Discovery and evaluation of SIPI11594: a novel mitochondrial pyruvate carrier inhibitor with anti-hair loss efficacy [0.03%]
SIPI11594的发现及评价：一种治疗脱发的新颖线粒体丙酮酸载体抑制剂
Han Zhang,Xingyu Wu,Yilei Huang et al.
Han Zhang et al.
Inhibition of the mitochondrial pyruvate carrier (MPC) is a promising strategy to promote hair follicle stem cell activation via lactate production for treating alopecia. To identify new MPC inhibitors, we designed and synthesized 32 novel ...
Discovery of a novel covalent allosteric site CYS434 in Keap1 and its ligand for the treatment of acute lung injury [0.03%]
凯因1新型共价别构位点半胱氨酸434的发现及其配体在治疗急性肺损伤中的应用
Ying Shi,Xin Tie,Guojing Tao et al.
Ying Shi et al.
Keap1 is a central negative regulator of the Nrf2 antioxidant pathway, yet its covalent allosteric modulation remains incompletely understood. Here, we provide evidence that Cys434 may represent a previously unrecognized covalent allosteric...
Evaluation of the meroterpenoids callistrilone O, E and their epimers as potent antiausterity agents [0.03%]
评估紫穗槐松二醇O、E及其差向异构体作为强力抗吝啬剂的效果
Kensuke Okuda,Akira Takagi
Kensuke Okuda
This structure activity relationship study reports the synthesis and evaluation of the meroterpenoids callistrilone O, E, their epimers at the 4-benzylic position, and their pentacyclic precursors as antiausterity agents to starvation-toler...
An HOCl-activated chemiluminescent prodrug enabling self-reporting camptothecin release and imaging-guided therapy in peritoneal metastasis [0.03%]
一种激活HOCl的化学发光前药，可在腹膜转移中自报告喜树碱释放和影像引导治疗
Yanhan Zhou,Hongchao Wang,Maocheng Yang et al.
Yanhan Zhou et al.
Prodrug strategies that exploit tumor-microenvironment abnormalities can enable spatiotemporally controlled chemotherapy; however, most prodrugs are intrinsically silent and cannot report their activation in vivo. We designed and synthesize...
O4-Modified thymidine analogues with photolabile o-nitrobenzyl group derivatives for modulating polymerase primer extension reaction [0.03%]
一种用于调节聚合酶引物延伸反应的含光解o-硝基苄基衍生物的O4-修饰胸腺嘧啶类似物
Ritsuki Sugiura,Hidenori Okamura,Naohiro Yonezawa et al.
Ritsuki Sugiura et al.
Photocaging has emerged as a robust and versatile strategy for achieving precise spatiotemporal control of complex biological processes through UV-induced photoactivation. Here, we sought to develop molecules that allow highly controlled mo...
Design and therapeutic landscape of copper ionophores: From coordination chemistry to cuproptosis modulation [0.03%]
铜离子载体的设计与治疗景观：从配位化学到杯硫调控
Hongmin Zhang,Jiali Xu,Chonglu Li et al.
Hongmin Zhang et al.
Copper ionophores have evolved from serendipitous discoveries into rationally designed therapeutics following the elucidation of cuproptosis. This review analyzes the core design principles that govern ionophore functions, focusing on the d...
New high affinity AT2 receptor ligands comprising a 2-methyl substituted phenylthiophene scaffold [0.03%]
一类新型高亲和力AT2受体配基化合物及其作为生长素受体激动剂的应用权利要求书说明书摘要说明书附图说明书扉页说明书目录说明书实施例说明书ClaimsDescriptionDrawingsCoverSheet说明书AbstractTableofContentsSpecificationExamples
Johan Gising,Johan Wannberg,Rebecka Isaksson et al.
Johan Gising et al.
A series of 2-substituted methylene imidazolephenylthiophene and tert-butylimidazolyl acetylphenylthiophene sulfonylcarbamate and sulfonamide derivatives were synthesized and assessed as AT2R ligands. Substitution at this position of the ph...
Edeildo Ferreira da Silva-Júnior
Edeildo Ferreira da Silva-Júnior
Endosomal escape and cytosolic delivery of cell-penetrating peptide conjugates [0.03%]
内体逃逸和细胞穿透肽缀合物的胞质递送
Kathryn J Fincham,Cameron J Nowell,Macgregor A Matthews et al.
Kathryn J Fincham et al.
Cell-penetrating peptides (CPPs) are sequences designed to enhance the cytosolic delivery of a range of cargoes. We are interested in delivering peptides containing the sequence DINNN, which are high-affinity inhibitors of the interaction b...
SHP2-targeted cancer therapeutics: Structural insights, inhibitor development and emerging modalities [0.03%]
SHP2靶向抗癌疗法：结构洞察、抑制剂开发及新兴模式
Yang Zhang,Chengchun Zhu,Chaojin Si et al.
Yang Zhang et al.
Src homology 2 domain-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a ubiquitously expressed non-receptor protein tyrosine phosphatase that functions as a central signaling hub in multiple oncogenic pathwa...