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

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor

对 KRAS 上 Switch II 口袋的可逆结合进行片段优化,可产生有效的体内活性 KRASG12C 抑制剂

Joachim Bröker, Alex G Waterson, Chris Smethurst, Dirk Kessler, Jark Böttcher, Moriz Mayer, Gerhard Gmaschitz, Jason Phan, Andrew Little, Jason R Abbott, Qi Sun, Michael Gmachl, Dorothea Rudolph, Heribert Arnhof, Klaus Rumpel, Fabio Savarese, Thomas Gerstberger, Nikolai Mischerikow, Matthias Treu, L

Synthesis of MDM2-p53 Inhibitor BI-0282 via a Dipolar Cycloaddition and Late-Stage Davis-Beirut Reaction

通过偶极环加成和后期 Davis-Beirut 反应合成 MDM2-p53 抑制剂 BI-0282

Juergen Ramharter, Michael Kulhanek, Maike Dettling, Gerhard Gmaschitz, Jale Karolyi-Oezguer, Harald Weinstabl, Andreas Gollner

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

通过基于结构的 PROTAC 设计证明癌症中的 BAF 复合物脆弱性

William Farnaby, Manfred Koegl, Michael J Roy, Claire Whitworth, Emelyne Diers, Nicole Trainor, David Zollman, Steffen Steurer, Jale Karolyi-Oezguer, Carina Riedmueller, Teresa Gmaschitz, Johannes Wachter, Christian Dank, Michael Galant, Bernadette Sharps, Klaus Rumpel, Elisabeth Traxler, Thomas Ger

Drugging an undruggable pocket on KRAS

对 KRAS 上的一个无法用药的口袋进行药物治疗

Kessler, Dirk; Gmachl, Michael; Mantoulidis, Andreas; Martin, Laetitia J; Zoephel, Andreas; Mayer, Moriz; Gollner, Andreas; Covini, David; Fischer, Silke; Gerstberger, Thomas; Gmaschitz, Teresa; Goodwin, Craig; Greb, Peter; Häring, Daniela; Hela, Wolfgang; Hoffmann, Johann; Karolyi-Oezguer, Jale; Knesl, Petr; Kornigg, Stefan; Koegl, Manfred; Kousek, Roland; Lamarre, Lyne; Moser, Franziska; Munico-Martinez, Silvia; Peinsipp, Christoph; Phan, Jason; Rinnenthal, Jörg; Sai, Jiqing; Salamon, Christian; Scherbantin, Yvonne; Schipany, Katharina; Schnitzer, Renate; Schrenk, Andreas; Sharps, Bernadette; Siszler, Gabriella; Sun, Qi; Waterson, Alex; Wolkerstorfer, Bernhard; Zeeb, Markus; Pearson, Mark; Fesik, Stephen W; McConnell, Darryl B

Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions

高度选择性 PTK2 蛋白水解靶向嵌合体以探测粘着斑激酶支架功能

Johannes Popow, Heribert Arnhof, Gerd Bader, Helmut Berger, Alessio Ciulli, David Covini, Christian Dank, Teresa Gmaschitz, Peter Greb, Jale Karolyi-Özguer, Manfred Koegl, Darryl B McConnell, Mark Pearson, Maria Rieger, Joerg Rinnenthal, Vanessa Roessler, Andreas Schrenk, Markus Spina, Steffen Steur

Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

通过对初始无活性蛋白水解靶向嵌合体(PROTACs)进行迭代设计和优化,鉴定出VZ185是一种高效、快速且选择性的基于von Hippel-Lindau(VHL)的BRD9和BRD7双重降解探针。

Vittoria Zoppi ,Scott J Hughes ,Chiara Maniaci ,Andrea Testa ,Teresa Gmaschitz ,Corinna Wieshofer ,Manfred Koegl ,Kristin M Riching ,Danette L Daniels ,Andrea Spallarossa ,Alessio Ciulli

Targeted Synthesis of Complex Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2-p53 Inhibitors

通过亚胺叶立德的分子内环化靶向合成复杂的螺[3H-吲哚-3,2'-吡咯烷]-2(1H)-酮:高效的MDM2-p53抑制剂

Gollner, Andreas; Weinstabl, Harald; Fuchs, Julian E; Rudolph, Dorothea; Garavel, Geraldine; Hofbauer, Karin S; Karolyi-Oezguer, Jale; Gmaschitz, Gerhard; Hela, Wolfgang; Kerres, Nina; Grondal, Elisabeth; Werni, Patrick; Ramharter, Juergen; Broeker, Joachim; McConnell, Darryl B