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Items: 1 to 50 of 146

1.

Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity.

Quambusch L, Landel I, Depta L, Weisner J, Uhlenbrock N, Müller MP, Glanemann F, Althoff K, Siveke JT, Rauh D.

Angew Chem Int Ed Engl. 2019 Oct 4. doi: 10.1002/anie.201909857. [Epub ahead of print]

PMID:
31584233
2.

Structure Defines Function: Clinically Relevant Mutations in ErbB Kinases.

Niggenaber J, Hardick J, Lategahn J, Rauh D.

J Med Chem. 2019 Aug 28. doi: 10.1021/acs.jmedchem.9b00964. [Epub ahead of print]

PMID:
31414802
3.

Mutant-Specific Targeting of Ras G12C Activity by Covalently Reacting Small Molecules.

Goody RS, Müller MP, Rauh D.

Cell Chem Biol. 2019 Oct 17;26(10):1338-1348. doi: 10.1016/j.chembiol.2019.07.005. Epub 2019 Aug 1. Review.

PMID:
31378709
4.

Characterization of Covalent Pyrazolopyrimidine-MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7).

Wolle P, Engel J, Smith S, Goebel L, Hennes E, Lategahn J, Rauh D.

J Med Chem. 2019 Jun 13;62(11):5541-5546. doi: 10.1021/acs.jmedchem.9b00472. Epub 2019 May 31.

PMID:
31083997
5.

Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.

Uhlenbrock N, Smith S, Weisner J, Landel I, Lindemann M, Le TA, Hardick J, Gontla R, Scheinpflug R, Czodrowski P, Janning P, Depta L, Quambusch L, Müller MP, Engels B, Rauh D.

Chem Sci. 2019 Feb 13;10(12):3573-3585. doi: 10.1039/c8sc05212c. eCollection 2019 Mar 28.

6.

2-Azo-, 2-diazocine-thiazols and 2-azo-imidazoles as photoswitchable kinase inhibitors: limitations and pitfalls of the photoswitchable inhibitor approach.

Schehr M, Ianes C, Weisner J, Heintze L, Müller MP, Pichlo C, Charl J, Brunstein E, Ewert J, Lehr M, Baumann U, Rauh D, Knippschild U, Peifer C, Herges R.

Photochem Photobiol Sci. 2019 Jun 12;18(6):1398-1407. doi: 10.1039/c9pp00010k.

PMID:
30924488
7.

Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal Cancer.

Weisner J, Landel I, Reintjes C, Uhlenbrock N, Trajkovic-Arsic M, Dienstbier N, Hardick J, Ladigan S, Lindemann M, Smith S, Quambusch L, Scheinpflug R, Depta L, Gontla R, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Maghnouj A, Müller MP, Pohl M, Teschendorf C, Wolters H, Viebahn R, Tannapfel A, Uhl W, Hengstler JG, Hahn SA, Siveke JT, Rauh D.

Cancer Res. 2019 May 1;79(9):2367-2378. doi: 10.1158/0008-5472.CAN-18-2861. Epub 2019 Mar 11.

PMID:
30858154
8.

Co-crystal structure determination and cellular evaluation of 1,4-dihydropyrazolo[4,3-c] [1,2] benzothiazine 5,5-dioxide p38α MAPK inhibitors.

Bartolini D, Bührmann M, Barreca ML, Manfroni G, Cecchetti V, Rauh D, Galli F.

Biochem Biophys Res Commun. 2019 Apr 9;511(3):579-586. doi: 10.1016/j.bbrc.2019.02.063. Epub 2019 Feb 27.

PMID:
30824186
9.

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.

Wolle P, Hardick J, Cronin SJF, Engel J, Baumann M, Lategahn J, Penninger JM, Rauh D.

J Med Chem. 2019 Mar 14;62(5):2843-2848. doi: 10.1021/acs.jmedchem.9b00102. Epub 2019 Feb 21.

PMID:
30768270
10.

A novel scaffold for EGFR inhibition: Introducing N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives.

do Amaral DN, Lategahn J, Fokoue HH, da Silva EMB, Sant'Anna CMR, Rauh D, Barreiro EJ, Laufer S, Lima LM.

