Joerger AC - Search Results

1

Discovery of Nanomolar-Affinity Pharmacological Chaperones Stabilizing the Oncogenic p53 Mutant Y220C.

Stephenson Clarke JR, Douglas LR, Duriez PJ, Balourdas DI, Joerger AC, Khadiullina R, Bulatov E, Baud MGJ. Stephenson Clarke JR, et al. Among authors: joerger ac. ACS Pharmacol Transl Sci. 2022 Oct 11;5(11):1169-1180. doi: 10.1021/acsptsci.2c00164. eCollection 2022 Nov 11. ACS Pharmacol Transl Sci. 2022. PMID: 36407959 Free PMC article.

2

Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53.

Joerger AC, Bauer MR, Wilcken R, Baud MGJ, Harbrecht H, Exner TE, Boeckler FM, Spencer J, Fersht AR. Joerger AC, et al. Structure. 2015 Dec 1;23(12):2246-2255. doi: 10.1016/j.str.2015.10.016. Structure. 2015. PMID: 26636255 Free PMC article.

3

Harnessing Fluorine-Sulfur Contacts and Multipolar Interactions for the Design of p53 Mutant Y220C Rescue Drugs.

Bauer MR, Jones RN, Baud MG, Wilcken R, Boeckler FM, Fersht AR, Joerger AC, Spencer J. Bauer MR, et al. Among authors: joerger ac. ACS Chem Biol. 2016 Aug 19;11(8):2265-74. doi: 10.1021/acschembio.6b00315. Epub 2016 Jun 21. ACS Chem Biol. 2016. PMID: 27267810 Free PMC article.

4

Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines.

Baud MGJ, Bauer MR, Verduci L, Dingler FA, Patel KJ, Horil Roy D, Joerger AC, Fersht AR. Baud MGJ, et al. Among authors: joerger ac. Eur J Med Chem. 2018 May 25;152:101-114. doi: 10.1016/j.ejmech.2018.04.035. Epub 2018 Apr 21. Eur J Med Chem. 2018. PMID: 29702446 Free PMC article.

5

A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C.

Bauer MR, Jones RN, Tareque RK, Springett B, Dingler FA, Verduci L, Patel KJ, Fersht AR, Joerger AC, Spencer J. Bauer MR, et al. Among authors: joerger ac. Future Med Chem. 2019 Oct;11(19):2491-2504. doi: 10.4155/fmc-2019-0181. Future Med Chem. 2019. PMID: 31633398 Free PMC article.

6

Evolutionary history of the p53 family DNA-binding domain: insights from an Alvinella pompejana homolog.

Zhang Q, Balourdas DI, Baron B, Senitzki A, Haran TE, Wiman KG, Soussi T, Joerger AC. Zhang Q, et al. Among authors: joerger ac. Cell Death Dis. 2022 Mar 7;13(3):214. doi: 10.1038/s41419-022-04653-8. Cell Death Dis. 2022. PMID: 35256607 Free PMC article.

7

Structure-Reactivity Studies of 2-Sulfonylpyrimidines Allow Selective Protein Arylation.

Pichon MM, Drelinkiewicz D, Lozano D, Moraru R, Hayward LJ, Jones M, McCoy MA, Allstrum-Graves S, Balourdas DI, Joerger AC, Whitby RJ, Goldup SM, Wells N, Langley GJ, Herniman JM, Baud MGJ. Pichon MM, et al. Among authors: joerger ac. Bioconjug Chem. 2023 Sep 20;34(9):1679-1687. doi: 10.1021/acs.bioconjchem.3c00322. Epub 2023 Sep 1. Bioconjug Chem. 2023. PMID: 37657082 Free PMC article.

8

Synthesis of Pyrazole-Based Macrocycles Leads to a Highly Selective Inhibitor for MST3.

Amrhein JA, Berger LM, Balourdas DI, Joerger AC, Menge A, Krämer A, Frischkorn JM, Berger BT, Elson L, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T. Amrhein JA, et al. Among authors: joerger ac. J Med Chem. 2024 Jan 11;67(1):674-690. doi: 10.1021/acs.jmedchem.3c01980. Epub 2023 Dec 21. J Med Chem. 2024. PMID: 38126712

9

Development of Potent Dual BET/HDAC Inhibitors via Pharmacophore Merging and Structure-Guided Optimization.

Bauer N, Balourdas DI, Schneider JR, Zhang X, Berger LM, Berger BT, Schwalm MP, Klopp NA, Siveke JT, Knapp S, Joerger AC. Bauer N, et al. Among authors: joerger ac. ACS Chem Biol. 2024 Feb 16;19(2):266-279. doi: 10.1021/acschembio.3c00427. Epub 2024 Jan 31. ACS Chem Biol. 2024. PMID: 38291964

10

Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors.

Rak M, Menge A, Tesch R, Berger LM, Balourdas DI, Shevchenko E, Krämer A, Elson L, Berger BT, Abdi I, Wahl LM, Poso A, Kaiser A, Hanke T, Kronenberger T, Joerger AC, Müller S, Knapp S. Rak M, et al. Among authors: joerger ac. J Med Chem. 2024 Mar 14;67(5):3813-3842. doi: 10.1021/acs.jmedchem.3c02217. Epub 2024 Feb 29. J Med Chem. 2024. PMID: 38422480

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