Results 31 to 40 of about 8,212 (230)
In Situ Bioorthogonal Synthesis of PROTACs via Dual-Responsive Cleavage for Synergistic Photo-Immunotherapy. [PDF]
Adv Sci (Weinh)A bioactive self‐delivering SNAP‐TAC platform responds to tumor‐associated cathepsin B and glutathione, enabling in situ bioorthogonal synthesis of a BRD4‐degrading proteolysis‐targeting chimera within the tumor microenvironment. The resulting BRD4 degradation and PD‐L1 downregulation synergize with photodynamic therapy‐induced immunogenic cell death ...
Jian S +14 more
europepmc +2 more sources
Frontiers in Oncology, 2022 Focal adhesion kinase (FAK) is highly expressed in a variety of human cancers and is a target for cancer therapy. Since FAK kinase inhibitors only block the kinase activity of FAK, they are not highly effective in clinical trials. FAK also functions as a
Xueyun Huo +15 more
doaj +1 more source
Specific MHC-I Peptides Are Induced Using PROTACs
Frontiers in Immunology, 2018 Peptides presented by the class-I major histocompatibility complex (MHC-I) are important targets for immunotherapy. The identification of these peptide targets greatly facilitates the generation of T-cell-based therapeutics.
Stephanie M. Jensen +3 more
doaj +1 more source
The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents
Molecules, 2020 The induction of protein degradation in a highly selective and efficient way by means of druggable molecules is known as targeted protein degradation (TPD).
Bernat Coll-Martínez +2 more
doaj +1 more source
Current strategies for the design of PROTAC linkers: a critical review
Exploration of Targeted Anti-tumor Therapy, 2020 PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to bind to a protein of interest, connected by a chemical linker.
Robert I. Troup +2 more
doaj +1 more source
PROTACs: A novel strategy for cancer drug discovery and development
MedComm, 2023 Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists of three components: a small molecule that binds to a target protein, an ...
Xin Han, Yi Sun
doaj +1 more source
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
Journal of Hematology & Oncology, 2020 Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently ...
Xin Li, Yongcheng Song
doaj +1 more source
PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective
Acta Materia Medica, 2022 Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed.
Xin Han, Wenyi Wei, Yi Sun
doaj +1 more source
Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1)
Journal of Enzyme Inhibition and Medicinal Chemistry, 2020 Poly(ADP-ribose) polymerase-1 (PARP-1), a critical DNA repair enzyme in the base excision repair pathway, has been pursued as an attractive cancer therapeutic target.
Zhimin Zhang +8 more
doaj +1 more source
PROTAC technology for the treatment of Alzheimer’s disease: advances and perspectives
Acta Materia Medica, 2022 Neurodegenerative diseases are characterized by the progression of neuronal degeneration, resulting in dysfunction of cognition and mobility. Many neurodegenerative diseases are due to proteinopathies arising from unusual protein accumulation and ...
Hiroyuki Inuzuka +3 more
doaj +1 more source