Sci Rep. 2019 Jan 9;9(1):14. doi: 10.1038/s41598-018-36846-7.

11.

The unraveling of substrate specificity of histone deacetylase 6 domains using acetylome peptide microarrays and peptide libraries.

Kutil Z, Skultetyova L, Rauh D, Meleshin M, Snajdr I, Novakova Z, Mikesova J, Pavlicek J, Hadzima M, Baranova P, Havlinova B, Majer P, Schutkowski M, Barinka C.

FASEB J. 2019 Mar;33(3):4035-4045. doi: 10.1096/fj.201801680R. Epub 2018 Nov 29.

PMID:
30496698
12.

Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors.

Fassunke J, Müller F, Keul M, Michels S, Dammert MA, Schmitt A, Plenker D, Lategahn J, Heydt C, Brägelmann J, Tumbrink HL, Alber Y, Klein S, Heimsoeth A, Dahmen I, Fischer RN, Scheffler M, Ihle MA, Priesner V, Scheel AH, Wagener S, Kron A, Frank K, Garbert K, Persigehl T, Püsken M, Haneder S, Schaaf B, Rodermann E, Engel-Riedel W, Felip E, Smit EF, Merkelbach-Bruse S, Reinhardt HC, Kast SM, Wolf J, Rauh D, Büttner R, Sos ML.

Nat Commun. 2018 Nov 7;9(1):4655. doi: 10.1038/s41467-018-07078-0.

13.

Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α.

Roser P, Weisner J, Simard JR, Rauh D, Drescher M.

Chem Commun (Camb). 2018 Oct 23;54(85):12057-12060. doi: 10.1039/c8cc06128a.

PMID:
30295691
14.

Chemical modulation of transcription factors.

Wiedemann B, Weisner J, Rauh D.

Medchemcomm. 2018 Jul 11;9(8):1249-1272. doi: 10.1039/c8md00273h. eCollection 2018 Aug 1. Review.

15.

C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer?

Grabe T, Lategahn J, Rauh D.

ACS Med Chem Lett. 2018 Jul 23;9(8):779-782. doi: 10.1021/acsmedchemlett.8b00314. eCollection 2018 Aug 9.

16.

RASPELD to Perform High-End Screening in an Academic Environment toward the Development of Cancer Therapeutics.

Wolle P, Weisner J, Keul M, Landel I, Lategahn J, Rauh D.

ChemMedChem. 2018 Oct 8;13(19):2065-2072. doi: 10.1002/cmdc.201800477. Epub 2018 Aug 23.

PMID:
30079978
17.

Insights into the Kinetics of the Resistance Formation of Bacteria against Ciprofloxacin Poly(2-methyl-2-oxazoline) Conjugates.

Schmidt M, Romanovska A, Wolf Y, Nguyen TD, Krupp A, Tumbrink HL, Lategahn J, Volmer J, Rauh D, Luetz S, Krumm C, Tiller JC.

Bioconjug Chem. 2018 Aug 15;29(8):2671-2678. doi: 10.1021/acs.bioconjchem.8b00361. Epub 2018 Jul 11.

PMID:
29927244
18.

An Unusual Intramolecular Halogen Bond Guides Conformational Selection.

Tesch R, Becker C, Müller MP, Beck ME, Quambusch L, Getlik M, Lategahn J, Uhlenbrock N, Costa FN, Polêto MD, Pinheiro PSM, Rodrigues DA, Sant'Anna CMR, Ferreira FF, Verli H, Fraga CAM, Rauh D.

Angew Chem Int Ed Engl. 2018 Jul 26;57(31):9970-9975. doi: 10.1002/anie.201804917. Epub 2018 Jul 9.

PMID:
29873877
19.

Donated chemical probes for open science.

Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A.

Elife. 2018 Apr 20;7. pii: e34311. doi: 10.7554/eLife.34311.

20.

Augmented Reality in Scientific Publications-Taking the Visualization of 3D Structures to the Next Level.

Wolle P, Müller MP, Rauh D.

ACS Chem Biol. 2018 Mar 16;13(3):496-499. doi: 10.1021/acschembio.8b00153.

PMID:
29544257
21.

