Publications

146. Design, Synthesis, and SAR of Covalent KIT and PDGFRA Inhibitors─Exploring Their Potential in Targeting GIST
T. Schulz, R, Gontla, A. Teuber, M. Beerbaum, B. S. Fletcher, T. Mühlenberg, H. Kaitsiotou, J. Hardick, K. Jeyakumar, M. Keul, M. P. Müller, S. Sievers, S. Bauer and D. Rauh
J. Med. Chem.2025

145. Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises
K. A. Pervanidis, G. D. D’Angelo, J. Weisner, S. Brandherm and D. Rauh
J. Med. Chem.202467 (8)6052–6063

144. Targeting KRAS Diversity: Covalent Modulation of G12X and Beyond in Cancer Therapy
T. Kirschner, M. P. Müller and D. Rauh
J. Med. Chem.202467 (8)6044-6051

143. Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA
A. Teuber, T. Schulz, B. S. Fletcher, R. Gontla, T. Mühlenberg, M-L Zischinsky, J. Niggenaber, J. Weisner, S. B. Kleinbölting, J. Lategahn , S. Sievers, M. P. Müller, S. Bauer and D. Rauh
Nat. Communications202415Article number: 63

142. KIT ATP-Binding Pocket/Activation Loop Mutations in GI Stromal Tumor: Emerging Mechanisms of Kinase Inhibitor Escape
T. Mühlenberg, J. Falkenhorst, T. Schulz, B. S. Fletcher, A. Teuber, D. Krzeciesa, I. Klooster, M. Lundberg, L. Wilson, J. Lategahn, M. von Mehren, S. Grunewald, A. I. Tüns, E. Wardelmann, J. K. Sicklick, M. Brahmi, C. Serrano, H. U. Schildhaus, S. Sievers, J. Treckmann, M.C. Heinrich, C. P. Raut, W. B. Ou, A. Marino-Enriquez, S. George, D. Rauh, J. A. Fletcher and S. Bauer
Journal of Clinical Oncology202442 (12)1439-1449

141. Fragtory: Pharmacophore-Focused Design, Synthesis, and Evaluation of an sp3-Enriched Fragment Library
M. Bührmann, S. Kallepu, J. D. Warmuth, J. N. Wiese, C. Ehrt, H, Vatheuer, W. Hiller, C. Seitz, L. Levy, P. Czodrowski, S. Sievers, M. P. Müller, and D. Rauh
J. Med. Chem.202366 (9)6297–6314

140. Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines
T. Grabe, K. Jeyakumar, J. Niggenaber, T. Schulz, S. Koska, S. Kleinbölting, M. E. Beck, M. P. Müller, and D. Rauh
ACS Med. Chem. Lett.202314 (5)591–598

139. Glucocorticoid activation by HSD11B1 limits T cell-driven interferon signaling and response to PD-1 blockade in melanoma
L. M. N. Melo, D. Herrera-Rios, D. Hinze, S. Löffek, I. Oezel, R. Turiello, J. Klein, S. Leonardelli, I.-V. Westedt, Y. Al-Matary, S. Egea-Rodriguez, A. Brenzel, M. Bau, A. Sucker, E. Hadaschik, F. Wirsdörfer, H. Hanenberg, N. Uhlenbrock, D. Rauh, J. Poźniak, F. Rambow, J.-C. Marine, M. Effern, N. Glodde, D. Schadendorf, J. Jablonska, M. Hölzel, and I. Helfrich
J. Immunother. Cancer202311e004150

138. Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors
L. Goebel, T. Kirschner, S. Koska, A. Rai, P. Janning, S. Maffini, H. Vatheuer, P. Czodrowski, R. S. Goody, M. P. Müller, and D. Rauh
eLife202382184

137. Insights into the Conformational Plasticity of the Protein Kinase Akt1 by Multi-Lateral Dipolar Spectroscopy
J. Stehle, J. Weisner, L. Eichhorn, D. Rauh, and M. Drescher
Chem. Eur. J.2023e202203959

136. A high-throughput effector screen identifies a novel small molecule scaffold for inhibition of ten-eleven translocation dioxygenase 2
S. Palei, J. Weisner, M. Vogt, R. Gontla, B. Buchmuller, C. Ehrt, T. Grabe, S. Kleinbölting, M. P. Müller, G. H. Clever, D. Rauh, and D. Summerer
RSC Med. Chem.202313(12)1540–1548

135. Functional noninvasive detection of glycolytic pancreatic ductal adenocarcinoma
I. Heid, C. Münch, S. Karakaya, S. S. Lueong, A. M. Winkelkotte, S. T. Lifers, L. Godfrey, P. F. Y. Cheung, K. Savvatakis, G. J. Topping, F. Englert, L. Kritzner, M. Grashei, A. Tannapfel, R. Viebahn, H. Wolters, W. Uhl, D. Vangala, E. M. M. Smeets, E. H. J. G. Aarntzen, D. Rauh, W. Weichert, J. D. Hoheisel, S. A. Hahn, F. Schilling, R. Braren, M. Trajkovic‑Arsic, and J. T. Siveke
Cancer Metab.202210(24)

134. Optimization of Covalent MKK7 Inhibitors via Crude Nanomole-Scale Libraries
P. Gehrtz, S. Marom, M. Bührmann, J. Hardick, S. Kleinbölting, A. Shraga, C. Dubiella, R. Gabizon, J. N. Wiese, M. P. Müller, G. Cohen, I. Babaev, K. Shurrush, L. Avram, E. Resnick, H. Barr, D. Rauh*, and N. London*
J. Med. Chem.202265 (15)10341–10356

133. Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions
B. Wiedemann , D. Kamps , L. Depta , J. Weisner, J. Cvetreznik, S. Tomassi, S. Gentz, J.-E. Hoffmann, M. P. Müller, O. Koch, L. Dehmelt, and D. Rauh
PLoS One202217 (6)e0267651

132. Persister state-directed transitioning and vulnerability in melanoma
H. Chauvistré, B. Shannan, S. M. Daignault-Mill, R. J. Ju, D. Picard, S. Egetemaier, R. Váraljai, C. S. Gibhardt, A. Sechi, F. Kaschani, O. Keminer, S. J. Stehbens, Q. Liu, X. Yin, K. Jeyakumar, F. C. E. Vogel, C. Krepler, V. W. Rebecca, L. Kubat, S. S. Lueong , J. Forster, S. Horn, M. Remke, M. Ehrmann, A. Paschen, J. C. Becker , I. Helfrich , D. Rauh, M. Kaiser, S. Gul, M. Herlyn, I. Bogeski, J. N. Rodríguez-López, N. K. Haass, D. Schadendorf, A. Roesch
Nat. Commun.202213Article number: 3055

131. Insight Into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors
J. Lategahn, H. L. Tumbrink, C. Schultz-Fademrecht, A. Heimsoeth, L. Werr, J. Niggenaber, M. Keul, F. Parmaksiz, M. Baumann, S. Menninger, E. Zent, I. Landel, J. Weisner, K. Jeyakumar, L. Heyden, N. Russ, F. Müller, C. Lorenz, J. Brägelmann, I. Spille, T. Grabe, M. P. Müller, J. M. Heuckmann, B. Klebl, P. Nussbaumer, M. L. Sos, and D. Rauh
J. Med. Chem.202265 (9)6643–6655

130. Covalent Allosteric Inhibitors of Akt Generated Using a Click Fragment Approach
L. van der Westhuizen, J. Weisner, A. Taher, I. Landel, L. Quambusch, M. Lindemann, N. Uhlenbrock, M. P. Müller, I. R. Green, S. C. Pelly, D. Rauh, and W. A. L. van Otterlo
Chem Med Chem2022e20210077619

10. Cellular model system to dissect the isoform-selectivity of Akt inhibitors
L. Quambusch, L. Depta, I. Landel, M. Lubeck, T. Kirschner, J. Nabert, N. Uhlenbrock, J. Weisner, M. Kostka, L. M. Levy, C. Schultz-Fademrecht, F. Glanemann, K. Althoff, M. P. Müller, J. T. Siveke, and D. Rauh
Nat Commun202112(1)Article number: 5297

09. Resistance to Avapritinib in PDGFRA-driven GIST is caused by secondary mutations 2 in the PDGFRA kinase domain
S. Grunewald, L. R. Klug, T. Mühlenberg, J. Lategahn, J. Falkenhorst, A. Town, C. Ehrt, E. Wardelmann, W. Hartmann, H. Schildhaus, J. Treckmann, J. A. Fletcher, S. Jung, P. Czodrowski, S. Miller, O. Schmidt-Kittler, D. Rauh, M. C. Heinrich, and S. Bauer
Cancer Discov.202111(1)108-125

08. Targeting Her2-insYVMA with Covalent Inhibitors—A Focused Compound Screening and Structure-Based Design Approach
J. Lategahn, J. Hardick, T. Grabe, J. Niggenaber, K. Jeyakumar, M. Keul, H. L. Tumbrink, C. Becker, L. Hodson, T. Kirschner, P. Klövekorn, J. Ketzer, M. Baumann, S. Terheyden, A. Unger, J. Weisner, M. P. Müller, W. A. L. van Otterlo, S. Bauer, and D. Rauh
J. Med. Chem.202063(20)11725–11755

07. KRasG12C inhibitors in clinical trials: a short historical perspective
L. Goebel, M. P. Müller, R. S. Goody and D. Rauh
RSC Med. Chem.202011760-770

06. Conformational selection vs. induced fit: insights into the binding mechanisms of p38α MAP Kinase inhibitors
P. Roser, J. Weisner, J. Stehle, D. Rauh, and M. Drescher
Chem. Commun.2020568818-8821

05. Spotlight on AKT: Current Therapeutic Challenges
I. Landel, L. Quambusch, L. Depta, and D. Rauh
ACS Med. Chem. Lett.202011(3)225-227

04. Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity
L. Quambusch, I. Landel, L. Depta, J. Weisner, N. Uhlenbrock, M. P. Müller, F. Glanemann, K. Althoff, J. T. Siveke, and D. Rauh
Angew. Chem. Int. Ed.2019131(52)18999-19005

03. Inhibition of Osimertinib-Resistant Epidermal Growth Factor Receptor EGFR-T790M/C797S
J. Lategahn, M. Keul, P. Klövekorn, H. L. Tumbrink, J. Niggenaber, M. P. Müller, L. Hodson, M. Flaßhoff, J. Hardick, T. Grabe, J. Engel, C. Schultz-Fademrecht, M. Baumann, J. Ketzer, T. Mühlenberg, W. Hiller, G. Günther, A. Unger, H. Müller, A. Heimsoeth, C. Golz, B. Blank-Landeshammer, L. Kollipara, R. Zahedi, C. Strohmann, J. G. Hengstler, W. van Otterlo, S. Bauer, and D. Rauh
Chemical Science20191010789-10801

02. Structure Defines Function: Clinically Relevant Mutations in ErbB Kinases
J. Niggenaber, J. Hardick, J. Lategahn, D. Rauh
J. Med. Chem.201963(1)40-51

01. 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)
P. Wolle, J. Engel, S. Smith, L. Goebel, E. Hennes, J. Lategahn, and D. Rauh
J. Med. Chem.201962(11)5541-5546

Coordinator

Project contact

Publications