Results 51 to 60 of about 24,681 (243)

O‐GlcNAcylation Regulation of SNAP29‐Dependent Autophagy Activation Dictates Chemoresistance in Gastric Cancer

Advanced Science, EarlyView.
Model illustrating the proposed mechanism by which chemotherapy‐induced downregulation of OGT disrupts SNAP29 O‐GlcNAcylation, promoting STX17‐SNAP29‐VAMP8 SNARE complex assembly and protective autophagy, leading to chemoresistance, which in turn establishes a feedforward loop to perpetuate drug tolerance.
Liang Tang, Shaoji Zhao, Ziling Shao, Tao Luo, Baifu Peng, Yifan Liu, Jinning Ye, Jianjun Peng, Kaiyu Sun, Jianbo Xu   +9 more
wiley   +1 more source

Exploration of Novel Biomarkers for Neurodegenerative Diseases Using Proteomic Analysis and Ligand-Binding Assays

Biomedicines
Background/Objectives: Neurodegenerative diseases are a major cause of morbidity and mortality worldwide, and their public health burden continues to increase.
Annalena Kenzelmann, Christina Boch, Ronny Schmidt, Mario Richter, Michael Schulz   +4 more
doaj   +1 more source

Recapitulating In Vivo Pharmacokinetics and Size‐Dependent Nanomedicine Delivery in a Microfluidic Platform

Advanced Science, EarlyView.
A microfluidic tumor platform integrates pharmacokinetic flow control, vascular‐like barriers, and 3D tumor spheroids to emulate in vivo drug exposure. The system reproduces dynamic concentration–time profiles and enables size‐dependent nanoparticle transport and efficacy evaluation, providing a predictive framework for assessing nanomedicine ...
Su Jeong Kang, Moon Sup Yoon, Jae Min Lee, Min Jeong Jo, Chae Eun Jin, Dae Hwan Shin   +5 more
wiley   +1 more source

Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Journal of the Turkish Chemical Society, Section A: Chemistry, 2023
In this study, the synthesis of chalcone compounds (1-11) derived from 4-(imidazol-1-yl)acetophenone and the structure determination of these compounds by various spectroscopic methods were carried out.
Bedriye Seda KURŞUN AKTAR, Abdulraheem Mustafa ALKARABASH , Ayşe ŞAHİN YAĞLIOĞLU, Emine Elçin ORUÇ-EMRE   +3 more
doaj   +1 more source

Large‐Scale Machine Learning to Screen for Small‐Molecule Senolytics

Advanced Intelligent Discovery, EarlyView.
A consistent workflow underpins all experiments in this study. A dedicated model‐selection dataset first identifies optimal hyperparameters for each algorithm. Models are then trained and rigorously evaluated on independent sets of molecules using the senolytic ratio SR. Comprehensive hyperparameter exploration across SMILES representations, task types,
Alexis Dougha, Jesus Gil, Pedro J. Ballester   +2 more
wiley   +1 more source

Structure-Based Virtual Screening of Pseudomonas aeruginosa LpxA Inhibitors using Pharmacophore-Based Approach

Biomolecules, 2020
Multidrug resistance in Pseudomonas aeruginosa is a noticeable and ongoing major obstacle for inhibitor design. In P. aeruginosa, uridine diphosphate N-acetylglucosamine (UDP-GlcNAc) acetyltransferase (PaLpxA) is an essential enzyme of lipid A ...
Baki Vijaya Bhaskar, Tirumalasetty Muni Chandra Babu, Aluru Rammohan, Gui Yu Zheng, Grigory V. Zyryanov, Wei Gu   +5 more
doaj   +1 more source

Mechanistically transparent models for predicting aqueous solubility of rigid, slightly flexible, and very flexible drugs (MW<2000) Accuracy near that of random forest regression

ADMET and DMPK, 2023
Yalkowsky’s General Solubility Equation (GSE), with its three fixed constants, is popular and easy to apply, but is not very accurate for polar, zwitterionic, or flexible molecules. This review examines the findings of a series of studies, where we have
Alex Avdeef
doaj   +1 more source

Acetylpromazine maleate revisited: deep-dive equilibrium analysis revealing drug salt acting as a pH- and pS-stat counter-titrant

AAPS Open
Acetylpromazine is a phenothiazine derivative that is prone to form sub-micellar aggregates and micelles in water above pH 5. This study revisits the determination of the equilibrium constants (Avdeef et al., ADMET DMPK 4:117-178, 2016) describing the ...
Alex Avdeef
doaj   +1 more source

Design, synthesis and molecular modelling studies of some pyrazole derivatives as carbonic anhydrase inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
In this study, newly synthesised compounds 6, 8, 10 and other compounds (1–5, 7 and 9) and their inhibitory properties against the human isoforms hCA I and hCA II were reported for the first time.
Yazgı Dizdaroglu, Canan Albay, Tayfun Arslan, Abdulilah Ece, Emir A. Turkoglu, Asiye Efe, Murat Senturk, Claudiu T. Supuran, Deniz Ekinci   +8 more
doaj   +1 more source

adm kepemimpinan

, 2019
Educational leadershipis a leader in aneducational unit. Without the presence of educational leadership, the educational process including learning will not run effectively. Educational leadership is a leader whose existence can be directly elected, determined by a foundation, or determined by the government.
null mutiararahmadila, Hade Afriansyah
openaire   +2 more sources