Try Me: Promiscuous Inhibitors Still Allow for Selective Targeted Protein Degradation.

Müller MP, Rauh D.

Cell Chem Biol. 2018 Jan 18;25(1):4-6. doi: 10.1016/j.chembiol.2018.01.004.

22.

Lessons To Be Learned: The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer.

Lategahn J, Keul M, Rauh D.

Angew Chem Int Ed Engl. 2018 Feb 23;57(9):2307-2313. doi: 10.1002/anie.201710398. Epub 2018 Jan 12. Review.

PMID:
29178586
23.

Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.

Kaitsiotou H, Keul M, Hardick J, Mühlenberg T, Ketzer J, Ehrt C, Krüll J, Medda F, Koch O, Giordanetto F, Bauer S, Rauh D.

J Med Chem. 2017 Nov 9;60(21):8801-8815. doi: 10.1021/acs.jmedchem.7b00841. Epub 2017 Oct 24.

PMID:
28991465
24.

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

Brägelmann J, Dammert MA, Dietlein F, Heuckmann JM, Choidas A, Böhm S, Richters A, Basu D, Tischler V, Lorenz C, Habenberger P, Fang Z, Ortiz-Cuaran S, Leenders F, Eickhoff J, Koch U, Getlik M, Termathe M, Sallouh M, Greff Z, Varga Z, Balke-Want H, French CA, Peifer M, Reinhardt HC, Örfi L, Kéri G, Ansén S, Heukamp LC, Büttner R, Rauh D, Klebl BM, Thomas RK, Sos ML.

Cell Rep. 2017 Sep 19;20(12):2833-2845. doi: 10.1016/j.celrep.2017.08.082.

25.

Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK.

Bührmann M, Wiedemann BM, Müller MP, Hardick J, Ecke M, Rauh D.

PLoS One. 2017 Sep 11;12(9):e0184627. doi: 10.1371/journal.pone.0184627. eCollection 2017.

26.

Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.

Engel J, Smith S, Lategahn J, Tumbrink HL, Goebel L, Becker C, Hennes E, Keul M, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Hengstler JG, Rauh D.

J Med Chem. 2017 Sep 28;60(18):7725-7744. doi: 10.1021/acs.jmedchem.7b00515. Epub 2017 Sep 18.

PMID:
28853575
27.

Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.

Walter NM, Wentsch HK, Bührmann M, Bauer SM, Döring E, Mayer-Wrangowski S, Sievers-Engler A, Willemsen-Seegers N, Zaman G, Buijsman R, Lämmerhofer M, Rauh D, Laufer SA.

J Med Chem. 2017 Oct 12;60(19):8027-8054. doi: 10.1021/acs.jmedchem.7b00745. Epub 2017 Sep 7.

PMID:
28834431
28.

Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants.

Bührmann M, Hardick J, Weisner J, Quambusch L, Rauh D.

Angew Chem Int Ed Engl. 2017 Oct 16;56(43):13232-13236. doi: 10.1002/anie.201706345. Epub 2017 Sep 22.

PMID:
28834017
29.

Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.

Günther M, Lategahn J, Juchum M, Döring E, Keul M, Engel J, Tumbrink HL, Rauh D, Laufer S.

J Med Chem. 2017 Jul 13;60(13):5613-5637. doi: 10.1021/acs.jmedchem.7b00316. Epub 2017 Jun 21.

PMID:
28603991
30.

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

Robke L, Laraia L, Carnero Corrales MA, Konstantinidis G, Muroi M, Richters A, Winzker M, Engbring T, Tomassi S, Watanabe N, Osada H, Rauh D, Waldmann H, Wu YW, Engel J.

Angew Chem Int Ed Engl. 2017 Jul 3;56(28):8153-8157. doi: 10.1002/anie.201703738. Epub 2017 Jun 12.

PMID:
28544137
31.

Characterization of Covalent-Reversible EGFR Inhibitors.

Smith S, Keul M, Engel J, Basu D, Eppmann S, Rauh D.

ACS Omega. 2017 Apr 30;2(4):1563-1575. doi: 10.1021/acsomega.7b00157. Epub 2017 Apr 20.

32.

