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

Covalent Targeting Leads to the Development of a LIMK1 Isoform-Selective Inhibitor

共价靶向导致LIMK1亚型选择性抑制剂的开发

Sebastian Mandel ,Thomas Hanke ,Niall Prendiville ,María Baena-Nuevo ,Lena Marie Berger ,Frederic Farges ,Martin Peter Schwalm ,Benedict-Tilman Berger ,Andreas Kraemer ,Lewis Elson ,Hayuningbudi Saraswati ,Kamal R Abdul Azeez ,Verena Dederer ,Sebastian Mathea ,Ana Corrionero ,Patricia Alfonso ,Sabrina Keller ,Matthias Gstaiger ,Daniela S Krause ,Susanne Müller ,Sandra Röhm ,Stefan Knapp

Un-LOK-ing a New Approach for Conformational Selective Targeting of STK10 (LOK)

针对 STK10 (LOK) 构象选择性靶向的新方法——解构 LOK

Dettenhöfer, Martina; Tandara, Laura Nadine; Amrhein, Jennifer Alisa; Kurz, Christian Georg; Schwalm, Martin Peter; Mensing, Theresa Elisabeth; Wahl, Laurenz Maximilian; Krämer, Andreas; Gerninghaus, Joshua; Lenz, Christopher; Elson, Lewis; Berger, Benedict-Tilman; Schröder, Martin; Saxena, Krishna; Müller, Susanne; Knapp, Stefan; Greco, Francesco Aleksy; Hanke, Thomas

Repurposing of the RIPK1-Selective Benzo[1,4]oxazepin-4-one Scaffold for the Development of a Type III LIMK1/2 Inhibitor.

RIPK1 选择性苯并[1,4]氧氮杂环庚酮-4-酮骨架的再利用,用于开发 III 型 LIMK1/2 抑制剂

Mandel Sebastian, Hanke Thomas, Mathea Sebastian, Chatterjee Deep, Saraswati Hayuningbudi, Berger Benedict-Tilman, Schwalm Martin Peter, Yamamoto Satoshi, Tawada Michiko, Takagi Terufumi, Ahmed Mahmood, Röhm Sandra, Corrionero Ana, Alfonso Patricia, Baena Maria, Elson Lewis, Menge Amelie, Krämer Andreas, Pereira Raquel, Müller Susanne, Krause Daniela S, Knapp Stefan

Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.

2-氨基嘧啶基大环化合物的后口袋优化可得到强效的EPHA2/GAK激酶抑制剂

Gerninghaus Joshua, Zhubi Rezart, Krämer Andreas, Karim Marwah, Tran Do Hoang Nhu, Joerger Andreas C, Schreiber Christian, Berger Lena M, Berger Benedict-Tilman, Ehret Theresa A L, Elson Lewis, Lenz Christopher, Saxena Krishna, Müller Susanne, Einav Shirit, Knapp Stefan, Hanke Thomas

Discovery of Carbonic Anhydrase 9 as a Novel CLEC2 Ligand in a Cellular Interactome Screen

在细胞相互作用组筛选中发现碳酸酐酶 9 作为新型 CLEC2 配体

Sebastian Hoffmann, Benedict-Tilman Berger, Liane Rosalie Lucas, Felix Schiele, John Edward Park

Splice variants of CK1α and CK1α-like: Comparative analysis of subcellular localization, kinase activity, and function in the Wnt signaling pathway

CK1α 和 CK1α 样蛋白的剪接变体:亚细胞定位、激酶活性和在 Wnt 信号通路中的功能的比较分析

Tomáš Gybeľ ,Štěpán Čada ,Darja Klementová ,Martin P Schwalm ,Benedict-Tilman Berger ,Marek Šebesta ,Stefan Knapp ,Vítězslav Bryja

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

Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent dual EPHA2/GAK kinase inhibitors with antiviral activity

对 2-氨基嘧啶大环化合物进行后袋优化,可得到具有抗病毒活性的强效双重 EPHA2/GAK 激酶抑制剂

Joshua Gerninghaus, Rezart Zhubi, Andreas Krämer, Marwah Karim, Do Hoang Nhu Tran, Andreas C Joerger, Christian Schreiber, Lena M Berger, Benedict-Tilman Berger, Theresa A L Ehret, Lewis Elson, Christopher Lenz, Krishna Saxena, Susanne Müller, Shirit Einav, Stefan Knapp, Thomas Hanke

MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core

MSC-1186,一种基于特殊修饰的苯并咪唑-嘧啶核心的高选择性 Pan-SRPK 抑制剂

Martin Schröder, Matthias Leiendecker, Ulrich Grädler, Juliane Braun, Andreas Blum, Marek Wanior, Benedict-Tilman Berger, Andreas Krämer, Susanne Müller, Christina Esdar, Stefan Knapp, Timo Heinrich

Death by a thousand cuts through kinase inhibitor combinations that maximize selectivity and enable rational multitargeting

通过激酶抑制剂组合,最大限度地提高选择性并实现合理的多靶向治疗,从而实现千刀万剐

Ian R Outhwaite, Sukrit Singh, Benedict-Tilman Berger, Stefan Knapp, John D Chodera, Markus A Seeliger