Results 181 to 190 of about 827,025 (271)

Proteolysis Targeting Chimera (PROTAC) Linkerology Enhances the CDK-Degradation Selectivity Profile of a Multi-CDK Inhibitor: Discovery of Potent, Anti-Leukemic CDK9 Degraders. [PDF]

ACS Pharmacol Transl Sci
Chan AM, Eberly C, Goodis CC, Nordquist EB, Weldemariam M, Carter-Cooper BA, Pogash S, Lapidus R, Kane MA, MacKerell AD, Civin CI, Fletcher S.   +11 more
europepmc   +1 more source

Synthesis and Activity‐Based Protein Profiling Identifies Aldo‐Keto Reductase 1C3 as Target Protein of Myxoglucamides

Angewandte Chemie International Edition, Volume 65, Issue 41, 5 October 2026.
Myxoglucamide A—a novel glycolipopeptide isolated from myxobacteria—was synthesized, and activity‐based protein profiling identified aldo‐keto reductase 1C3 (AKR1C3) as its main target in human cells. Structure‐activity relationship studies, together with biophysical characterization and X‐ray crystallography, elucidated the structural basis of AKR1C3 ...
Thomas Siemon, Vivek K. Mishra, Mingming Zhao, Konrad Büssow, Alexander Popoff, Chengzhang Fu, Rolf Müller, Lothar Jänsch, Wulf Blankenfeldt, Mark Brönstrup   +9 more
wiley   +1 more source

Correction to 'Proteolysis Targeting Chimera Loaded Extracellular Vesicles for Developing Triple Negative Breast Cancer Treatment'. [PDF]

J Extracell Vesicles
europepmc   +1 more source

Arginine methylation as a regulatory ratchet in cancer: From substrate selection to malignant‐state stabilization

Molecular Oncology, Volume 20, Issue 10, Page 2466-2489, October 2026.
Arginine methylation can be viewed as a persistence‐prone post‐translational modification regulated by a network of PRMTs. Competitive and compensatory interactions among PRMTs can redistribute methylation across substrate pools shaped by sequence, structural, spatial, and environmental layers, reinforcing RNA‐processing, chromatin, and signaling ...
So Hyun Kwon, Ji Min Lee
wiley   +1 more source

Targeted Degradation of STING by a Neutrophil Membrane‐Coated Nanoplatform Suppresses Microglial Pyroptosis After Subarachnoid Hemorrhage

Advanced Science, Volume 13, Issue 55, 5 October 2026.
MG1@NM‐Px serves as a microglia‐targeted STING‐degrading nanoplatform for subarachnoid hemorrhage. Following systemic administration, it crosses the blood–brain barrier and accumulates in activated microglia. STP1‐mediated STING ubiquitination and degradation suppress MAPK/inflammasome signaling, GSDME‐mediated pyroptosis, and IL‐1β release, revealing ...
Ruotian Zhang, Kaikun Yuan, Haoyu Zou, Hanfeng Qin, Jiale Liu, Jianda Sun, Feifan Zhang, Yuankui Wang, Tong Wang, Jiaxing Dai, Chunxu Li, Yichi Chen, Yingfeng Tu, Huaizhang Shi   +13 more
wiley   +1 more source

Correction to "Proteolysis-targeting chimera (PROTAC): current applications and future directions". [PDF]

MedComm (2020)
europepmc   +1 more source

Cell‐Selective Delivery of RIBOTACs via an Anti‐EGFR Nanobody for Pancreatic Cancer Treatment

Advanced Science, Volume 13, Issue 55, 5 October 2026.
This study introduces an innovative strategy for the tumor‐selective catalytic degradation of oncogenic non‐coding RNA by interfacing a ribonuclease‐recruiting small molecule (RIBOTAC) with an EGFR‐targeting nanobody via a CTSB (Cathepsin B)‐responsive linker.
Tianli Luo, Yijuan Wang, Dengwang Chen, Yinghan Zhang, Yi Shuai, Hualiang Yao, Tao Jiang, Hang Jiang, Ming Zhong, Xiangeng Wang, Ziwei Wang, Chenchen Xu, Ajay Goel, Hoi Tang MA, Feng Gao, Xin Wang   +15 more
wiley   +1 more source

DNA-Templated Spatially Controlled Proteolysis Targeting Chimera for Cyclin D1-CDK4/6 Complex Protein Degradation. [PDF]

J Am Chem Soc
Zheng R, Prasad A, Satyabola D, Xu Y, Roy S, Yan Y, Šulc P, Yan H.   +7 more
europepmc   +1 more source

Imine Reductase‐Mediated Regio‐ and Stereoselective Reductive Amination of Diamines

ChemCatChem, Volume 18, Issue 19, 14 October 2026.
Imine reductases (IREDs) have been employed as biocatalysts for the regioselective modification of diamines via reductive amination. The use of racemic diamines resulted in both regio‐ and enantio‐selective reductive amination via kinetic resolution. The application of this methodology has been demonstrated on a preparative scale by the synthesis of a ...
Arnau Rué Casamajo, Yuqi Yu, Lucian Pirvu, Christian Schnepel, Simon J. Charnock, Francesco Falcioni, Martin A. Hayes, Nicholas J. Turner   +7 more
wiley   +1 more source

Identification of a Proteolysis-Targeting-Chimera that Addresses Activated Checkpoint Kinase-1 Reveals its Non-Catalytic Functions in Tumor Cells. [PDF]

Angew Chem Int Ed Engl
Ashry R, Abdelsalam M, Hausen J, Hieber C, Zeyn Y, Sarnow AC, Schmidt M, Najafi S, Oehme I, Bros M, Chen JX, Dejung M, Sippl W, Krämer OH.   +13 more
europepmc   +1 more source