Optimized Target Residence Time: Type I1/2 Inhibitors for p38α MAP Kinase with Improved Binding Kinetics through Direct Interaction with the R-Spine.

Wentsch HK, Walter NM, Bührmann M, Mayer-Wrangowski S, Rauh D, Zaman GJR, Willemsen-Seegers N, Buijsman RC, Henning M, Dauch D, Zender L, Laufer S.

Angew Chem Int Ed Engl. 2017 May 2;56(19):5363-5367. doi: 10.1002/anie.201701185. Epub 2017 Apr 11.

PMID:
28397331
33.

Optimized 4,5-Diarylimidazoles as Potent/Selective Inhibitors of Protein Kinase CK1δ and Their Structural Relation to p38α MAPK.

Halekotte J, Witt L, Ianes C, Krüger M, Bührmann M, Rauh D, Pichlo C, Brunstein E, Luxenburger A, Baumann U, Knippschild U, Bischof J, Peifer C.

Molecules. 2017 Mar 24;22(4). pii: E522. doi: 10.3390/molecules22040522.

34.

Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.

Tomassi S, Lategahn J, Engel J, Keul M, Tumbrink HL, Ketzer J, Mühlenberg T, Baumann M, Schultz-Fademrecht C, Bauer S, Rauh D.

J Med Chem. 2017 Mar 23;60(6):2361-2372. doi: 10.1021/acs.jmedchem.6b01626. Epub 2017 Mar 10.

PMID:
28225269
35.

Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR.

Engel J, Becker C, Lategahn J, Keul M, Ketzer J, Mühlenberg T, Kollipara L, Schultz-Fademrecht C, Zahedi RP, Bauer S, Rauh D.

Angew Chem Int Ed Engl. 2016 Aug 26;55(36):10909-12. doi: 10.1002/anie.201605011. Epub 2016 Aug 5.

PMID:
27496389
36.

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

Radi M, Schneider R, Fallacara AL, Botta L, Crespan E, Tintori C, Maga G, Kissova M, Calgani A, Richters A, Musumeci F, Rauh D, Schenone S.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3436-40. doi: 10.1016/j.bmcl.2016.06.051. Epub 2016 Jun 18.

PMID:
27374241
37.

11th German Conference on Chemoinformatics (GCC 2015) : Fulda, Germany. 8-10 November 2015.

