Suchergebnisse - "Proteolysis"

Ligand-embedded photoswitching PROTAC for spatiotemporal tubulin degradation.

Autoren: Zhang W Zeng H Xu M et al.

Quelle: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2025 Dec 15; Vol. 131, pp. 118414. Date of Electronic Publication: 2025 Sep 26.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Antineoplastic Agents*/chemistry , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemical synthesis , Azo Compounds*/chemistry , Azo Compounds*/pharmacology , Stilbenes*/chemistry , Stilbenes*/pharmacology , Tubulin*/metabolism , Tubulin*/chemistry , Tubulin Modulators*/chemistry , Tubulin Modulators*/pharmacology , Proteolysis Targeting Chimera*/chemical synthesis , Proteolysis Targeting Chimera*/chemistry , Proteolysis Targeting Chimera*/pharmacology, Humans ; Cell Line, Tumor ; Drug Screening Assays, Antitumor ; Ligands ; Proteasome Endopeptidase Complex/metabolism ; Proteolysis/drug effects ; Structure-Activity Relationship ; Ultraviolet Rays

Proteolysis targeting chimeras as senolytics: An emerging senotherapy for combating aging.

Autoren: Cruickshank-Taylor AB Kozora JS Carew JS et al.

Quelle: The Journal of pharmacology and experimental therapeutics [J Pharmacol Exp Ther] 2025 Nov; Vol. 392 (11), pp. 103752. Date of Electronic Publication: 2025 Oct 15.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Elsevier Country of Publication: Netherlands NLM ID: 0376362 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1521-0103 (Electronic) Linking ISSN: 00223565 NLM ISO Abbreviation: J Pharmacol Exp Ther Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Senotherapeutics*/pharmacology , Senotherapeutics*/therapeutic use , Aging*/drug effects , Aging*/metabolism , Cellular Senescence*/drug effects, Humans ; Animals ; Proteolysis Targeting Chimera

Targeted protein degradation in pancreatic cancer: advances and challenges of PROTAC-based therapeutics.

Autoren: Huang M Wei F Cao J et al.

Quelle: Bioorganic chemistry [Bioorg Chem] 2025 Oct; Vol. 165, pp. 108985. Date of Electronic Publication: 2025 Sep 12.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2120 (Electronic) Linking ISSN: 00452068 NLM ISO Abbreviation: Bioorg Chem Subsets: MEDLINE

MeSH-Schlagworte: Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Pancreatic Neoplasms*/drug therapy , Pancreatic Neoplasms*/metabolism , Pancreatic Neoplasms*/pathology , Proteolysis Targeting Chimera*/chemistry , Proteolysis Targeting Chimera*/pharmacology , Proteolysis Targeting Chimera*/therapeutic use, Animals ; Humans ; Molecular Structure ; Proteolysis/drug effects

Molecular glues and PROTACs in targeted protein degradation: mechanisms, advances, and therapeutic potential.

Autoren: Eladl O; Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. Electronic address: sobhyeladl@zu.edu.eg.

Quelle: Biochemical pharmacology [Biochem Pharmacol] 2025 Dec; Vol. 242 (Pt 3), pp. 117297. Date of Electronic Publication: 2025 Sep 02.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Elsevier Science Country of Publication: England NLM ID: 0101032 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-2968 (Electronic) Linking ISSN: 00062952 NLM ISO Abbreviation: Biochem Pharmacol Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Drug Discovery*/methods , Small Molecule Libraries*/chemistry , Small Molecule Libraries*/pharmacology, Humans ; Animals ; Ubiquitin-Protein Ligases/metabolism ; Proteasome Endopeptidase Complex/metabolism ; Proteolysis Targeting Chimera

Expanding the Scope of PROTACs: Opportunities and Challenges in Topical Delivery.

Autoren: Gioiello L Di Martino RMC Pirali T

Quelle: Journal of medicinal chemistry [J Med Chem] 2025 Nov 27; Vol. 68 (22), pp. 23676-23689. Date of Electronic Publication: 2025 Nov 19.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Drug Delivery Systems*, Humans ; Administration, Topical ; Animals ; Proteolysis Targeting Chimera

Highly efficient and long-acting split-and-mix proteolysis targeting chimera based on self-assembled polylactic acid.

Autoren: Zhan MM Chen H He M et al.

Quelle: Nature communications [Nat Commun] 2025 Nov 26; Vol. 16 (1), pp. 10555. Date of Electronic Publication: 2025 Nov 26.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Nature Pub. Group Country of Publication: England NLM ID: 101528555 Publication Model: Electronic Cited Medium: Internet ISSN: 2041-1723 (Electronic) Linking ISSN: 20411723 NLM ISO Abbreviation: Nat Commun Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis* , Polyesters*/chemistry, Animals ; Mice ; Female ; Humans ; Cell Line, Tumor ; Mice, Inbred BALB C ; Proteolysis Targeting Chimera

Discovery of a Proteolysis Targeting Chimera for TRKA and RET-derived oncoproteins.

