Results 101 to 110 of about 11,341 (256)

First Generation Proteolysis Targeting Chimeras (PROTACs) for the Treatment of Progeria

Advanced Science, EarlyView.
We report the first PROTACs designed to degrade progerin, introducing a novel therapeutic approach for progeria. The best compound, UCM‐18142, significantly reduces progerin levels and improves key disease phenotypes in patient‐derived cells and in the LmnaG609G/G609G mouse model, paving the way for new treatment strategies targeting the root cause of ...
Jon Macicior‐Michelena, Marcelino Telechea, Daniel Fernández, Alba García‐Martín, Ángeles Canales, Silvia Ortega‐Gutiérrez   +5 more
wiley   +1 more source

Boletín oficial de la provincia de León: Num. 137 (13/02/1924) [PDF]

, 1924
Copia digital. Valladolid : Junta de Castilla y León.
León (Provincia). Diputación Provincial
core   +3 more sources

Proteasome Inhibitors: Harnessing Proteostasis to Combat Disease [PDF]

, 2020
The proteasome is the central component of the main cellular protein degradation pathway. During the past four decades, the critical function of the proteasome in numerous physiological processes has been revealed, and proteasome activity has been linked
Li, Jing, Sherman, David J.
core  

Targeting STAT3 in Cancer with Nucleotide Therapeutics. [PDF]

, 2019
Signal transducer and activator of transcription 3 (STAT3) plays a critical role in promoting the proliferation and survival of tumor cells. As a ubiquitously-expressed transcription factor, STAT3 has commonly been considered an "undruggable" target for ...
Grandis, Jennifer R, Johnson, Daniel E, Lau, Yue-Ting K, Ramaiyer, Malini   +3 more
core   +2 more sources

ESCRT‐Mimetic Nanodegrader Targets STING for Anti‐Inflammatory Therapy

Advanced Science, EarlyView.
A nanoplatform‐enabled targeted protein degradation strategy is presented to regulate aberrant STING signaling. STING‐ATTEC induces selective autophagic degradation of STING via formation of a STING–ATTEC–LC3 ternary complex, while the cationic FA‐LNP+ system enhances LC3 generation and targeted delivery. Together, this synergistic approach efficiently
Fuyuan Zhou, Qiming Zhai, Zhihao Yao, Qing Li, Yan Yang, Si Wang, Chao Huang, Liangjing Xin, Tao Chen, Jinlin Song   +9 more
wiley   +1 more source

Covalent Reprogramming of Kinase Binders to Modulate Protein Abundance

Advanced Science, EarlyView.
Electrophilic remodeling of a broad‐spectrum kinase binder reveals how subtle chemical changes reprogram protein fate. An acrylamide analog of a multi‐kinase binder selectively stabilizes Aurora kinase A (AURKA) by suppressing its ubiquitination, while a short‐linker variant converts this stabilizer into a degrader.
Chen Mozes, Xiaokang Jin, Miguel A. Campos, Chen Zhou, Xiaoyu Zhang   +4 more
wiley   +1 more source

Thioamide substitution to probe the hydroxyproline recognition of VHL ligands [PDF]

, 2018
Thioamide substitution influences hydrogen bond and n→π* interactions involved in the conformational stability of protein secondary structures and oligopeptides.
Alemán, Alessio Ciulli, Bartlett, Bartlett, Bondeson, Buckley, Buckley, Bürgi, Chan, Choudhary, Choudhary, Choudhary, Culik, Engel-Andreasen, Frost, Gadd, Galdeano, Hon, Lee, Maniaci, Min, Miwa, Mukherjee, Newberry, Pedro Soares, Platts, Rahim, Reiner, Seebach, Soares, Tran, Van Molle, Walters, Wiberg, Xavier Lucas, Zengerle   +35 more
core   +2 more sources

Rational Design of Broad‐Spectrum Anti‐Enteroviral Molecular Glues Targeting Enteroviral RNAi Suppressors

Advanced Science, EarlyView.
By leveraging this homodimerization mechanism, molecular glues were rationally designed to induce dysfunctional 3A dimerization, thereby restoring antiviral RNAi. The optimal molecular glue, VTP‐32, demonstrated potent and pan‐enterovirus (groups A, B, D) antiviral effects.
Yuan Fang, Xiong Xie, Huidi Fan, Botao Wu, An Wang, Wenhao Dai, Zezhong Liu, Jian Li, Huoyan Tong, Jianan Li, Yujie Ren, Jinlin Wang, Xi Zhou, Hong Liu   +13 more
wiley   +1 more source

Phytochemicals derived from Piper longum in insect and mite pests management: A review [PDF]

, 2018
The need for the development of alternative types of selective control methods for crop protection with reduced use of chemical pesticides was the main objective of this present review article.
Rahman, S., Sharmah, A. Khound, Sharmah, D.   +2 more
core   +2 more sources

Revisiting Target‐Aware de novo Molecular Generation with TarPass: Between Rational Design and Texas Sharpshooter

Advanced Science, EarlyView.
TarPass provides a rigorous benchmark for target‐aware de novo molecular generation by jointly evaluating protein‐ligand interactions, molecular plausibility, and drug‐likeness on 18 well‐studied targets. Results show that current models often fail to consistently surpass random baseline in target‐specific enrichment, while post hoc multi‐tier virtual ...
Rui Qin, Zijie Chen, Yurong Li, Meijing Fang, Longji Shen, Yilong Su, Odin Zhang, Qinghan Wang, Qun Su, Jike Wang, Tingjun Hou, Yu Kang   +11 more
wiley   +1 more source