SAR study of niclosamide derivatives in the human glioblastoma U-87 MG cells [0.03%]
尼卡 stools 胺衍生物的人胶质母细胞瘤 U-87 MG 细胞 SAR 研究
Shizue Mito,Benxu Cheng,Benjamin A Garcia et al.
Shizue Mito et al.
Glioblastoma is a lethal malignant brain tumor, and the development of efficient chemotherapeutic agents remains an urgent need. Niclosamide, an anthelmintic drug, which has been used to treat tapeworm infections more than 50 years, has rec...
Development and evaluation of mitochondria-targeted caseinolytic protease (ClpP) agonist chemical probes in in vitro breast cancer models [0.03%]
用于体外乳腺癌模型的线粒体靶向乳酸蛋白酶（ClpP）激动剂化学探针的开发与评估
Xiaoyu Hao,Gunjan Purohit,Yahani P Jayasinghe et al.
Xiaoyu Hao et al.
Mitochondria carry out a plethora of functions that are vital for cellular physiology and metabolism. Mitochondrial caseinolytic protease (ClpP) is part of the larger CLPXP machinery that is critical for mitochondrial protein homeostasis an...
Dynamic tail amine interactions drive isoform selectivity for potent human neuronal nitric oxide synthase inhibitors [0.03%]
动态尾胺相互作用驱动高效的人类神经型一氧化氮合酶同工酶选择性抑制剂的作用机制
Amardeep Awasthi,Koon Mook Kang,Richard B Silverman
Amardeep Awasthi
Achieving isoform-selective inhibition of neuronal nitric oxide synthase (nNOS) remains a significant challenge due to the high structural similarity with other NOS isoforms. Here, we report the design, synthesis, and characterization of no...
Inactivation of ornithine aminotransferase by (1 R,4 S)-4-Amino-3-(trifluoromethyl)cyclopent-2-ene-1-carboxylic acid via a stable quinonoid intermediate [0.03%]
通过稳定的醌类中间体由(1R,4S)-4-氨基-3-(三氟甲基)环戊烯-1-羧酸使鸟氨酸转氨酶失活
Koon Mook Kang,Abigail L Vargas,Wei Zhu et al.
Koon Mook Kang et al.
Ornithine aminotransferase (OAT), a pyridoxal 5'-phosphate (PLP)-dependent enzyme, is a key contributor to glutamine supply in cancer cells, suggesting its therapeutic potential for hepatocellular carcinoma (HCC), the most common form of li...
Increased Plasma Concentrations of 6-oxo-Methylphenidate in CES1 G134E Carriers Following a Single Oral Dose of Methylphenidate [0.03%]
单次口服哌甲酯后CES1 G134E携带者的血浆6-氧代-甲基苯环利定浓度升高
Qingchen Zhang,Philip W Melchert,Ahmed Awad et al.
Qingchen Zhang et al.
Attention-deficit/hyperactivity disorder (ADHD) is a neurodevelopmental disorder, with methylphenidate used as a first-line treatment. Methylphenidate is primarily hydrolyzed by carboxylesterase 1 (CES1) to inactive ritalinic acid, with min...
IND-Enabling Preclinical Studies of [11C]COU, a Trapped Metabolite PET Radiotracer for Monoamine Oxidase-B [0.03%]
一种单胺氧化酶B的PET放射示踪剂[11C]COU被俘获代谢物的药代动力学预临床研究
Madison Frazier,Tanpreet Kaur,Jenelle Stauff et al.
Madison Frazier et al.
[11C]COU is a trapped metabolite radiotracer for in vivo analysis of Monoamine Oxidase B activity using positron emission tomography (PET) imaging. [11C]COU has the potential to quantify astrocytosis in the early stages of Alzheimer's disea...
Peptide halogenation biochemistry: interfacing pharmaceutical deliverables with chemical innovation [0.03%]
肽卤化生物化学：药物传输与化工创新之间的接口问题研究
Vinayak Agarwal
Vinayak Agarwal
The biosynthetic schemes for the production of halogenated peptidic natural products offer avenues for the discovery of peptide halogenases, and opportunities for development of biocatalysts for derivatization of peptides and proteins. Here...
Discovery of CRBN-recruiting PROTAC degraders of the METTL3-METTL14 complex [0.03%]
发现CRBN募集型PROTAC降解METTL3-METTL14复合物的分子
Alexis R Smith,Rukiye Nar,Yafang Li et al.
Alexis R Smith et al.
METTL3 and METTL14, key components of the m6A writer complex, are frequently overexpressed in various malignancies, including acute myeloid leukemia (AML), where aberrant methylation has been linked to the upregulation of oncogenic transcri...
Anaeic and tumoic acids, new functionalized fatty acids from marine cyanobacteria, inhibit quorum sensing in Pseudomonas aeruginosa [0.03%]
来源于海洋蓝绿藻的两种新型功能化脂肪酸анаeic和tumoic酸可抑制铜绿假单胞菌的群体感应
Emma K Ellis,Sarath P Gunasekera,Sofia Kokkaliari et al.
Emma K Ellis et al.
Quorum sensing (QS) is the mechanism in which bacteria assess the threshold concentration of small signaling molecules to induce cell survival by overwhelming the host's defenses. It is one of the fundamental mechanisms controlling bacteria...
Halogenated quinoline kill agent rapidly induces iron starvation of Staphylococcal biofilms [0.03%]
卤代喹啉杀菌剂可快速导致金黄色葡萄球菌生物被膜铁缺乏
Robert W Huigens rd,Ke Liu,Nana Shao et al.
Robert W Huigens rd et al.
Bacterial biofilms are surface-attached communities comprised of slow- or non-replicating bacteria. Transcriptomic responses of bacterial biofilms to anti-biofilm small molecules have been largely unexplored, with existing studies typically...