Discovery of "Molecular Switches" within a Series of mGlu5 Allosteric Ligands Driven by a "Magic Methyl" Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype [0.03%]
发现一类mAChR M1变构调节剂化学类型中的“魔法甲基”效应产生“分子开关”，同时获得正向和负向变构调节剂，并具有体内活性
Lisa Barbaro,Alice L Rodriguez,Ashlyn N Blevins et al.
Lisa Barbaro et al.
In the course of optimizing an M1 PAM chemotype, introduction of an ether moiety unexpectedly abolished M1 PAM activity while engendering a "molecular switch" to afford a weak, pure mGlu5 PAM. Further optimization was able to deliver a pote...
Squire J Booker,Stuart J Conway,Afsaneh Lavasanifar
Squire J Booker
Azithromycin Protects Retinal Glia Against Oxidative Stress-Induced Morphological Changes, Inflammation, and Cell Death [0.03%]
阿奇霉素保护视网膜神经胶质细胞免受氧化应激引起的形态变化、炎症和细胞死亡的影响
Binapani Mahaling,Narendra Pandala,Heuy-Ching Wang et al.
Binapani Mahaling et al.
The reactivity of retinal glia in response to oxidative stress has a significant effect on retinal pathobiology. The reactive glia change their morphology and secret cytokines and neurotoxic factors in response to oxidative stress associate...
Collision-Induced Affinity Selection Mass Spectrometry for Identification of Ligands [0.03%]
基于碰撞诱导亲和富集的配体识别质谱分析法
Tin Mak,Jamie Rossjohn,Dene R Littler et al.
Tin Mak et al.
Hyphenated mass spectrometry has been used to identify ligands binding to proteins. It involves mixing protein and compounds, separation of protein-ligand complexes from unbound compounds, dissociation of the protein-ligand complex, separat...
Characterization of a Class A β-Lactamase from Francisella tularensis (Ftu-1) Belonging to a Unique Subclass toward Understanding AMR [0.03%]
一類β-內酰胺酶(Ftu-1)的表征：歸入特異subclass以求理解抗藥性問題
Sourya Bhattacharya,Vivek Junghare,Mousumi Hazra et al.
Sourya Bhattacharya et al.
β-lactamase production with vast catalytic divergence in the pathogenic strain limits the antibiotic spectrum in the clinical environment. Class A carbapenemase shares significant sequence similarities, structural features, and common cata...
Alex Golubovic,Shannon Tsai,Bowen Li
Alex Golubovic
RNA therapy is a disruptive technology comprising a rapidly expanding category of drugs. Further translation of RNA therapies to the clinic will improve the treatment of many diseases and help enable personalized medicine. However, in vivo ...
Inhibition of 3-Hydroxykynurenine Transaminase from Aedes aegypti and Anopheles gambiae: A Mosquito-Specific Target to Combat the Transmission of Arboviruses [0.03%]
抑制埃及伊蚊和按蚊3-羟基苦味酸转氨酶：对抗媒介病毒传播的蚊特异性靶点
Larissa G Maciel,Matheus V F Ferraz,Andrew A Oliveira et al.
Larissa G Maciel et al.
Arboviral infections such as Zika, chikungunya, dengue, and yellow fever pose significant health problems globally. The population at risk is expanding with the geographical distribution of the main transmission vector of these viruses, the...
Antifungal Development and the Urgency of Minimizing the Impact of Fungal Diseases on Public Health [0.03%]
抗真菌药物研发及减少真菌疾病对公众健康影响的紧迫性
Haroldo C de Oliveira,Bárbara T Bezerra,Marcio L Rodrigues
Haroldo C de Oliveira
Fungal infections are a major public health problem resulting from the lack of public policies addressing these diseases, toxic and/or expensive therapeutic tools, scarce diagnostic tests, and unavailable vaccines. In this Perspective, we d...
Controlling Amyloid Beta Peptide Aggregation and Toxicity by Protease-Stable Ligands [0.03%]
稳定的蛋白酶底物调节淀粉样β肽聚集及毒性的研究进展
Rathnam Mallesh,Juhee Khan,Prabir Kumar Gharai et al.
Rathnam Mallesh et al.
Polymerization of soluble amyloid beta (Aβ) peptide into protease-stable insoluble fibrillary aggregates is a critical step in the pathogenesis of Alzheimer's disease (AD). The N-terminal (NT) hydrophobic central domain fragment 16KLVFF20 ...
Targeting Oncogene Promoters and Ribosomal RNA Biogenesis by G-Quadruplex Binding Ligands Translate to Anticancer Activity [0.03%]
通过G-四链体结合配体靶向癌基因启动子和核糖体RNA生物发生展现其抗癌活性
Yelisetty Venkata Suseela,Pallabi Sengupta,Tanaya Roychowdhury et al.
Yelisetty Venkata Suseela et al.
G-Quadruplex (GQ) nucleic acids are promising therapeutic targets in anticancer research due to their structural robustness, polymorphism, and gene-regulatory functions. Here, we presented the structure-activity relationship of carbazole-ba...