Results 81 to 90 of about 1,970 (208)

Protein Structuromics Reveals a Loop‐Controlled Half‐Open Active Pocket Conformation Throughout Fe(II)/α‐ketoglutarate‐Dependent Dioxygenase Catalytic Cycle

Advanced Science, EarlyView.
This study reveals a conserved half‐open active pocket in Fe(II)/α‐ketoglutarate‐dependent dioxygenases through protein structuromics, distinguished by structural features comprising highly flexible loop elements. Enhanced sampling simulations‐guided mutagenesis experiments elucidated how this flexible loop regulates pocket open/closed conformations ...
Lunjie Wu, Huan Liu, Songyin Zhao, Lei Qin, Jiarui Li, Jun Wang, Zixuan Dai, Jie Gu, Yan Xu, Feiran Li, Yao Nie   +10 more
wiley   +1 more source

Mastering particle size analysis: lessons, challenges, and future directions from the FDA–CRCG workshop

AAPS Open
Particle-size distribution (PSD) measurement is a cornerstone of pharmaceutical development and regulatory assessment, influencing formulation stability, dissolution, product quality, and performance.
Xiaoming Xu, William C. Smith, James E. Polli, Christine L. Plavchak, Bin Qin, Yan Wang, Nicholas Holtgrewe, Sam G. Raney, Andre O’Reilly Beringhs, Yihua Bruce Yu, Marc Taraban, Vishalakshi Krishnan, Anna Schwendeman, Dana C. Hammell, Jeffrey D. Clogston, Alan F. Rawle, Jernej Grmaš, Yousif Ayoub, Bernard Domnic, Rama Subba Reddy, Joseph Duncan, Matthew McGann, Jeff Bodycomb, Carl C. L. Schuurmans, Michiel Hermes, Jonathan G. Mehtala, Prashun Roy, Kevin Lance, Collin Britten, Kiwan Park, Daniel Beach, Matthew Elmer, Keith B. Rodenhausen, Zhen Xu, Haiou Qu, Kai-Wei Wu, Maxwell Korang-Yeboah, Yuan Zou, Ji Li, Alaa H. Abuznait, Colette Quinn, Anabelle Ethier, Kendice Ip, Dinesh Dhamecha, Qi Li, Dongkai Zhu, Rutu Valapil   +46 more
doaj   +1 more source

SuFEx‐Enabled Reprogramming of Flavonoids for Selective α‐Glucosidase Covalent Inhibition

Advanced Science, EarlyView.
Selective inhibition of intestinal α‐glucosidase remains limited by poor enzyme specificity and off‐target metabolic effects. Here, SuFEx click chemistry is used to reprogram natural flavonoids into covalent inhibitors with enhanced α‐glucosidase selectivity and controlled reactivity. This strategy enables effective regulation of carbohydrate digestion
Fengyu Guo, Liwei Zhang, Minlong Wang, Yanjin Du, Tianyu Zhang, Hao Chen, Jiazeng Sun, Yang Yu, Zude He, Jie An, Xiaoxu Zhang, Weilin Lin, Fazheng Ren, Pengjie Wang, Ping Liu   +14 more
wiley   +1 more source

Lesion Site‐Targeted Microspheres Modulate Nav1.7‐Related Signaling for Osteoarthritis Treatment

Advanced Science, EarlyView.
Cartilage‐targeted carbamazepine‐loaded WYRGRL‐modified composite microspheres (CBZ/WCOM) anchor to exposed type II collagen in osteoarthritic lesions and release carbamazepine under acidic conditions. This bind‐then‐release platform modulates Nav1.7‐related sodium signaling, Na⁺/Ca²⁺ exchanger‐associated Ca2+ dynamics, and heat shock protein 70 ...
Cheng Chen, Jiaying Li, Jinjin Ma, Xiaonan Yuan, Yao Xiao, Yang Zhang, Yuan Chen, Hao Jiang, Hui He, Jie Hu, Qianglong Chen, Jinniu Zhang, Bin Li, Yun Zhou, Fengxuan Han, Yong Wang   +15 more
wiley   +1 more source

Development and comparison of model‐integrated evidence approaches for bioequivalence studies with pharmacokinetic end points

CPT: Pharmacometrics & Systems Pharmacology
By applying nonlinear mixed‐effect (NLME) models, model‐integrated evidence (MIE) approaches are able to analyze bioequivalence (BE) data with pharmacokinetic end points that have sparse sampling, which is problematic for non‐compartmental analysis (NCA).
Xiaomei Chen, Henrik B. Nyberg, Mark Donnelly, Liang Zhao, Lanyan Fang, Mats O. Karlsson, Andrew C. Hooker   +6 more
doaj   +1 more source

RNF138‐Mediated Ubiquitination and Degradation of NS5 Restricts Tick‐Borne Encephalitis Virus Infection

Advanced Science, EarlyView.
Host‐specific compatibility between RNF138‐like proteins and flavivirus NS5 determines NS5 stability. Mammalian RNF138 but not arthropod homologs recognizes and induces conserved NS5/RdRp K48‐linked ubiquitination and proteasomal degradation, thereby restricting viral replication. Ectopic RNF138 in mice attenuates TBEV‐induced pathogenesis. (Created in
Jialiang Sun, Weijing Yang, Hao Zhou, Shuai Li, Xin Jiang, Jianyang Gu, Wenyan Zhang   +6 more
wiley   +1 more source

A Novel Lactose/MCC/L-HPC Triple-Based Co-Processed Excipients with Improved Tableting Performance Designed for Metoclopramide Orally Disintegrating Tablets

Pharmaceutics
New co-processed excipients comprising lactose (filler and sweetener), microcrystalline cellulose (MCC, filler), and low-substituted hydroxypropyl cellulose (L-HPC, disintegrant and binder) were developed via solvent evaporation for the preparation of ...
Xiaorong Dai, Jiamin Wang, Bo Yan, Qian Wang, Yan Shen, Yongkang Chen, Yu Tian   +6 more
doaj   +1 more source

Microplastics‐Induced Gut Microbiota Dysbiosis Accelerates Alzheimer's‐Like Pathology and Cognitive Decline via the Gut–Brain Axis

Advanced Science, EarlyView.
Microplastics (MPs) breach the gut‐brain axis by triggering taurine‐depleting microbiota dysbiosis that accelerates Alzheimer‐like pathology in 5XFAD mice. Taurine supplementation normalizes autophagy, microglial quiescence, and cognition, and plasma taurine inversely tracks cognitive decline in ADNI participants, revealing a readily translatable ...
Zifeng Wu, Jiarong Yang, Miaoxuan Zhang, Yi Li, Zhuling Tu, Ji Wang, Jin‐Tai Yu, Kun Guo, Rongcan Luo   +8 more
wiley   +1 more source

Multi‐Targeting Carnosic Acid Kills Drug‐Resistant Helicobacter pylori With Narrow‐Spectrum Activity

Advanced Science, EarlyView.
Carnosic acid selectively eradicates drug‐resistant Helicobacter pylori through a multi‐targeted mechanism involving urease inhibition, membrane disruption, and biofilm eradication. It exhibits no detectable resistance, potent in vivo efficacy, and minimal impact on gut microbiota, positioning it as a promising narrow‐spectrum lead compound against ...
Yuefan Bai, Hongming Huang, Xudong Hang, Shanwei Hu, Qian Tong, Jingchen Xu, Jia Jia, Hongkai Bi   +7 more
wiley   +1 more source

Generic Drugs [PDF]

Diabetes Care, 2007
openaire   +2 more sources