日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Targeting the p53 cancer mutants Y220C, Y220N, and Y220S with the small-molecule stabilizer rezatapopt.

使用小分子稳定剂rezatapopt靶向p53癌症突变体Y220C、Y220N和Y220S。

Mavridi Danai, Funk Julianne S, Balourdas Dimitrios-Ilias, Krämer Andreas, Khan Tareque Raysa, Timofeev Oleg, Spencer John, Stiewe Thorsten, Joerger Andreas C

Deep CRISPR mutagenesis characterizes the functional diversity of TP53 mutations.

深度 CRISPR 诱变表征了 TP53 突变的功能多样性

Funk Julianne S, Klimovich Maria, Drangenstein Daniel, Pielhoop Ole, Hunold Pascal, Borowek Anna, Noeparast Maxim, Pavlakis Evangelos, Neumann Michelle, Balourdas Dimitrios-Ilias, Kochhan Katharina, Merle Nastasja, Bullwinkel Imke, Wanzel Michael, Elmshäuser Sabrina, Teply-Szymanski Julia, Nist Andrea, Procida Tara, Bartkuhn Marek, Humpert Katharina, Mernberger Marco, Savai Rajkumar, Soussi Thierry, Joerger Andreas C, Stiewe Thorsten

Structure-Guided Design of ISOX-DUAL-Based Degraders Targeting BRD4 and CBP/EP300: A Case of Degrader Collapse.

基于 ISOX-DUAL 的结构导向降解剂设计:针对 BRD4 和 CBP/EP300 的降解剂崩溃案例

Edmonds Anthony K, Balourdas Dimitrios-Ilias, Marsh Graham P, Felix Robert, Brasher Bradley, Cooper Jeff, Graber-Feesl Cari, Kollareddy Madhu, Malik Karim, Stewart Helen, Chevassut Timothy J T, Lineham Ella, Morley Simon, Fedorov Oleg, Bennett James, Rajasekaran Mohan B, Ojeda Samuel, Harrison Drew A, Ott Christopher J, Joerger Andreas C, Maple Hannah J, Spencer John

Structural basis of p53 inactivation by cavity-creating cancer mutations and its implications for the development of mutant p53 reactivators

p53失活的结构基础及其对突变型p53激活剂研发的影响

Balourdas, Dimitrios-Ilias; Markl, Anja M; Krämer, Andreas; Settanni, Giovanni; Joerger, Andreas C

Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε

新型二氢蝶啶酮衍生物作为未充分研究的人类激酶痘苗相关激酶 1 和酪蛋白激酶 1δ/ε 的有效抑制剂

Fernando H de Souza Gama, Luiz A Dutra, Michael Hawgood, Caio Vinícius Dos Reis, Ricardo A M Serafim, Marcos A Ferreira Jr, Bruno V M Teodoro, Jéssica Emi Takarada, André S Santiago, Dimitrios-Ilias Balourdas, Ann-Sofie Nilsson, Bruno Urien, Vitor M Almeida, Carina Gileadi, Priscila Z Ramos, Anita S

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

通过药效团合并和结构引导优化开发有效的双重 BET/HDAC 抑制剂

Nicolas Bauer, Dimitrios-Ilias Balourdas, Joel R Schneider, Xin Zhang, Lena M Berger, Benedict-Tilman Berger, Martin P Schwalm, Nick A Klopp, Jens T Siveke, Stefan Knapp, Andreas C Joerger

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

2-磺酰基嘧啶的结构-反应性研究实现了选择性蛋白质芳基化

Pichon, Maëva M; Drelinkiewicz, Dawid; Lozano, David; Moraru, Ruxandra; Hayward, Laura J; Jones, Megan; McCoy, Michael A; Allstrum-Graves, Samuel; Balourdas, Dimitrios-Ilias; Joerger, Andreas C; Whitby, Richard J; Goldup, Stephen M; Wells, Neil; Langley, Graham J; Herniman, Julie M; Baud, Matthias G J

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

p53家族DNA结合域的进化史:来自庞贝古菌同源物的启示

Zhang, Qiang; Balourdas, Dimitrios-Ilias; Baron, Bruno; Senitzki, Alon; Haran, Tali E; Wiman, Klas G; Soussi, Thierry; Joerger, Andreas C

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

发现具有纳摩尔级亲和力的药理学伴侣蛋白,可稳定致癌性p53突变体Y220C

Stephenson Clarke, Joseph R; Douglas, Leon R; Duriez, Patrick J; Balourdas, Dimitrios-Ilias; Joerger, Andreas C; Khadiullina, Raniya; Bulatov, Emil; Baud, Matthias G J

Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinoma

双重 BET/HDAC 抑制剂治疗胰腺导管腺癌的表征

Xin Zhang, Tim Zegar, Tim Weiser, Feda H Hamdan, Benedict-Tilman Berger, Romain Lucas, Dimitrios-IIias Balourdas, Swetlana Ladigan, Phyllis F Cheung, Sven-Thorsten Liffers, Marija Trajkovic-Arsic, Bjoern Scheffler, Andreas C Joerger, Stephan A Hahn, Steven A Johnsen, Stefan Knapp, Jens T Siveke