Results 121 to 130 of about 7,362 (230)

Development of a PROTAC Targeting Chk1

A series of Chk1 degraders were designed and synthesized. The degraders were developed through the conjugation of a promiscuous kinase binder and thalidomide. One of the degraders PROTAC-2 was able to decrease Chk1 levels in a concentration-dependent manner in A375 cells.
Chowdhury, Sandipan Roy, Chuong, Patrick, Mgbemena, Victoria E., Statsyuk, Alexander   +3 more
openaire   +2 more sources

Synthesis of β‐ and γ‐Carbolinones Through a Fe(III)‐Mediated Radical 6‐Endo‐Trig Cyclization of Indole‐Based Ugi 4‐CR Adducts

European Journal of Organic Chemistry, Volume 29, Issue 38, 13 October 2026.
A practical strategy for synthesizing β‐ and γ‐carbolinones from indole‐based Ugi 4‐CR adducts through an intramolecular radical cyclization using Fe(III)–H species is presented. This approach enables the efficient synthesis of spiro‐carbolinones under mild reaction conditions and demonstrates the effectiveness of secondary radicals in both cyclization
María F. Olvera‐Granados, Luis A. Polindara‐García   +1 more
wiley   +1 more source

Synthese und aktivitätsbasierte Proteinprofilierung identifizieren die Aldo‐Keto‐Reduktase 1C3 als Zielprotein der Myxoglucamide

Angewandte Chemie, Volume 138, Issue 41, 5 October 2026.
Myxoglucamid A – ein neuartiges, aus Myxobakterien isoliertes Glykolipopeptid – wurde erstmals totalsynthetisch hergestellt. Mittels aktivitätsbasierter Proteinprofilierung (ABPP) wurde die Aldo‐Keto‐Reduktase 1C3 (AKR1C3) als primäres Zielprotein in menschlichen Zellen identifiziert.
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

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

PROTAC-Based Strategies in Neurodegenerative Diseases: Challenges and Perspectives. [PDF]

Pharmaceuticals (Basel)
Degennaro P, Ghafir El Idrissi I, Purgatorio R, Fanizzi A, Rullo M, Pisani L, Macchia E, Torsi L, Stefanachi A, Leonetti F.   +9 more
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

Pocket-PROTACs: an interpretable pocket-aware deep learning framework for predicting PROTAC-induced protein degradation. [PDF]

Bioinformatics
Chen K, Huang Z, Wang Y, Shen S, Song J, Deng L.   +5 more
europepmc   +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

Chemical tools for BAZ2A/B biology: discovery of dual and BAZ2B-selective PROTAC degraders. [PDF]

RSC Med Chem
Cheng-Sánchez I, Gosselé KA, Palaferri L, Krummhaar M, Laul E, Ciulli A, Nevado C.   +6 more
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