Results 91 to 100 of about 988,006 (285)

Compound-target network of ELP.

, 2022
In the network, there are 167 nodes and 292 edges. 22 potential bioactive compounds have interactions with 145 protein targets. The red circles represent the bioactive compounds, and the blue squares represent the targets.
Yi Zhang (9093), Chuan Liu (367528), Ya Tu (10836785), Jinsong Su (12055152), Fangfang Fan (312738), Lu Zhong (5277710)   +5 more
core   +1 more source

A New Recruitable E3 Ligase UHRF1 Supporting Targeted Protein Degradation: A Minimal Azide as a Recruitment Ligand

Advanced Science, EarlyView.
Targeted protein degradation is often limited by the scarcity of usable E3 ligases. Herein, we report the first small‐molecule GPX4 degraders that incorporate either electrophilic warheads or a minimal azide group as an E3 recruitment ligand. The azide‐based degrader DK‐5070 effectively drives potent GPX4 degradation; mechanistic studies reveal that ...
Zehong Lin, Kang Duan, Rui Wan, Tao Jiang, Jinzhe Wei, Miao Sun, Mariia A. Skryl'nikova, Maxim A. Gureev, Zhi‐Min Zhang, Zhang Zhang, Ke Ding, Nan Ma, Tongzheng Liu, Yi Tan, Zhengqiu Li   +14 more
wiley   +1 more source

Photoactivated Platinum Complexes: Targeting Membrane Proteins and Organelles for Precision Cancer Therapy

Angewandte Chemie, EarlyView.
This review highlights an emerging anticancer approach integrating platinum agents into photodynamic therapy (PDT) and photoactivated chemotherapy (PACT) systems, further augmented by cancer cell membrane‐ and organelle‐targeting. By directing photoactivated platinum complexes from nontargeted distribution to cancer cells or defined subcellular sites ...
Shu Chen, Qiyuan Zhou, Jiaqian Xu, Guangyu Zhu   +3 more
wiley   +2 more sources

Enantioselective Access to Trifluoromethylated Spirocyclopropyl Heterocycles

Advanced Science, EarlyView.
We report a rhodium‐catalyzed asymmetric [2+1] spirocyclopropanation of methylene azacycles with trifluoromethyl carbenes in situ derived from fluoroalkyl triftosylhydrazones. ABSTRACT Chiral spirocyclopropyl heterocycles have emerged as privileged three‐dimensional structural motifs in medicinal chemistry.
Yuanhao Zhu, Youzhi Xu, Weitao Zhang, Yongyue Ning, Yaojia Jiang, Yongquan Ning, Genping Huang, Jiawei Cheng, Paramasivam Sivaguru, Xihe Bi   +9 more
wiley   +1 more source

Polyproline: A Synthetic Polypeptide With Unique Properties

Angewandte Chemie, EarlyView.
Poly‐L‐proline is a unique polypeptide distinguished by its well‐defined secondary structures and unusual thermal behavior. This mini review highlights recent advances in the synthesis of poly‐L‐proline by N‐carboxyanhydride (NCA) polymerization, the formation of structurally defined architectures and nanostructures, and emerging strategies that ...
Rosanna Le Scouarnec, Josué M. Galindo, Colin Bonduelle, Andreas Heise   +3 more
wiley   +2 more sources

A Brief Review of Machine Learning-Based Bioactive Compound Research

, 2022
Bioactive compounds are often used as initial substances for many therapeutic agents. In recent years, both theoretical and practical innovations in hardware-assisted and fast-evolving machine learning (ML) have made it possible to identify desired ...
Hoo Hyun Kim, Keunsoo Kang, Bo Ram Beck, Sangbum Lee, Jihye Park   +4 more
core   +1 more source

AS‐TLC‐Based High‐Throughput Screening Integrated with CuAAC Optimization Strategy Facilitates the Rapid Discovery of YTHDC1 Inhibitor

Advanced Science, EarlyView.
We developed Affinity Selection Thin‐Layer Chromatography (AS‐TLC) as a method for high‐throughput screening (HTS) of compound mixtures. Furthermore, we integrated activity assays with AS‐TLC and identified a YTH domain‐containing protein 1 (YTHDC1) inhibitor. Building on this hit, we applied copper(I)‐catalyzed azide–alkyne cycloaddition (CuAAC) click
Mingchen Wang, Shuiping Fu, Ye Xu, Jia Gao, Jiwei Ren, Xu Yang, Hesong Xu, Ge Sun, Yanjie Li, Yanlin Wang, Lu Jin, Peijuan Chen, Ying Xu, Jianhao Li, Hua Lin, Chujiao Hu, Kaixian Chen, Huan Xiong, Cheng Luo, Shijie Chen   +19 more
wiley   +1 more source

Computational and experimental insights into the interaction of the seaweed-derived steroidal metabolite 11α-hydroxyprogesterone with the glucocorticoid receptor

Computational and Structural Biotechnology Journal
Seaweed-derived metabolites offer a rich source of bioactive compounds with therapeutic potential. In this study, 112 steroidal metabolites from Sargassum polycystum, Gracilaria fisheri, and Caulerpa lentillifera were computationally screened to identify
Supatchar Sermsakulwat, Phuphiphat Jaikaew, Tiwtawat Napiroon, Worawat Surarit, Thrissawan Traijitt, Theppanya Charoenrat, Bodee Nutho, Arachaporn Thong-olran, Supenya Chittapun   +8 more
doaj   +1 more source

Mesenchymal Stromal Cell‐Based Cell–Drug Conjugates for the Treatment of Acute Liver Failure

Advanced Science, EarlyView.
Mesenchymal stromal cell (MSC)‐based cell‐drug conjugates are constructed by anchoring rosiglitazone‐loaded nanoparticles onto the MSC surface. Sustained rosiglitazone release enhances MSC proliferation and paracrine activity while promoting anti‐inflammatory macrophage polarization.
Tenghui Ye, Jiamin Wu, Zixin Wu, Xi Liu, Jiajia Luo, Leyi Yang, Peng Shi   +6 more
wiley   +1 more source

Broad‐Spectrum, Cell Envelope‐Active Marinocyclin Antibiotics From a Coral‐Derived Bacterium Are Effective Against Colistin‐Resistant Bacteria

Angewandte Chemie, EarlyView.
Marinocyclins, polycationic macrocyclic depsipeptides, were discovered by genome mining from the marine coral‐derived bacterium Aquimarina megaterium. The compounds have broad‐spectrum activity against gram‐positive and gram‐negative ESKAPE bacteria.
Clara Chepkirui, Sandra Silva, Jan Straetener, Chandrashekhar Padhi, Tina Keller‐Costa, Tess Lamer, Laura Reinke, Heike Brötz‐Oesterhelt, Rodrigo Costa, Jörn Piel   +9 more
wiley   +2 more sources