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...
Discovery of potential covalent TYK2 inhibitors targeting Cys736 for the treatment of psoriasis [0.03%]
用于治疗银屑病的靶向半胱天冬酶736的潜在共价TYK2抑制剂的发现
Han Wang,Chang Liu,Tong Liu et al.
Han Wang et al.
TYK2 regulates the signaling of pro-inflammatory cytokines such as IL-12, IL-23, and type I interferons, which directly modulates immune cell activation and inflammatory responses, thereby has emerged as a promising therapeutic target for p...
Design and evaluation of the bactericidal activity of new hydroxamic acid and hydrazide derivatives against mature S. aureus biofilms [0.03%]
新型羟胺酸和肼衍生物的杀菌活性的设计、评价及其对成熟金黄色葡萄球菌生物被膜的作用
Maëva Corneiller,Allison Faure,Rémy Tisserand et al.
Maëva Corneiller et al.
Bacterial biofilms represent a major clinical challenge due to their high tolerance to conventional antibiotics and their implication in persistent infections. Staphylococcus aureus is particularly known for its ability to form biofilms tha...
Borneol-loaded liposomes modified with 5-hydroxy-1H-pyrazole-3-carboxylic acid enhance neuroprotection and brain specific for ischemic stroke therapy [0.03%]
负载薄荷脑的5-羟基-1H-吡唑-3-羧酸修饰脂质体增强神经保护作用并具有脑靶向性以治疗缺血性中风
Yulu Wu,Siyi Li,Ru Xiao et al.
Yulu Wu et al.
Ischemic stroke is a cardiovascular and cerebrovascular disease with high mortality and disability rates, characterized by complex pathophysiological mechanisms. In this study, 5-hydroxy-1H-pyrazole-3-carboxylic acid compound (3g) was ident...
PROTACs for central nervous system disorders: challenges and opportunities [0.03%]
蛋白降解嵌合体用于中枢神经系统疾病：挑战与机遇
Na Zheng,Jikuan Shao,Baichen Xiong et al.
Na Zheng et al.
Central nervous system (CNS) disorders, particularly neurodegenerative diseases and brain tumors, pose substantial and long-standing challenges to the global public health system. Current therapeutic approaches for CNS disorders are primari...
Efficient gram-scale synthesis and preclinical evaluation of an escin-derived therapeutic for ovarian cancer [0.03%]
高效克级合成和卵巢癌治疗的Escin衍生物药物的临床前评估
Chin Leong Wong,Tiffany Yuen Kwan Au,Chi-Shing Chan
Chin Leong Wong
Ovarian cancer is the most lethal gynecologic malignancy, characterized by a poor five-year survival rate for patients with advanced-stage disease. EV-S008, an escin derivative, exhibits potent anti-ovarian cancer activity; however, its pre...
Novel 1H-imidazo[4,5-c]quinoline derivatives as TLR-7 modulators with pro-apoptotic properties in breast cancer cell line [0.03%]
新型1h-咪唑并[4,5-c]喹啉衍生物作为tlr-7调节剂在乳腺癌细胞系中具有促凋亡特性
Katarzyna Grychowska,Olga Szewczyk-Roszczenko,Piotr Roszczenko et al.
Katarzyna Grychowska et al.
A new class of 4-chloro-substituted 1H-imidazo[4,5-c]quinoline derivatives was identified as functional TLR7 agonists. Molecular modeling suggests that, in selected cases, replacing the C4 amino group with chlorine does not abolish receptor...