Results 91 to 100 of about 8,212 (230)

Application of PROTACs in target identification and validation

Acta Materia Medica
Proteolysis targeting chimeras (PROTACs), as a novel therapeutic drug model, has received widespread attention from academia and the pharmaceutical industry.
Yang Liu, Jing Liang, Rui Zhu, Yueying Yang, Yali Wang, Wenyi Wei, Hua Li, Lixia Chen   +7 more
doaj   +1 more source

MEGA PROTAC, MEGA DOCK-based PROTAC mediated ternary complex formation pipeline with sequential filtering and rank aggregation

Scientific Reports
Proteolysis-targeting chimaeras (PROTACs), which induce proteolysis by recruiting an E3 ligase to dock into a target protein, are acquiring popularity as a novel pharmacological modality because of the unique features of PROTAC, including high potency ...
Sadettin Y. Ugurlu, David McDonald, Ramazan Enisoglu, Zexuan Zhu, Shan He   +4 more
doaj   +1 more source

Tackling cancer stemness with nanotechnology in the era of precision medicine

BMEMat, EarlyView.
Precise customization of nanoparticles (NPs) enables active targeting of cancer stem cells (CSCs), thereby improving drug delivery and therapeutic efficacy. NP‐based probing enhances CSC detection through imaging and liquid biopsy, whereas diverse therapeutic payloads improve therapeutic outcomes.
Shaolei Guo, Shun Yao, Lihui Meng, Chunyuan Chen, Yuechu Lucinda Lu, Rong Lu, Kashif Rafiq Zahid, Umar Raza, Qingzhi Wu, Wenli Chen   +9 more
wiley   +1 more source

Mitochondria‐endoplasmic reticulum organelle glue as maturation promoter for origination/dimensional dual‐cross cardiomyocytes

BMEMat, EarlyView.
Mitochondria‐endoplasmic reticulum contact sites (MERCS) are areas where the mitochondria and endoplasmic reticulum closely interact. In this study, we utilize synthetic organelle glues to artificially engineer MERCS for regulating cardiomyocyte development, through which the immature and chemo‐plasticity issues of undifferentiated cells are addressed.
Wei Tang, Hao Sun, Chenqi Duan, Jiajia Chang, Yuxing Wang, Ming Zhao, Huiyue Zhao, Shan Lu, Yang Yang, Da Huo   +9 more
wiley   +1 more source

Fibrilpaint: A Class of Amyloid‐Targeting Peptides

Chemistry – A European Journal, EarlyView.
FibrilPaints are modular peptides engineered to recognize amyloid fibrils. By systematically varying charge, sequence, and termini, their binding behavior can be tuned while retaining recognition. Successful binding ″paints″ fibrils for visualization and opens routes toward targeted degradation and diagnostic applications.
Júlia Aragonès Pedrola, Françoise A. Dekker, Katrin Guttmann, Litske M. van Leeuwen, Shalini Singh, Guy Mayer, Tommaso Garfagnini, Assaf Friedler, Stefan G. D. Rüdiger   +8 more
wiley   +1 more source

A region-confined PROTAC nanoplatform for spatiotemporally tunable protein degradation and enhanced cancer therapy

Nature Communications
The antitumor performance of PROteolysis-TArgeting Chimeras (PROTACs) is limited by its insufficient tumor specificity and poor pharmacokinetics. These disadvantages are further compounded by tumor heterogeneity, especially the presence of cancer stem ...
Jing Gao, Xingyu Jiang, Shumin Lei, Wenhao Cheng, Yi Lai, Min Li, Lei Yang, Peifeng Liu, Xiao-hua Chen, Min Huang, Haijun Yu, Huixiong Xu, Zhiai Xu   +12 more
doaj   +1 more source

Trends and Future Directions in Organic Chemistry for Drug Discovery

Chemistry – A European Journal, EarlyView.
Organic synthesis is being reshaped by the convergence of catalytic innovation, automation, artificial intelligence, and emerging therapeutic modalities. Late‐stage functionalization, photoredox and electrochemical methods, biocatalysis, flow chemistry, DELs, and proximity‐based drugs are examined as components of closed‐loop discovery.
Paweł Kozyra, Maciej Masłyk
wiley   +1 more source

Property-based optimisation of PROTACs

RSC Medicinal Chemistry
PROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical properties.
James S. Scott, Iacovos N. Michaelides, Markus Schade   +2 more
openaire   +3 more sources

Synthesis of β‐ and γ‐Carbolinones Through a Fe(III)‐Mediated Radical 6‐Endo‐Trig Cyclization of Indole‐Based Ugi 4‐CR Adducts

European Journal of Organic Chemistry, EarlyView.
A practical strategy for synthesizing β‐ and γ‐carbolinones from indole‐based Ugi 4‐CR adducts through an intramolecular radical cyclization using Fe(III)–H species is presented. This approach enables the efficient synthesis of spiro‐carbolinones under mild reaction conditions and demonstrates the effectiveness of secondary radicals in both cyclization
María F. Olvera‐Granados, Luis A. Polindara‐García   +1 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