Results 31 to 40 of about 7,362 (230)

Cereblon-Recruiting PROTACs: Will New Drugs Have to Face Old Challenges?

Pharmaceutics, 2023
The classical low-molecular-weight drugs are designed to bind with high affinity to the biological targets endowed with receptor or enzymatic activity, and inhibit their function.
Marcin Cieślak, Marta Słowianek
doaj   +1 more source

PROTAC Technology: Opportunities and Challenges [PDF]

ACS Medicinal Chemistry Letters, 2020
PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions, large pharmaceutical enterprises (e.g., AstraZeneca, Bayer, Novartis, Amgen, Pfizer, GlaxoSmithKline, Merck, and Boehringer Ingelheim, etc.), and biotechnology companies.
Hongying Gao, Xiuyun Sun, Yu Rao
openaire   +2 more sources

Antiviral PROTACs: Opportunity borne with challenge

Cell Insight, 2023
Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of the ubiquitin-proteasome-system has become a promising strategy in drug design. The overwhelming advantages of PROTAC technology have ensured a rapid and wide usage,
Jinsen Liang, Yihe Wu, Ke Lan, Chune Dong, Shuwen Wu, Shu Li, Hai-Bing Zhou   +6 more
doaj   +1 more source

Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation. [PDF]

Adv Sci (Weinh)
Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Liu K, Yuan X, Zhou Y, Yuan R, Xie S, Chen Y, Wang P, Gao J, Gong Q.   +8 more
europepmc   +2 more sources

The multidimensional biology of SKP2: mechanisms, pathologies, and emerging therapeutic frontiers

Acta Materia Medica
S phase kinase-associated protein 2 (SKP2), the rate-limiting substrate receptor of the SKP1-Cullin1-F-box (SCF) E3 ubiquitin ligase complex, is considered a canonical gatekeeper of cell cycle progression.
Tao Hou, Xiangmei Hua, Peiqiang Yan, Wei Ni, Jingchao Wang, Hiroyuki Inuzuka, David K. Simon, Wenyi Wei   +7 more
doaj   +1 more source

Towards the targeted protein degradation of CK2: design and synthesis of CAM4066-based PROTACs

Beilstein Journal of Organic Chemistry
Human protein kinase CK2 is a constitutively active serine/threonine kinase implicated in numerous cancers. Although ATP-competitive inhibitors such as CX-4945 show therapeutic potential, they are limited by off-target effects and incomplete or transient
Sophie Day-Riley, Sona Krajcovicova, Aryaman Raj Sokhal, Jan L. Venne, Paul Brear, Marko Hyvönen, Benjamin C. Whitehurst, Jason S. Carroll, David R. Spring   +8 more
doaj   +1 more source

PROTAC-PatentDB: A PROTAC Patent Compound Dataset

Scientific Data
Proteolysis-targeting chimeras (PROTAC) are emerging and promising molecules for targeted protein degradation which have the potential to overcome critical bottlenecks in traditional small molecule drug development. However, the scarcity of publicly available data on molecular compound structures has significantly hindered computational drug discovery ...
Hong Cai, Gengyuan Yao, Yulong Shi, Tianyi Zhang, Yuanjia Hu   +4 more
openaire   +2 more sources

The PROTAC technology in drug development [PDF]

Cell Biochemistry and Function, 2019
Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein.
Yutian Zou, Danhui Ma, Yinyin Wang
openaire   +2 more sources

The ubiquitin system in normal and infected germinal center B cells

FEBS Letters, EarlyView.
The ubiquitin system plays a central role in germinal center (GC) B cells, influencing differentiation to long‐lived memory B cells. Oncogenic gammaherpesviruses gain access to memory B cells by establishing latency in GC B cells. Mapping ubiquitin mechanisms in normal and infected GC B cells will define specific molecular circuits in B cells germane ...
Destiny Davis, Lesly Mejia, Emily K Moser   +2 more
wiley   +1 more source

PROTACs: Mechanism and Bioavailability enhancement strategies by nanotechnology, RNA viral infections (vaccine strategy) and Prodrug development

German Journal of Pharmaceuticals and Biomaterials
Proteolysis Targeting Chimera (PROTACs) are a brand-new concept of therapeutics that use the ubiquitin-proteasome system for selective degradation of disease-related proteins.
Sanaul Mustafa, Md Sabir Hussain Siddiquee   +1 more
doaj   +3 more sources