Results 201 to 210 of about 504,672 (298)

A FAP‐Targeted SMDC Platform Enables Synergistic Radionuclide–Chemotherapy with PET‐Guided Evaluation

Advanced Science, EarlyView.
A fibroblast activation protein (FAP)‐targeted small molecule–drug conjugate (SMDC) platform is developed to integrate PET imaging with synergistic radionuclide–chemotherapy. Linker chemistry governs stability, exposure, and tolerability, with the VC linker providing superior in vivo performance.
Ruitao Yang, Hongxin Li, Zexin Xu, Baocheng Chen, Ningjie Li, Yuhua Zhong, Kongzhen Hu   +6 more
wiley   +1 more source

Alkyl gallates disrupt Trypanosoma brucei lipid droplets. [PDF]

PLoS One
Amisigo CM, Amegatcher G, Sunter JD, Gwira TM.   +3 more
europepmc   +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

Inhibition of Focal Adhesion Restricts Chemoresistance in Pancreatic Cancer by Targeting SLC7A11 Mediated Ferroptosis

Advanced Science, EarlyView.
FAK signaling drives chemoresistance and tumor evolution in pancreatic ductal adenocarcinoma. The FAK inhibitor IN10018 restores gemcitabine sensitivity by inducing SLC7A11‐mediated ferroptosis through the PI3K‐Akt pathway and remodeling the tumor microenvironment, reducing mesenchymal components while enhancing CD8+ T‐cell infiltration in preclinical ...
Yingjin Wang, Hui Yang, Baoyuan Zhang, Yongsu Ma, Kuangen Zhang, Peng Wang, Jiapeng Yang, Zaiqi Wang, Rong Liu, Xiaodong Tian, Ning Zhang, Yinmo Yang   +11 more
wiley   +1 more source

Ferulic and <i>p</i>-coumaric acid derivatives as dual EGFR-VEGFR2 inhibitors: design, semi-synthesis, and biological investigations. [PDF]

RSC Adv
Elrayess R, Nafie MS, Ahmed SA, Alkazzaz YK, Darwish KM, Gad El-Hak HN, Eltamany EE.   +6 more
europepmc   +1 more source

ANXA2‐mediated Phagocytosis Generates AR+ Macrophages to Confer Enzalutamide Resistance in Prostate Cancer

Advanced Science, EarlyView.
A novel resistance mechanism is mediated through phagocytosis of cancer cells by AR+ TAMs. This process, dependent on ANXA2, enables macrophages to acquire AR protein from engulfed tumor cells. The internalized AR translocates into the macrophage nucleus, where it binds directly to the IL‐6 promoter, augmenting IL‐6 transcription and secretion ...
Yong Luo, Tianlong Luo, Lingfeng Li, Qi Sun, Dongquan Li, Shanhe Huang, Zonglin Li, Weilong Lin, Yuan Ou, Tao Du, Shengmeng Peng, Kewei Xu, Bisheng Cheng, Hai Huang   +13 more
wiley   +1 more source

Medicinal attributes of nitrogen heterocycles directing aldose reductase selectivity and potency. [PDF]

RSC Med Chem
Kumari A, Manna SK, Rani K, Kohal R, Gupta GD, Verma SK.   +5 more
europepmc   +1 more source

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

Binding properties of marine sulfated glycans to coagulation (co)-factors using surface plasmon resonance spectroscopy. [PDF]

Sci Rep
Al Ahmed H, Pomin VH.
europepmc   +1 more source