Results 91 to 100 of about 11,335 (243)

YX-112, a novel celastrol-derived PROTAC, inhibits the development of triple-negative breast cancer by targeting the degradation of multiple proteins

Frontiers in Pharmacology
BackgroundCelastrol is an effective component of the plant Tripterygium wilfordii Hook. f., which has a high inhibitory effect on triple-negative breast cancer.
Yongxue Gu, Mengmeng Yang, Wenbin Wang, Lihua Li, Ying Ma, Wenshan Liu, Wenshan Liu, Qiang Zhao   +7 more
doaj   +1 more source

Non-invasive in vivo monitoring of PROTAC-mediated protein degradation using an environment-sensitive reporter

Nature Communications
Proteolysis targeting chimeras (PROTACs) represent a groundbreaking therapeutic technology for selectively degrading proteins of interest (POIs). The structural variations in PROTACs unpredictably influence their protein degradation efficiency, which is ...
Tao Li, Qingyu Zong, He Dong, Ihsan Ullah, Zhenhai Pan, Youyong Yuan   +5 more
semanticscholar   +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

Advancing Design Strategy of PROTACs for Cancer Therapy

MedComm
Proteolysis targeting chimeras (PROTACs) have emerged as a groundbreaking class of anticancer therapeutics. These bifunctional molecules harness the endogenous ubiquitin–proteasome system to facilitate the degradation of targeted proteins of interest ...
Hang Luo, Yuan Tian, Razack Abdullah, Baoting Zhang, Yuan Ma, Ge Zhang   +5 more
doaj   +1 more source

PROTAC^® technology and potential for its application in infection control

Тонкие химические технологии
Objectives. To describe the pharmaceutical technology of controlled degradation of protein molecules (PROTAC®, Proteolysis Targeting Chimera), approaches to the design of the PROTAC® molecule, methods of ligand and linker selection and synthesis, as well
M. A. Zakharova, M. V. Chudinov
doaj   +1 more source

Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease.

Journal of Medicinal Chemistry
We have witnessed three coronavirus (CoV) outbreaks in the past two decades, including the COVID-19 pandemic caused by SARS-CoV-2. Main protease (MPro), a highly conserved protease among various CoVs, is essential for viral replication and pathogenesis ...
Yugendar R. Alugubelli, Jing Xiao, Kaustav Khatua, Sathish Kumar, Long Sun, Yuying Ma, Xinyu R Ma, Veerabhadra Vulupala, Sandeep Atla, Lauren R. Blankenship, Demonta D. Coleman, Xuping Xie, Benjamin W. Neuman, W. Liu, Shiqing Xu   +14 more
semanticscholar   +1 more source

G Protein–Coupled Receptors in Olfactory Signaling and Related Disorders: Mechanisms and Therapeutic Implications

Sensory Neuroscience, EarlyView.
This schematic highlights GPCRs as the central hub of olfactory signaling in health and disease. The central GPCR shows odorant activation and downstream pathways. Surrounding quadrants illustrate four GPCR‐mediated themes: odor perception and adaptation, mucosal immunity and regeneration, memory consolidation via neural circuits, and GPCR‐related ...
Zishuo Guo, Hongjie Du, Fanyu Yuan, Yuhan Dong, Fangyuan Zhu, Jian Liu, Chengzhilin Li, Xu Guo, Zhaoze Yang, Wenwen Qi, Ming Xia, Chengcheng Liu   +11 more
wiley   +1 more source

PROTAC Design v1

, 2022
PROTAC (protein degradation targeted chimera) is a special protein degradation technology, which uses ubiquitin proteasome pathway, a natural protein degradation pathway in cells, to remove specific proteins that need to be degraded. A PROTAC molecule consists of two key domains: the domain that specifically binds to the target protein that needs to be
openaire   +1 more source

Update on Non‐Biological and RNA‐Based Therapeutics in Chronic Inflammatory Diseases: Precision Medicine Through Small Molecules: An EAACI Position Paper

Allergy, EarlyView.
ABSTRACT In the last decades, critical advancements in research technology and knowledge on disease mechanisms steered therapeutic approaches for chronic inflammatory diseases towards unprecedented target specificity. For allergic and chronic lung diseases, biologic drugs pioneered this goal, acquiring on the way—through the clinical use of monoclonal ...
F. Roth‐Walter, I. M. Adcock, C. Benito‐Villalvilla, R. Bianchini, L. Bjermer, G. Caramori, L. Cari, K. F. Chung, Z. Diamant, I. Eguiluz‐Gracia, E. F. Knol, M. Jesenak, F. Levi‐Schaffer, G. Nocentini, L. O'Mahony, O. Palomares, F. Redegeld, M. Sokolowska, B. Van Esch, M. Zurlo, C. Stellato   +20 more
wiley   +1 more source

Selective small molecule targeting of KDM4 as a therapeutic strategy to reduce proliferation of acute myeloid leukaemia

British Journal of Haematology, EarlyView.
Summary Acute myeloid leukaemia (AML) is an aggressive disease with poor survival and high relapse rates. Coupled with the complex mutational burden observed, there is an unmet clinical need for more targeted therapies. Epigenetic therapies have shown promise both as monotherapy and in combination strategies and specifically histone lysine demethylase,
Laura Monaghan, Roderick P. Bunschoten, Joana Bittencourt‐Silvestre, Taeju Park, Susan Gannon, Petrisor Alin Pirvan, Alex Hoose, Helen Wheadon, Robert M. J. Liskamp, Xu Huang, Heather G. Jørgensen   +10 more
wiley   +1 more source