Results 141 to 150 of about 288,159 (307)

Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

Advanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng, Peipei Wang, Pengfei Wang, Jiamin Wang, Baiyang Li, Daqing Fang, Jian He, Xiaobei Hu, Weijuan Kan, Yubo Zhou, Chunpu Li, Jia Li, Hong Liu   +12 more
wiley   +1 more source

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

Neuronal in vitro activity is more sensitive to valproate than intracellular ATP: Considerations on conversion problems of IC50 in vitro data for animal replacement

, 2016
Matthias Nissen, Sebastian Buehler, Marco Stubbe, Jan Gimsa   +3 more
openalex   +1 more source

A Cationic Supramolecule With Potent Antifungal Activity, Single‐Species Selectivity, and Strong Synergy With Echinocandins

Advanced Science, EarlyView.
We introduce a new membrane‐active antifungal design, Gua‐SMACS‐16, that exhibits high potency and single‐species selectivity for C. tropicalis while sparing other close species in the Candida genus. Moreover, when combining with caspofungin, a clinical antifungal drug inhibiting 1,3‐β‐glucan synthase, they exhibit ultra‐strong synergy across a panel ...
Tianjiao Dai, Adrielle Xianwen Chen, Eve Wai Ling Chow, Li Mei Pang, Jianguo Li, Chandra Shekhar Verma, Stefan H. Oehlers, Yue Wang, Ning Li   +8 more
wiley   +1 more source

Therapeutic Potential of Tetrandrine Compared to Temozolomide in Treating Glioblastoma Multiforme Under Normoxic and Hypoxic Conditions. [PDF]

Int J Mol Sci
Khamis MA, Abdo D, Mohamed FG, Emara M.
europepmc   +1 more source

CD44‐Targeting Hydroxyapatite Nanoparticles (HAP) Induce Mitochondrial Dysfunction‐Driven PANoptosis and Immunogenic Cell Death (ICD) via Ca Overload in Colorectal Cancer

Advanced Science, EarlyView.
ABSTRACT Colorectal cancer (CRC) remains therapeutically challenging due to high metastasis, recurrence, and immunotherapy resistance driven by tumor microenvironment‐mediated immune evasion. Immunogenic cell death (ICD) offers a promising strategy to reshape the immune microenvironment, yet existing ICD inducers suffer from poor targeting efficiency ...
Yao Xiao, Yuxuan Yang, Haosen Qiu, Jia Yang, Hao Liang, Zhaojun Jiang, Xiao Tong, Yongying Li, Qunfeng Huang, Jiaming Wu, Tian Lin, Jiang Yu, Min Liang   +12 more
wiley   +1 more source

Anticancer Potential of Cucurbitaceae, Brassicaceae, Liliaceae and Chenopodiaceae: A Review of In Vitro Evidence. [PDF]

Molecules
Blanco-Torres EC, Rivera G, Delgado-Maldonado T, Ortiz-Pérez E, Paz-González AD, Martínez-Vázquez AV, De Luna-Santillana EJ, Ortega-Balleza JL, Vázquez-Jiménez LK.   +8 more
europepmc   +1 more source

Microbial IC50 Reference Control Result [PDF]

, 2020
openaire   +1 more source

A Catalytic Osmium Redox Couple Collapses Cancer Redox Balance

Advanced Science, EarlyView.
A stable Os(III)/Os(IV) redox couple is developed to disrupt the tumor cell redox balance by concurrently catalyzing ROS generation and GSH depletion. Osmium‐treated cells exhibit multiple cell death pathways, including apoptosis, ferroptosis, and immunogenic cell death.
Wan‐Qiong Huang, Tao Huang, Yiming Hao, Gui‐Feng Huang, Yi‐Lang Yan, Xin Fang, Ying Chen, Xiao‐Long Wei, Wai‐Lun Man, Wen‐Xiu Ni   +9 more
wiley   +1 more source

Distribution and bioactivities of tirucallane-type triterpenoids from Meliaceae family. [PDF]

Nat Prod Bioprospect
Abdullah FF, Putri SA, Najihah NA, Nurlelasari, Safriansyah W, Awang K, Supratman U.   +6 more
europepmc   +1 more source