Results 91 to 100 of about 43,723 (349)

HSP70 Interactome‐Mediated Proteolysis Targeting Chimera (HSP70‐PROTAC) for Ferroptosis‐Driven Cancer Treatment

open access: yesAdvanced Science, EarlyView.
This study reports a novel targeted protein degradation strategy termed “HSP70‐PROTAC” that recruits Hsc70 complex to a target protein for inducing degradation. Among them, GDAz‐3 exhibits effective GPX4 degradation activity via UPS/CMA processes, triggering ferroptosis‐driven anticancer activity in vitro and in vivo.
Jinyun Dong   +15 more
wiley   +1 more source

Copper‐Catalyzed Three‐Component Selective 1,4‐Amino Oxygenation of 1,3‐Dienes

open access: yesAngewandte Chemie, EarlyView.
Enclosed is a copper‐catalyzed selective 1,4‐amino oxgenation of 1,3‐dienes with the presence of a strong Brønsted acid. This three‐component transformation offers a novel and powerful approach to construct (E)‐1,4‐allylic amino oxygenated motifs by the simultaneous installation of structurally diverse alkylamines and alcohols directly onto 1,3‐dienes.
Guangshou Feng   +2 more
wiley   +2 more sources

Market Analysis of Synthetic Drugs: Amphetamine-type Stimulants, New Psychoactive Substances [PDF]

open access: yes, 2017
An estimated quarter of a billion people, or around 5 per cent of the global adult population, used drugs at least once in 2015. Even more worrisome is the fact that about 29.5 million of those drug users, or 0.6 per cent of the global adult population ...

core  

Increases in use of novel synthetic stimulant are not directly linked to decreased use of 3,4-methylenedioxy-N-methylamphetamine (MDMA) [PDF]

open access: yes, 2013
A decline in 3,4-methylenedioxy-N-methylamphetamine (MDMA) use in Adelaide, Australia from 2009 to 2010 was confirmed by us previously. Reports suggested that the shortage in MDMA supply was associated with an increased prevalence of other synthetic ...
Chen, C.   +3 more
core   +1 more source

A Simplified Three‐Tailed N‐Alkyl Phosphoramidate Lipid Platform Enables Inguinal Adipose‐Accumulated mRNA Delivery for Anti‐Obesity Therapy

open access: yesAdvanced Science, EarlyView.
This study develops an mRNA therapy encoding a long‐acting GLP‐1/FGF21 fusion protein. A three‐tailed ionizable lipid engineered three‐component lipid nanoparticle delivers the mRNA to inguinal adipose tissue. In obese mice, this targeted, dual‐hormone treatment potently reduces body weight, fat mass, presenting a localized strategy for metabolic ...
Bin Ma   +10 more
wiley   +1 more source

Iridium-Catalyzed Asymmetric Ring-Opening of Oxabenzonorbornadienes with N-Substituted Piperazine Nucleophiles

open access: yesMolecules, 2015
Iridium-catalyzed asymmetric ring-opening of oxabenzonorbornadienes with N-substituted piperazines was described. The reaction afforded the corresponding ring-opening products in high yields and moderate enantioselectivities in the presence of 2.5 mol % [
Wen Yang, Renshi Luo, Dingqiao Yang
doaj   +1 more source

Simplified Procedure for General Synthesis of Monosubstituted Piperazines—From a Batch Reaction Vessel to a Flow (Microwave) Reactor

open access: yesMolecules, 2020
We reported a novel simplified synthetic procedure for the preparation of monosubstituted piperazine derivatives which can now be easily prepared in a one-pot-one-step way from a protonated piperazine with no need of introduction of a protecting group ...
Dana Němečková   +4 more
doaj   +1 more source

Simultaneous detection of controlled substances in waste water [PDF]

open access: yes, 2013
This study presents a method of simultaneous detection of both traditional and newly emerged drugs of abuse in wastewater. The method is based on solid phase extraction and gas chromatography-mass spectrometry analysis.
Cole, Michael D.   +4 more
core   +3 more sources

Development of Dimethylsulfonium Probes for Broad Profiling of Methyllysine Reader Proteins

open access: yesAdvanced Science, EarlyView.
Development of oligoglycine‐based dimethylsulfonium probes for unbiased crosslinking to methyllysine readers. The general probe facilitates profiling of site‐specific methyllysine readers, evaluation of selectivity and activity of reader inhibitors, and global profiling of methyllysine readers.
Jinyu Yang   +3 more
wiley   +1 more source

AI‐Based D‐Amino Acid Substitution for Optimizing Antimicrobial Peptides to Treat Multidrug‐Resistant Bacterial Infection

open access: yesAdvanced Science, EarlyView.
This study constructed the first D‐amino acid antimicrobial peptide dataset and developed an AI model for efficient screening of substitution sites, with 80% of candidate peptides showing enhanced activity. The lead peptide dR2‐1 demonstrated potent antimicrobial activity in vitro and in vivo, high stability, and low toxicity.
Yinuo Zhao   +14 more
wiley   +1 more source

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