Andre Richters

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Publications by authors named "Andre Richters"

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23Publications

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An Array-Based Ligand Discovery Platform for Proteins With Short Half-Lives.

Authors:

Becky S Leifer Shelby K Doyle André Richters Helen L Evans Angela N Koehler

Methods Enzymol 2018 19;610:191-218. Epub 2018 Oct 19.

David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA, United States; Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA, United States; The Broad Institute of MIT and Harvard, Cambridge, MA, United States; Department of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA, United States. Electronic address:

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http://dx.doi.org/10.1016/bs.mie.2018.09.019	DOI Listing

June 2019

Targeting protein arginine methyltransferase 5 in disease.

Authors:

André Richters

Future Med Chem 2017 11 27;9(17):2081-2098. Epub 2017 Oct 27.

Department of Biological Engineering, David H Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA.

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http://dx.doi.org/10.4155/fmc-2017-0089	DOI Listing

November 2017

Systematic Kinase Inhibitor Profiling Identifies CDK9 as a Synthetic Lethal Target in NUT Midline Carcinoma.

Cell Rep 2017 Sep;20(12):2833-2845

Molecular Pathology, Institute of Pathology, University of Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Department of Translational Genomics, Medical Faculty, University of Cologne, Weyertal 115b, 50931 Cologne, Germany; Center for Molecular Medicine Cologne, University of Cologne, 50931 Cologne, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2017.08.082	DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5622049	PMC

September 2017

Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34.

Authors:

Lucas Robke Luca Laraia Marjorie A Carnero Corrales Georgios Konstantinidis Makoto Muroi André Richters Michael Winzker Tobias Engbring Stefano Tomassi Nobumoto Watanabe Hiroyuki Osada Daniel Rauh Herbert Waldmann Yao-Wen Wu Julian Engel

Angew Chem Int Ed Engl 2017 07 12;56(28):8153-8157. Epub 2017 Jun 12.

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/anie.201703738	DOI Listing

July 2017

Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.

Sci Transl Med 2017 06;9(394)

Molecular Pathology, Institute of Pathology, Center of Integrated Oncology, University Hospital Cologne, 50937 Cologne, Germany.

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http://dx.doi.org/10.1126/scitranslmed.aah6144	DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5805089	PMC

June 2017

Epigenetic Modulation Using Small Molecules - Targeting Histone Acetyltransferases in Disease.

Authors:

Andre Richters Angela N Koehler

Curr Med Chem 2017 ;24(37):4121-4150

David H. Koch Institute for Integrative Cancer Research, Department of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA, United States.

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http://www.eurekaselect.com/150387/article	Publisher Site
http://dx.doi.org/10.2174/0929867324666170223153115	DOI Listing

January 2017

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant.

Authors:

Marco Radi Ralf Schneider Anna Lucia Fallacara Lorenzo Botta Emmanuele Crespan Cristina Tintori Giovanni Maga Miroslava Kissova Alessia Calgani André Richters Franesca Musumeci Daniel Rauh Silvia Schenone

Bioorg Med Chem Lett 2016 08 18;26(15):3436-40. Epub 2016 Jun 18.

Dipartimento di Farmacia, Università degli Studi di Genova, Viale Benedetto XV, 3, 16132 Genova, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2016.06.051	DOI Listing

August 2016

Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4.

Authors:

Peter Schröder Tim Förster Stefan Kleine Christian Becker André Richters Slava Ziegler Daniel Rauh Kamal Kumar Herbert Waldmann

Angew Chem Int Ed Engl 2015 Oct 23;54(42):12398-403. Epub 2015 Apr 23.

Max-Planck-Institut für Molekulare Physiologie, Abteilung Chemische Biologie, Otto-Hahn-Straße 11, 44227 Dortmund (Germany).

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http://dx.doi.org/10.1002/anie.201501515	DOI Listing

October 2015

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.

J Med Chem 2015 Sep 31;58(17):6844-63. Epub 2015 Aug 31.

Department of Chemistry and Chemical Biology, TU Dortmund University , Otto-Hahn-Straße 6, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01082	DOI Listing

September 2015

Covalent-Allosteric Kinase Inhibitors.

Authors:

Jörn Weisner Rajesh Gontla Leandi van der Westhuizen Sebastian Oeck Julia Ketzer Petra Janning André Richters Thomas Mühlenberg Zhizhou Fang Abu Taher Verena Jendrossek Stephen C Pelly Sebastian Bauer Willem A L van Otterlo Daniel Rauh

Angew Chem Int Ed Engl 2015 Aug 25;54(35):10313-6. Epub 2015 Jun 25.

Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).

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http://dx.doi.org/10.1002/anie.201502142	DOI Listing

August 2015

A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer.

Cell 2015 Jul;162(1):146-59

Department I of Internal Medicine, University Hospital Cologne, Weyertal 115B, 50931 Cologne, Germany; CECAD, University of Cologne, Weyertal 115B, 50931 Cologne, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2015.05.053	DOI Listing

July 2015

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.

Authors:

Debjit Basu André Richters Daniel Rauh

Bioorg Med Chem 2015 Jun 23;23(12):2767-80. Epub 2015 Apr 23.

Department of Chemistry and Chemical Biology, Technische Universität Dortmund, Otto-Hahn-Straße 6, 44227 Dortmund, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.04.038	DOI Listing

June 2015

Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma.

Authors:

Cristina Tintori Anna Lucia Fallacara Marco Radi Claudio Zamperini Elena Dreassi Emmanuele Crespan Giovanni Maga Silvia Schenone Francesca Musumeci Chiara Brullo André Richters Francesca Gasparrini Adriano Angelucci Claudio Festuccia Simona Delle Monache Daniel Rauh Maurizio Botta

J Med Chem 2015 Jan 3;58(1):347-61. Epub 2014 Dec 3.

Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena Via Aldo Moro 2, 53100 Siena, Italy.

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http://dx.doi.org/10.1021/jm5013159	DOI Listing

January 2015

Identification and further development of potent TBK1 inhibitors.

Authors:

André Richters Debjit Basu Julian Engel Meryem S Ercanoglu Hyatt Balke-Want Roberta Tesch Roman K Thomas Daniel Rauh

ACS Chem Biol 2015 Jan;10(1):289-98

Department of Chemistry and Chemical Biology, Technical University of Dortmund , Otto-Hahn-Straße 6, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/cb500908d	DOI Listing

January 2015

Identification of type II and III DDR2 inhibitors.

Authors:

André Richters Hoang D Nguyen Trang Phan Jeffrey R Simard Christian Grütter Julian Engel Daniel Rauh

J Med Chem 2014 May 5;57(10):4252-62. Epub 2014 May 5.

Department of Chemistry and Chemical Biology, Technical University of Dortmund , Otto-Hahn-Straße 6, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm500167q	DOI Listing

May 2014

Cell-autonomous and non-cell-autonomous mechanisms of transformation by amplified FGFR1 in lung cancer.

Cancer Discov 2014 Feb 3;4(2):246-57. Epub 2013 Dec 3.

1Department of Translational Genomics, University of Cologne; 2Max-Planck-Institute for Neurological Research; Institutes of 3Pathology and 4Virology, University of Cologne;5Department I of Internal Medicine and Center for Integrated Oncology, University Hospital of Cologne; 6Blackfield AG, Cologne; 7Technical University Dortmund, Dortmund, Germany; 8Medical Oncology and 9Institute of Pathology, Cantonal Hospital, Luzern; 10Novartis Pharma AG, Basel, Switzerland; and 11Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, India.

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http://cancerdiscovery.aacrjournals.org/cgi/doi/10.1158/2159	Publisher Site
http://dx.doi.org/10.1158/2159-8290.CD-13-0323	DOI Listing

February 2014

Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood.

Authors:

Benjamin Baur Kirsten Storch Kathrin E Martz Marcia I Goettert André Richters Daniel Rauh Stefan A Laufer

J Med Chem 2013 Nov 5;56(21):8561-78. Epub 2013 Nov 5.

Institute of Pharmacy , Department of Pharmaceutical and Medicinal Chemistry, Eberhard-Karls-University Tübingen , Auf der Morgenstelle 8, 72076 Tübingen, Germany.

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http://dx.doi.org/10.1021/jm401276h	DOI Listing

November 2013

Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.

Authors:

André Richters Julia Ketzer Matthäus Getlik Christian Grütter Ralf Schneider Johannes M Heuckmann Stefanie Heynck Martin L Sos Anu Gupta Anke Unger Carsten Schultz-Fademrecht Roman K Thomas Sebastian Bauer Daniel Rauh

J Med Chem 2013 Jul 10;56(14):5757-72. Epub 2013 Jul 10.

Department of Chemistry and Chemical Biology, Technical University of Dortmund, Otto-Hahn-Strasse 6, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm4004076	DOI Listing

July 2013

De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.

Authors:

Robert Urich Grant Wishart Michael Kiczun André Richters Naomi Tidten-Luksch Daniel Rauh Brad Sherborne Paul G Wyatt Ruth Brenk

ACS Chem Biol 2013 May 27;8(5):1044-52. Epub 2013 Mar 27.

Drug Discovery Unit (DDU), Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, DD1 5EH, UK.

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http://pubs.acs.org/doi/10.1021/cb300729y	Publisher Site
http://dx.doi.org/10.1021/cb300729y	DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3833278	PMC

May 2013

A framework for identification of actionable cancer genome dependencies in small cell lung cancer.

Proc Natl Acad Sci U S A 2012 Oct 3;109(42):17034-9. Epub 2012 Oct 3.

Department of Translational Genomics, University of Cologne, 50931 Cologne, Germany.

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http://dx.doi.org/10.1073/pnas.1207310109	DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3479457	PMC

October 2012

Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.

Authors:

Christian Grütter Jeffrey R Simard Svenja C Mayer-Wrangowski Peter H Schreier José Pérez-Martín André Richters Matthäus Getlik Oliver Gutbrod Christoph A Braun Michael E Beck Daniel Rauh

ACS Chem Biol 2012 Jul 15;7(7):1257-67. Epub 2012 May 15.

Fakultät Chemie - Chemische Biologie, Technische Universität Dortmund, Germany.

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http://dx.doi.org/10.1021/cb300128b	DOI Listing

July 2012

A chemical genetic approach for covalent inhibition of analogue-sensitive aurora kinase.

Authors:

André Koch Haridas B Rode André Richters Daniel Rauh Silke Hauf

ACS Chem Biol 2012 Apr 1;7(4):723-31. Epub 2012 Feb 1.

Friedrich Miescher Laboratory of the Max Planck Society, Tübingen, Germany.

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http://dx.doi.org/10.1021/cb200465c	DOI Listing

April 2012

Proteus in the world of proteins: conformational changes in protein kinases.

Authors:

Matthias Rabiller Matthäus Getlik Sabine Klüter André Richters Sandra Tückmantel Jeffrey R Simard Daniel Rauh

Arch Pharm (Weinheim) 2010 Apr;343(4):193-206

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://doi.wiley.com/10.1002/ardp.201000028	Publisher Site
http://dx.doi.org/10.1002/ardp.201000028	DOI Listing

April 2010