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Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.
Lategahn J, Tumbrink HL, Schultz-Fademrecht C, Heimsoeth A, Werr L, Niggenaber J, Keul M, Parmaksiz F, Baumann M, Menninger S, Zent E, Landel I, Weisner J, Jeyakumar K, Heyden L, Russ N, Müller F, Lorenz C, Brägelmann J, Spille I, Grabe T, Müller MP, Heuckmann JM, Klebl BM, Nussbaumer P, Sos ML, Rauh D. Lategahn J, et al. Among authors: weisner j. J Med Chem. 2022 May 12;65(9):6643-6655. doi: 10.1021/acs.jmedchem.1c02080. Epub 2022 Apr 29. J Med Chem. 2022. PMID: 35486541
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. Weisner J, et al. Angew Chem Int Ed Engl. 2015 Aug 24;54(35):10313-6. doi: 10.1002/anie.201502142. Epub 2015 Jun 25. Angew Chem Int Ed Engl. 2015. PMID: 26110718
Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants.
Bührmann M, Hardick J, Weisner J, Quambusch L, Rauh D. Bührmann M, et al. Among authors: weisner j. Angew Chem Int Ed Engl. 2017 Oct 16;56(43):13232-13236. doi: 10.1002/anie.201706345. Epub 2017 Sep 22. Angew Chem Int Ed Engl. 2017. PMID: 28834017
Chemical modulation of transcription factors.
Wiedemann B, Weisner J, Rauh D. Wiedemann B, et al. Among authors: weisner j. Medchemcomm. 2018 Jul 11;9(8):1249-1272. doi: 10.1039/c8md00273h. eCollection 2018 Aug 1. Medchemcomm. 2018. PMID: 30151079 Free PMC article. Review.
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. Weisner J, et al. Cancer Res. 2019 May 1;79(9):2367-2378. doi: 10.1158/0008-5472.CAN-18-2861. Epub 2019 Mar 11. Cancer Res. 2019. PMID: 30858154
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 . Schehr M , et al. Among authors: weisner j. Photochem Photobiol Sci. 2019 Jun 12;18(6):1398-1407. doi: 10.1039/c9pp00010k. Photochem Photobiol Sci. 2019. PMID: 30924488
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. Uhlenbrock N, et al. Among authors: weisner j. Chem Sci. 2019 Feb 13;10(12):3573-3585. doi: 10.1039/c8sc05212c. eCollection 2019 Mar 28. Chem Sci. 2019. PMID: 30996949 Free PMC article.
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. Quambusch L, et al. Among authors: weisner j. Angew Chem Int Ed Engl. 2019 Dec 19;58(52):18823-18829. doi: 10.1002/anie.201909857. Epub 2019 Nov 8. Angew Chem Int Ed Engl. 2019. PMID: 31584233 Free PMC article.
24 results