Literature DB >> 29451369

Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor.

Marie-Pierre Collin1, Mario Lobell1, Walter Hübsch1, Dirk Brohm1, Hartmut Schirok1, Rolf Jautelat1, Klemens Lustig2, Ulf Bömer3, Verena Vöhringer4, Mélanie Héroult4, Sylvia Grünewald4, Holger Hess-Stumpp4.   

Abstract

Rogaratinib (BAY 1163877) is a highly potent and selective small-molecule pan-fibroblast growth factor receptor (FGFR) inhibitor (FGFR1-4) for oral application currently being investigated in phase 1 clinical trials for the treatment of cancer. In this publication, we report its discovery by de novo structure-based design and medicinal chemistry optimization together with its pharmacokinetic profile.
© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  cancer; fibroblast growth factor receptor (FGFR); inhibitors; medicinal chemistry; structure-based design

Mesh：

Substances：

Year:  2018        PMID： 29451369     DOI： 10.1002/cmdc.201700718

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  13 in total

Review 1.  FGFR4: A promising therapeutic target for breast cancer and other solid tumors.

Authors:  Kevin M Levine; Kai Ding; Lyuqin Chen; Steffi Oesterreich
Journal:  Pharmacol Ther       Date:  2020-05-31       Impact factor: 12.310

2.  Therapeutic Targeting of FGFR Signaling in Head and Neck Cancer.

Authors:  Zechen Wang; Karen S Anderson
Journal:  Cancer J       Date:  2022 Sep-Oct 01       Impact factor: 2.074

Review 3.  Structure, activation and dysregulation of fibroblast growth factor receptor kinases: perspectives for clinical targeting.

Authors:  Brendan Farrell; Alexander L Breeze
Journal:  Biochem Soc Trans       Date:  2018-12-13       Impact factor: 5.407

Review 4.  Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors.

Authors:  Shuyan Dai; Zhan Zhou; Zhuchu Chen; Guangyu Xu; Yongheng Chen
Journal:  Cells       Date:  2019-06-18       Impact factor: 6.600

5.  Rogaratinib: A potent and selective pan-FGFR inhibitor with broad antitumor activity in FGFR-overexpressing preclinical cancer models.

Authors:  Sylvia Grünewald; Oliver Politz; Sebastian Bender; Mélanie Héroult; Klemens Lustig; Uwe Thuss; Christoph Kneip; Charlotte Kopitz; Dieter Zopf; Marie-Pierre Collin; Ulf Boemer; Stuart Ince; Peter Ellinghaus; Dominik Mumberg; Holger Hess-Stumpp; Karl Ziegelbauer
Journal:  Int J Cancer       Date:  2019-03-13       Impact factor: 7.396

Review 6.  Emerging therapeutic agents for genitourinary cancers.

Authors:  Kevin Zarrabi; Azzam Paroya; Shenhong Wu
Journal:  J Hematol Oncol       Date:  2019-09-04       Impact factor: 17.388

7.  FGFR1 amplification or overexpression and hormonal resistance in luminal breast cancer: rationale for a triple blockade of ER, CDK4/6, and FGFR1.

Authors:  Miguel Quintela-Fandino; Maria J Bueno; Silvana Mouron; Luis Manso; Eduardo Caleiras; Jose L Rodriguez-Peralto; Oscar M Rueda; Carlos Caldas; Ramon Colomer
Journal:  Breast Cancer Res       Date:  2021-02-12       Impact factor: 6.466

8.  An Online Repository of Solvation Thermodynamic and Structural Maps of SARS-CoV-2 Targets.

Authors:  Brian Olson; Anthony Cruz; Lieyang Chen; Mossa Ghattas; Yeonji Ji; Kunhui Huang; Daniel J McKay; Tom Kurtzman
Journal:  ChemRxiv       Date:  2020-05-13

9.  Cyanoamidine Cyclization Approach to Remdesivir's Nucleobase.

Authors:  Rachel R Knapp; Veronica Tona; Taku Okada; Richmond Sarpong; Neil K Garg
Journal:  Org Lett       Date:  2020-10-21       Impact factor: 6.005

10.  An online repository of solvation thermodynamic and structural maps of SARS-CoV-2 targets.

Authors:  Brian Olson; Anthony Cruz; Lieyang Chen; Mossa Ghattas; Yeonji Ji; Kunhui Huang; Steven Ayoub; Tyler Luchko; Daniel J McKay; Tom Kurtzman
Journal:  J Comput Aided Mol Des       Date:  2020-09-12       Impact factor: 4.179
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