Results 101 to 110 of about 7,362 (230)

Accelerating PROTACs Discovery Through a Direct‐to‐Biology Platform Enabled by Modular Photoclick Chemistry

Advanced Science
Proteolysis targeting chimeras (PROTACs) have emerged as a promising strategy for drug discovery and exploring protein functions, offering a revolutionary therapeutic modality.
Ke‐Nian Yan, Yong‐Qiang Nie, Jia‐Yu Wang, Guang‐Liang Yin, Qia Liu, Hao Hu, Xiaoxia Sun, Xiao‐Hua Chen   +7 more
doaj   +1 more source

Molecular Glue Degraders in Early Development for Cancer Therapy

Medicinal Research Reviews, EarlyView.
ABSTRACT Molecular glue degraders are an emerging class of small molecule allosteric modulators that induce or stabilize protein‐protein interactions, enabling targeted degradation of previously intractable proteins. By redirecting E3 ligases to recognize neosubstrates, proteins that are not typically recognized by a specific E3 ubiquitin ligase, they ...
E. Sila Ozdemir, Hyunbum Jang, Ozlem Keskin, Attila Gursoy, Ruth Nussinov   +4 more
wiley   +1 more source

Effects of bioinsecticide exposure route on aphids and their natural enemies in oilseed rape

Pest Management Science, EarlyView.
Fatty acids, silicone polymers and surfactants reduced aphid numbers but caused natural enemy mortality under direct exposure, while minimal residual activity suggests potential for targeted, compatible use in integrated pest management. Abstract BACKGROUND Myzus persicae Sulzer and Brevicoryne brassicae L.
Aimee J. Tonks, Tom W. Pope, Simon Cooper, Joe M. Roberts   +3 more
wiley   +1 more source

Innovation in pest management: can the past inform the future?

Pest Management Science, EarlyView.
Progress in pest management occurred incrementally, but occasionally, transformative discoveries introduced disruptive technologies. Looking ahead, generative artificial intelligence is expected to accelerate agricultural discovery by integrating vast datasets from mechanization, genetics, and chemistry.
Eric Moog, Franck E. Dayan
wiley   +1 more source

Molecular glues: Recent advances in cereblon substrate identification and mechanistic insights

Smart Molecules, EarlyView.
Molecular glues exert diverse core biological functions by inducing or stabilizing protein–protein interactions, extending far beyond the traditional scope of targeted protein degradation. Key breakthroughs include expanded cereblon substrate recognition, sustained G protein‐coupled receptor megacomplex signaling, and the first orthosteric molecular ...
Qingyun Guan, Xiaoyu Shi, Qian Yang, Xiangyi Jiang, Xinyong Liu, Peng Zhan   +5 more
wiley   +1 more source

Recent progress on the development of hydrogel‐based microneedles for transdermal drug delivery

VIEW, EarlyView.
This study provides a comprehensive and up‐to‐date analysis of recent progress in HMN technology, covering fundamental transdermal delivery mechanisms and design principles, biomaterials used in HMN fabrication, drug loading and release strategies, and emerging therapeutic applications.
Mohammad Muhtasim Ittisaf, Salman Farsi Taharat, Md. Sadek Miah, Hasan Tasnim Salehin, M. Azam Ali, Shoeb Ahmed   +5 more
wiley   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

PROTACs improve selectivity for targeted proteins

Acta Materia Medica
Proteolysis targeting chimera (PROTAC) technology has emerged as a powerful tool in drug discovery that enables targeted protein degradation through a unique bifunctional approach.
Lihua Liu, Xian Guan, Jiezhen Zhuo, Xifeng Wu, Xin Han   +4 more
doaj   +1 more source

Data-driven Design of PROTAC Linkers to Improve PROTAC Cell Membrane Permeability

JACS Au
Proteolysis-targeting chimeras (PROTACs) are promising next-generation therapeutics for the degradation of disease-associated proteins. However, optimizing the physicochemical properties of PROTACs, particularly their poor cell mem-brane permeability, remains challenging.
Yuki Murakami, Shoichi Ishida, Nobuo Cho, Hitomi Yuki, Masateru Ohta, Teruki Honma, Yosuke Demizu, Kei Terayama   +7 more
openaire   +2 more sources

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source