Fechner U, de Graaf C, Torda AE, Güssregen S, Evers A, Matter H, Hessler G, Richmond NJ, Schmidtke P, Segler MHS, Waller MP, Pleik S, Shea JE, Levine Z, Mullen R, van den Broek K, Epple M, Kuhn H, Truszkowski A, Zielesny A, Fraaije JH, Gracia RS, Kast SM, Bulusu KC, Bender A, Yosipof A, Nahum O, Senderowitz H, Krotzky T, Schulz R, Wolber G, Bietz S, Rarey M, Zimmermann MO, Lange A, Ruff M, Heidrich J, Onlia I, Exner TE, Boeckler FM, Bermudez M, Firaha DS, Hollóczki O, Kirchner B, Tautermann CS, Volkamer A, Eid S, Turk S, Rippmann F, Fulle S, Saleh N, Saladino G, Gervasio FL, Haensele E, Banting L, Whitley DC, Oliveira Santos JS, Bureau R, Clark T, Sandmann A, Lanig H, Kibies P, Heil J, Hoffgaard F, Frach R, Engel J, Smith S, Basu D, Rauh D, Kohlbacher O, Boeckler FM, Essex JW, Bodnarchuk MS, Ross GA, Finkelmann AR, Göller AH, Schneider G, Husch T, Schütter C, Balducci A, Korth M, Ntie-Kang F, Günther S, Sippl W, Mbaze LM, Ntie-Kang F, Simoben CV, Lifongo LL, Ntie-Kang F, Judson P, Barilla J, Lokajíček MV, Pisaková H, Simr P, Kireeva N, Petrov A, Ostroumov D, Solovev VP, Pervov VS, Friedrich NO, Sommer K, Rarey M, Kirchmair J, Proschak E, Weber J, Moser D, Kalinowski L, Achenbach J, Mackey M, Cheeseright T, Renner G, Renner G, Schmidt TC, Schram J, Egelkraut-Holtus M, van Oeyen A, Kalliokoski T, Fourches D, Ibezim A, Mbah CJ, Adikwu UM, Nwodo NJ, Steudle A, Masek BB, Nagy S, Baker D, Soltanshahi F, Dorfman R, Dubrucq K, Patel H, Koch O, Mrugalla F, Kast SM, Ain QU, Fuchs JE, Owen RM, Omoto K, Torella R, Pryde DC, Glen R, Bender A, Hošek P, Spiwok V, Mervin LH, Barrett I, Firth M, Murray DC, McWilliams L, Cao Q, Engkvist O, Warszycki D, Śmieja M, Bojarski AJ, Aniceto N, Freitas A, Ghafourian T, Herrmann G, Eigner-Pitto V, Naß A, Kurczab R, Bojarski AJ, Lange A, Günther MB, Hennig S, Büttner FM, Schall C, Sievers-Engler A, Ansideri F, Koch P, Stehle T, Laufer S, Böckler FM, Zdrazil B, Montanari F, Ecker GF, Grebner C, Hogner A, Ulander J, Edman K, Guallar V, Tyrchan C, Ulander J, Tyrchan C, Klute W, Bergström F, Kramer C, Nguyen QD, Frach R, Kibies P, Strohfeldt S, Böttcher S, Pongratz T, Horinek D, Kast SM, Rupp B, Al-Yamori R, Lisurek M, Kühne R, Furtado F, van den Broek K, Wessjohann L, Mathea M, Baumann K, Mohamad-Zobir SZ, Fu X, Fan TP, Bender A, Kuhn MA, Sotriffer CA, Zoufir A, Li X, Mervin L, Berg E, Polokoff M, Ihlenfeldt WD, Ihlenfeldt WD, Pretzel J, Alhalabi Z, Fraczkiewicz R, Waldman M, Clark RD, Shaikh N, Garg P, Kos A, Himmler HJ, Sandmann A, Jardin C, Sticht H, Steinbrecher TB, Dahlgren M, Cappel D, Lin T, Wang L, Krilov G, Abel R, Friesner R, Sherman W, Pöhner IA, Panecka J, Wade RC, Bietz S, Schomburg KT, Hilbig M, Rarey M, Jäger C, Wieczorek V, Westerhoff LM, Borbulevych OY, Demuth HU, Buchholz M, Schmidt D, Rickmeyer T, Krotzky T, Kolb P, Mittal S, Sánchez-García E, Nogueira MS, Oliveira TB, da Costa FB, Schmidt TJ.

J Cheminform. 2016 Apr 26;8(Suppl 1):18. doi: 10.1186/s13321-016-0119-5. No abstract available.

38.

Monitoring Conformational Changes in the Receptor Tyrosine Kinase EGFR.

Becker C, Öcal S, Nguyen HD, Phan T, Keul M, Simard JR, Rauh D.

Chembiochem. 2016 Jun 2;17(11):990-4. doi: 10.1002/cbic.201600115. Epub 2016 Apr 21.

PMID:
26991964
39.

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer.

Engel J, Lategahn J, Rauh D.

ACS Med Chem Lett. 2015 Dec 18;7(1):2-5. doi: 10.1021/acsmedchemlett.5b00475. eCollection 2016 Jan 14.

40.

Intermittent high-dose treatment with erlotinib enhances therapeutic efficacy in EGFR-mutant lung cancer.

Schöttle J, Chatterjee S, Volz C, Siobal M, Florin A, Rokitta D, Hinze Y, Dietlein F, Plenker D, König K, Albus K, Heuckmann JM, Rauh D, Franz T, Neumaier B, Fuhr U, Heukamp LC, Ullrich RT.

Oncotarget. 2015 Nov 17;6(36):38458-68. doi: 10.18632/oncotarget.6276.

41.

