Exploration and optimization of indole derivatives as novel anti-HBV agent with potential TLR7-agonistic effect [0.03%]
作为新型抗HBV化合物的吲哚衍生物的探索和优化及其潜在TLR7激动剂效应研究
Lihua Yang,Zibin Qiu,Xincheng Li et al.
Lihua Yang et al.
Hepatitis B virus (HBV) remains a major worldwide health challenge, with disease progression being closely associated with host immune dysregulation, and limited by the resistance of the current anti-HBV drugs. In this study, twenty-six ind...
Discovery of novel 1,2,4-triazoles derivatives acting as NF1 activators against cervical cancer [0.03%]
作为宫颈癌NF1激活剂的新型1,2,4-三唑衍生物的发现
Yao Yin,Zhibing Song,Luqi Wang et al.
Yao Yin et al.
The 1,2,4-triazole scaffold represents a class of bioactive molecules with distinctive physicochemical properties and broad-spectrum biological activities. Previous studies have explored compounds bearing triazole rings for their anti-tumor...
Development of Thieno[2,3-b]pyridin-6(7H)-one derivatives against drug-resistant Mycobacterium tuberculosis [0.03%]
用于抗药性结核分枝杆菌的噻诺并吡啶衍生物的研发
Qin Zha,Zhiyong Liu,Wanwen Li et al.
Qin Zha et al.
In this study, two series of thieno[2,3-b]pyridin-6(7H)-one derivatives were rationally designed via substituent swapping and scaffold flipping strategies. Structure-activity relationship (SAR) analysis identified four compounds exhibiting ...
BNANC clamp PCR for simple and sensitive detection of KRAS and EGFR mutations [0.03%]
适用于KRAS和EGFR突变简单灵敏检测的BNANC clamp PCR方法
Ikuya Ban,Ayako Orita,Haruhisa Yoshikawa et al.
Ikuya Ban et al.
2',4'-BNANC (BNANC)-modified oligonucleotides, which have excellent binding affinity to complementary RNA and DNA strands and high nuclease resistance, were successfully used to develop a new clamp polymerase chain reaction (PCR) method for...
Experimental and computational analysis of SERCA inhibition by naphthoquinone derivatives [0.03%]
萘醌衍生物抑制SERCA的实验和计算分析
Sophie Cheng,Sahil Kumar,Sydni Sobota et al.
Sophie Cheng et al.
Naphthoquinones are small aromatic compounds with diverse biological activities and established applications in medicine and industry. Previous studies have identified a limited number of naphthoquinones that inhibit the sarco/endoplasmic r...
Secondary structure engineering of an amphipathic arginine-rich CPP using non-proteinogenic amino acids for enhanced cell-membrane permeability [0.03%]
基于非蛋白氨基酸的细胞穿透肽二级结构工程改造以增强生物膜穿膜能力
Wataru Sato,Yurina Sekine,Takahito Ito et al.
Wataru Sato et al.
Cell-penetrating peptides (CPPs) represent a powerful class of drug delivery systems for transporting impermeable cargo into the intracellular space. While the B-peptide (Sequence: RXRRBRRXRRBRXB; B = β-alanine, X = 1-aminohexanoic acid) h...
Advancements in diverse chemical scaffolds for antimalarial drug discovery: a ten-year hit-to-lead retrospective [0.03%]
抗疟药物发现中的化学骨架多样性进展：为期十年的从苗头化合物到先导物研究回顾性分析
Marcelo Augusto Pereira Januário,Douglas Davison da Silva Oliveira,Flávio Luis Cardoso Silveira et al.
Marcelo Augusto Pereira Januário et al.
Malaria remains one of the most devastating parasitic diseases worldwide, accounting for hundreds of millions of cases and significant mortality annually. Despite the availability of therapeutic interventions, the efficacy of current pharma...
Improvements in potency and selectivity of triazine nitrile inhibitors targeting Toxoplasma gondii cathepsin L for the treatment of latent toxoplasmosis [0.03%]
三嗪腈抑制剂改善了针对弓形虫囊尾蚴猫泡状 протозоа酶的效力和特异性以治疗隐性弓形虫病
Timothy J Borel nd,Jacob R Hitchens,Hargobinder Kaur et al.
Timothy J Borel nd et al.
The protozoan Toxoplasma gondii is one of the most prevalent infectious agents, having infected approximately one third of the global population. It remains a leading cause of deaths due to foodborne illness, can cause serious complications...
A general tyrosinase-responsive prodrug strategy: design and synthesis of melanoma-selective anticancer agents [0.03%]
一种通用的酪氨酸酶响应型前药策略：用于设计和合成选择性黑色素瘤抗癌剂
Boxiang Qiu,Yening Zou,Binjie Li et al.
Boxiang Qiu et al.
Melanoma is highly aggressive with limited therapeutic options for advanced-stage disease, making it the leading cause of skin cancer-related deaths. This study developed a tyrosinase (TYR)-responsive prodrug design strategy by taking TYR-a...
Physicochemical and RNA structural features of selective RNA binding by drug-like small molecules [0.03%]
药物样小分子选择性结合RNA的理化、结构特征分析
Hiroki Yoshida,Ryosuke Nagasawa,Kaoru R Komatsu
Hiroki Yoshida
Binding selectivity is critical for small molecules targeting RNA in the therapeutic field, requiring rational design of selective compounds. However, the key features of selective binding remain incompletely understood due to lack of compr...