A one-step, resin-compatible Cys-Trp cross-linking system opens a new avenue for stapled peptide therapeutics [0.03%]
一步法半胱氨酸-色氨酸交联体系促进环肽药物开发
Masaya Denda,Yutaka Kohmura,Daishiro Kobayashi et al.
Masaya Denda et al.
Protein-protein interactions (PPIs) are attractive yet challenging drug targets, motivating the development of conformationally constrained peptides such as stapled α-helices. Here we report a one-pot cysteine-tryptophan (Cys-Trp) cross-li...
Enhancing RNAi activity through 4'-O-hexadecyl-2'-deoxythymidine modification in the passenger strand [0.03%]
通过乘客链中4'-O-十六烷基-2'-脱氧胸腺嘧啶修饰增强RNAi活性
Sumit Gangopadhyay,Swrajit Nath Sharma,Gourav Das et al.
Sumit Gangopadhyay et al.
Various lipid-based siRNA drug delivery strategies are being developed for efficient delivery to extrahepatic organs. In this report, we studied the synergistic effect of 4'-O-hexadecyl-2'-dT and terminal phosphorothioate modifications on s...
Novel antiviral compounds: Synthesis, biological studies on SARS-CoV-2, and structure-activity relationship analysis [0.03%]
新型抗病毒化合物的合成、SARS-CoV-2 生物学研究及构效关系分析
Sumit Kumar,Renata Pessôa Germano Mendes,Meenakshi Bansal et al.
Sumit Kumar et al.
SARS-CoV-2 has caused a global epidemic, causing grave public health concerns. In this work, we synthesized a library of 28 compounds derived from the fusion of hydroxyethylamine and aniline and evaluated their antiviral activity. During th...
N-aryl sulfonamide inhibitors of the bacterial enzyme diaminopimelate desuccinylase (DapE) as potential new antibiotics [0.03%]
作为新型抗生素的细菌酶脱氧氨基茋酸单succinyl酶（DapE）的N-芳基磺胺抑制剂
Sebastian Flieger,Emma H Kelley,Thahani S Habeeb Mohammad et al.
Sebastian Flieger et al.
A series of N-aryl sulfonamides was designed, synthesized, and evaluated for their ability to inhibit the bacterial enzyme N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE, EC 3.5.1.18). Our initial lead compound, N-(o-methoxyphenyl)-...
Zika virus entry inhibitors [0.03%]
寨卡病毒入侵抑制剂
Weiyi Yin,Rui Zhou,Wencui Zhang et al.
Weiyi Yin et al.
Viral entry step involves of complex host-virus interactions. Research progress of viral entry inhibitors lags significantly behind that of viral replication inhibitors targeting viral non-structural proteins. Here we take Zika virus (ZIKV)...
High-throughput fragment screening identifies a new small molecule scaffold that modulates TREM2 Signaling [0.03%]
高通量片段筛选发现了一种新的小分子支架可调节TREM2信号转导
Natalie Fuchs,Farida El Gaamouch,Hossam Nada et al.
Natalie Fuchs et al.
Fragment-based drug discovery (FBDD) remains a powerful tool in drug development for targeting a wide range of proteins and identifying new small molecule-based scaffolds. Here, we explored a fragment library of 3200 compounds using a tempe...
Peptidyl keto vinyl amides as improved inhibitors of cathepsin L [0.03%]
猫尿肽L的抑制剂茋衍生物及其药学上可接受的盐和酯类及包含其的药物组合物
Adrián Fernández-de-la-Pradilla,Clara Quílez,Tadej Uršič et al.
Adrián Fernández-de-la-Pradilla et al.
Cysteine protease cathepsin L (CatL) is linked to cancer, infection, and neurodegeneration, rendering it a compelling target for therapy. Expanding upon dipeptidyl enoates (keto vinyl esters, KVE), we introduce dipeptidyl keto vinyl amides ...
Discovery of 6-substituted indole and tetrahydroquinoline derivatives as selective HDAC8 inhibitors [0.03%]
一类6位取代的色胺和四氢异喹啉衍生物HDAC8选择性抑制剂的发现
Wen Li,Ruixue Cheng,Yingjie Chang et al.
Wen Li et al.
The pursuit of isoform-selective histone deacetylase (HDAC) inhibitors is a promising strategy to overcome the adverse effects associated with pan-HDAC inhibitors. Through systematic structural modification of the known inhibitor PCI-34051,...
Fragment merging design, synthesis, and biological evaluation of novel methyl Selanyl- And thiazolidinedione-based hybrids as potent anticancer inducing apoptosis and cell cycle arrest [0.03%]
一类新型的甲基硒亚基和噻唑烷二酮片段拼合抗肿瘤化合物的设计、合成及生物活性评价研究
Saad Shaaban,Samia S Hawas,Ayman Abo Elmaaty et al.
Saad Shaaban et al.
A novel series of methyl selanyl- and 2,4-thiazolidinedione-based hybrids (HB68-HB167) was rationally designed using a fragment-merging strategy, in which key pharmacophoric elements were combined to generate structurally integrated hybrid ...
Design, synthesis and biological evaluation of novel ursolic acid derivatives as potent anti-pancreatic cancer agents [0.03%]
设计、合成及生物活性评价新型熊果酸衍生物作为抗胰腺癌剂
Tharcisse Gatera,Yi-Dan Zheng,Jia-Rong Liu et al.
Tharcisse Gatera et al.
Pancreatic cancer is a highly lethal malignancy with an urgent need for novel therapeutic strategies. Triterpenoids represent key scaffolds, with compelling anticancer potential, yet further structural optimization is required to enhance th...