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

Engel J, Richters A, Getlik M, Tomassi S, Keul M, Termathe M, Lategahn J, Becker C, Mayer-Wrangowski S, Grütter C, Uhlenbrock N, Krüll J, Schaumann N, Eppmann S, Kibies P, Hoffgaard F, Heil J, Menninger S, Ortiz-Cuaran S, Heuckmann JM, Tinnefeld V, Zahedi RP, Sos ML, Schultz-Fademrecht C, Thomas RK, Kast SM, Rauh D.

J Med Chem. 2015 Sep 10;58(17):6844-63. doi: 10.1021/acs.jmedchem.5b01082. Epub 2015 Aug 31.

PMID:
26275028
42.

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

Dietlein F, Kalb B, Jokic M, Noll EM, Strong A, Tharun L, Ozretić L, Künstlinger H, Kambartel K, Randerath WJ, Jüngst C, Schmitt A, Torgovnick A, Richters A, Rauh D, Siedek F, Persigehl T, Mauch C, Bartkova J, Bradley A, Sprick MR, Trumpp A, Rad R, Saur D, Bartek J, Wolf J, Büttner R, Thomas RK, Reinhardt HC.

Cell. 2015 Jul 2;162(1):146-59. doi: 10.1016/j.cell.2015.05.053. Erratum in: Cell. 2015 Aug 27;162(5):1169.

43.

Covalent-Allosteric Kinase Inhibitors.

Weisner J, Gontla R, van der Westhuizen L, Oeck S, Ketzer J, Janning P, Richters A, Mühlenberg T, Fang Z, Taher A, Jendrossek V, Pelly SC, Bauer S, van Otterlo WA, Rauh D.

Angew Chem Int Ed Engl. 2015 Aug 24;54(35):10313-6. doi: 10.1002/anie.201502142. Epub 2015 Jun 25.

PMID:
26110718
44.

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

Basu D, Richters A, Rauh D.

Bioorg Med Chem. 2015 Jun 15;23(12):2767-80. doi: 10.1016/j.bmc.2015.04.038. Epub 2015 Apr 23. Erratum in: Bioorg Med Chem. 2015 Aug 1;23(15):5075.

PMID:
25975640
45.

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

Schröder P, Förster T, Kleine S, Becker C, Richters A, Ziegler S, Rauh D, Kumar K, Waldmann H.

Angew Chem Int Ed Engl. 2015 Oct 12;54(42):12398-403. doi: 10.1002/anie.201501515. Epub 2015 Apr 23.

PMID:
25908259
46.

Monitoring ligand-induced conformational changes for the identification of estrogen receptor agonists and antagonists.

Mayer-Wrangowski SC, Rauh D.

Angew Chem Int Ed Engl. 2015 Mar 27;54(14):4379-82. doi: 10.1002/anie.201410148. Epub 2015 Feb 9.

PMID:
25664555
47.

Identification and further development of potent TBK1 inhibitors.

Richters A, Basu D, Engel J, Ercanoglu MS, Balke-Want H, Tesch R, Thomas RK, Rauh D.

ACS Chem Biol. 2015 Jan 16;10(1):289-98. doi: 10.1021/cb500908d.

PMID:
25540906
48.

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.

Tintori C, Fallacara AL, Radi M, Zamperini C, Dreassi E, Crespan E, Maga G, Schenone S, Musumeci F, Brullo C, Richters A, Gasparrini F, Angelucci A, Festuccia C, Delle Monache S, Rauh D, Botta M.

J Med Chem. 2015 Jan 8;58(1):347-61. doi: 10.1021/jm5013159. Epub 2014 Dec 3.

PMID:
25469771
49.

FLiK: a direct-binding assay for the identification and kinetic characterization of stabilizers of inactive kinase conformations.

Simard JR, Rauh D.

Methods Enzymol. 2014;548:147-71. doi: 10.1016/B978-0-12-397918-6.00006-9. Review.

PMID:
25399645
50.

Correlating structure and ligand affinity in drug discovery: a cautionary tale involving second shell residues.

Tziridis A, Rauh D, Neumann P, Kolenko P, Menzel A, Bräuer U, Ursel C, Steinmetzer P, Stürzebecher J, Schweinitz A, Steinmetzer T, Stubbs MT.

Biol Chem. 2014 Jul;395(7-8):891-903. doi: 10.1515/hsz-2014-0158.

PMID:
25003390

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