Results 91 to 100 of about 7,362 (230)
PharmaceuticsProteolysis-targeting chimeras (PROTACs) selectively degrade target proteins by recruiting intracellular E3 ubiquitin ligases, overcoming the limitations of traditional small-molecule inhibitors that merely block protein function.
Xiaoqing Wu +7 more
doaj +1 more source
Property-based optimisation of PROTACs
RSC Medicinal ChemistryPROTACs 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 +2 more
openaire +3 more sources
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
An Update on Clinically Advanced PROTAC Degraders and Their Synthesis
MoleculesProteolysis-targeting chimeras (PROTACs) have emerged as a revolutionary therapeutic modality that enables degradation of therapeutically relevant proteins through the protein disposal machinery, the ubiquitin-proteasome system (UPS).
Ranjan Kumar Acharyya +6 more
doaj +1 more source
Multi‐omics–driven precision medicine
iMeta, EarlyView.Multi‐omics‐driven precision medicine (MODPM) provides a multiscale, continuously learnable framework that integrates genomics, epigenomics, transcriptomics, proteomics, metabolomics, microbiome profiles, and clinical data. Powered by artificial intelligence and foundation models, MODPM enables cross‐modal representation learning, contextual modeling ...
Huibo Li +20 more
wiley +1 more source
Protocol for constructing tumor-targeting ANM-PROTACs for degradation of transcription factors
STAR ProtocolsSummary: AS1411-NCL-MDM2-based proteolysis-targeting chimeras (ANM-PROTACs) are capable of inducing selective degradation of transcription factors (TFs) in tumor cells. Here, we present a protocol for constructing ANM-PROTACs.
Jin Li, Chao Liang
doaj +1 more source
Journal of the American Chemical SocietyProteolysis targeting chimera (PROTAC)-based degraders are highly potent pseudocatalytic drugs, but on-target off-site homing could yield undesirable consequences. We report here a generalizable AND-logic gated PROTAC, where the concurrent presence of two different disease-relevant endogenous stimuli liberates an active protein degrader. We design Dual-
Ranit Dutta +4 more
openaire +2 more sources
TRIM31–LOX‐1 Axis: A Novel Therapeutic Frontier in Atherosclerosis
iNew Medicine, EarlyView.ABSTRACT Atherosclerosis, driven by a vicious cycle of lipid accumulation and chronic inflammation, underlies most cardiovascular diseases. Macrophages exacerbate this process by internalizing oxidized low‐density lipoprotein (oxLDL), forming foam cells, and releasing inflammatory mediators. A recent study published in Circulation identified the TRIM31–
Qian Zhang, Cheng Xue Qin
wiley +1 more source
Click chemistry in the development of PROTACs
RSC Chemical BiologyThis review discusses leveraging click chemistry to address unmet needs in PROTAC development.
Ce Yang, Ravi Tripathi, Binghe Wang
openaire +2 more sources
Hsp90 Inhibition on the Western Blot: N‐Terminal Versus C‐Terminal Inhibitors in Breast Cancer
Medicinal Research Reviews, EarlyView.ABSTRACT Heat shock protein 90 (Hsp90) is an established and clinically validated anticancer target. By regulating the folding and maturation of diverse client proteins, it is indirectly involved in carcinogenesis. Key breast cancer oncogenic drivers, including estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2, are ...
Jaka Dernovšek +3 more
wiley +1 more source