), Centro de Biologia Molecular e Engenharia Genética (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas, SP 13083-875, Brazil

3. Structural Genomics Consortium, Departamento de Genética e Evolução, Instituto de Biologia, UNICAMP, Campinas, SP 13083-886, Brazil

4. Structural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany

5. Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 9, 60438 Frankfurt am Main, Germany

6. Department of Medical Oncology and Pneumology (Internal Medicine VIII), University Hospital Tübingen, 72076 Tübingen, Germany

7. Cluster of Excellence iFIT (EXC 2180) ‘Image-Guided & Functionally Instructed Tumor Therapies’, University of Tübingen, 72076 Tübingen, Germany

8. German Consortium for Translational Cancer Research (DKTK), Partner Site Tübingen, German Cancer Research Center (DKFZ), 72076 Tübingen, Germany

9. Frankfurt Cancer Institute (FCI) and German Translational Cancer Network (DKTK) Site Frankfurt/Mainz, 60596 Frankfurt am Main, Germany

10. Tübingen Center for Academic Drug Discovery, Auf der Morgenstelle 8, 72076 Tübingen, Germany

Funder

Deutsche Forschungsgemeinschaft

Conselho Nacional de Desenvolvimento Científico e Tecnológico

Innovative Medicines Initiative

Fundação de Amparo à Pesquisa do Estado de São Paulo

Baden-Württemberg Stiftung

Ministerium für Wissenschaft, Forschung und Kunst Baden-Württemberg

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior

Eberhard Karls Universität Tübingen

SGC

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c01165

Reference82 articles.

1. Bub3 reads phosphorylated MELT repeats to promote spindle assembly checkpoint signaling

2. Phosphodependent Recruitment of Bub1 and Bub3 to Spc7/KNL1 by Mph1 Kinase Maintains the Spindle Checkpoint

3. MPS1/Mph1 phosphorylates the kinetochore protein KNL1/Spc7 to recruit SAC components

4. Mps1 Phosphorylates Borealin to Control Aurora B Activity and Chromosome Alignment

5. Effects of the Selective MPS1 Inhibitor MPS1-IN-3 on Glioblastoma Sensitivity to Antimitotic Drugs

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