Results 131 to 140 of about 7,774 (200)

Histone deacetylase inhibitors as venetoclax‐sensitising partners in acute myeloid leukaemia: Mechanisms, pharmacology and translational perspectives

British Journal of Pharmacology, Volume 183, Issue 21, Page 6261-6290, November 2026.
Abstract Venetoclax combined with hypomethylating agents has improved treatment for older or unfit patients with acute myeloid leukaemia (AML), but resistance and relapse remain common. This review analyses the rationale for combining venetoclax with inhibitors of histone deacetylase (HDAC).
Jaebok Lee, Marc Diederich
wiley   +1 more source

Correction to "DNA-Programmable Protein Degradation: Dynamic Control of Proteolysis-Targeting Chimera Activity via DNA Hybridization and Strand Displacement". [PDF]

JACS Au
Kashyap D, Haider S, Milne TA, Booth MJ.
europepmc   +1 more source

Limiting Trial‐and‐Error: Linker‐Based 2D Descriptor Analysis to Support Very Early Proteolysis‐Targeting Chimeras Design

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
Can simple linker descriptors guide PROTAC design? Analysis of matched CRBN‐ and VHL‐recruiting degraders shows that basic 2D linker properties may capture trends linked to degradation efficiency, in vitro ADME and physicochemical properties. A practical approach to reduce trial‐and‐error in early targeted protein degradation programs. Targeted protein
Giulia Apprato, Serena Traversa, Giulia Caron, Giuseppe Ermondi   +3 more
wiley   +1 more source

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

Telomerase reverse transcriptase degradation via a rationally designed covalent proteolysis targeting chimera. [PDF]

Bioorg Med Chem Lett
Frost GB, Liu Y, Kron SJ, Scheidt KA.
europepmc   +1 more source