Autoren: Moccia M Zhang L Wang Z et al.

Quelle: Scientific reports [Sci Rep] 2025 Nov 25; Vol. 15 (1), pp. 41770. Date of Electronic Publication: 2025 Nov 25.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Nature Publishing Group Country of Publication: England NLM ID: 101563288 Publication Model: Electronic Cited Medium: Internet ISSN: 2045-2322 (Electronic) Linking ISSN: 20452322 NLM ISO Abbreviation: Sci Rep Subsets: MEDLINE

MeSH-Schlagworte: Proto-Oncogene Proteins c-ret*/metabolism , Proto-Oncogene Proteins c-ret*/antagonists & inhibitors , Proto-Oncogene Proteins c-ret*/genetics , Receptor, trkA*/metabolism , Receptor, trkA*/antagonists & inhibitors , Receptor, trkA*/genetics , Proteolysis*/drug effects , Oncogene Proteins, Fusion*/metabolism , Oncogene Proteins, Fusion*/antagonists & inhibitors , Oncogene Proteins, Fusion*/genetics , Antineoplastic Agents*/pharmacology, Humans ; Animals ; Cell Line, Tumor ; Mice ; Cell Proliferation/drug effects ; Ubiquitin-Protein Ligases/metabolism ; Ubiquitination/drug effects ; Xenograft Model Antitumor Assays ; Proteasome Endopeptidase Complex/metabolism ; Protein Kinase Inhibitors/pharmacology ; Proteolysis Targeting Chimera ; Adaptor Proteins, Signal Transducing

How Feasible Is Docking of PROTACs to POI-E3L Complexes? Testing Physics-Based and ML-Based Docking Tools.

Autoren: Jiménez-Boi R Miñán R Pallara C et al.

Quelle: Journal of chemical information and modeling [J Chem Inf Model] 2025 Nov 24; Vol. 65 (22), pp. 12551-12562. Date of Electronic Publication: 2025 Nov 12.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101230060 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1549-960X (Electronic) Linking ISSN: 15499596 NLM ISO Abbreviation: J Chem Inf Model Subsets: MEDLINE

MeSH-Schlagworte: Molecular Docking Simulation* , Ubiquitin-Protein Ligases*/metabolism , Ubiquitin-Protein Ligases*/chemistry , Proteolysis*/drug effects , Machine Learning*, Drug Discovery ; Protein Binding ; Feasibility Studies ; Proteolysis Targeting Chimera

Design and Synthesis of Novel Candidate CK1δ Proteolysis Targeting Chimeras (PROTACs).

Autoren: Arnold M Thompson T Glennie L et al.

Quelle: Molecules (Basel, Switzerland) [Molecules] 2025 Nov 18; Vol. 30 (22). Date of Electronic Publication: 2025 Nov 18.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Casein Kinase Idelta*/antagonists & inhibitors , Casein Kinase Idelta*/metabolism , Casein Kinase Idelta*/chemistry , Drug Design*, Humans ; Ubiquitin-Protein Ligases/metabolism ; Proteasome Endopeptidase Complex/metabolism ; Thalidomide/analogs & derivatives ; Thalidomide/chemistry ; Thalidomide/pharmacology ; Phosphorylation/drug effects ; Benzothiazoles/chemistry ; Benzothiazoles/pharmacology ; Models, Molecular ; Proteolysis Targeting Chimera ; Adaptor Proteins, Signal Transducing

Targeting Protein Tyrosine Phosphatases via PROteolysis-TArgeting Chimeras (PROTACs): Current Developments and Prospects.

Autoren: Maccari R; Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale F. Stagno d'Alcontres 31, 98166 Messina, Italy.

Quelle: Molecules (Basel, Switzerland) [Molecules] 2025 Nov 18; Vol. 30 (22). Date of Electronic Publication: 2025 Nov 18.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Protein Tyrosine Phosphatases*/antagonists & inhibitors , Protein Tyrosine Phosphatases*/metabolism , Protein Tyrosine Phosphatases*/chemistry , Enzyme Inhibitors*/chemistry , Enzyme Inhibitors*/pharmacology, Humans ; Animals ; Proteolysis Targeting Chimera

PROTACs in cancer immunotherapy: a minireview.

Autoren: J E K E S CA E T C et al.

Quelle: Biochemical Society transactions [Biochem Soc Trans] 2025 Oct 29; Vol. 53 (5), pp. 1273-1281.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Portland Press On The Behalf Of The Biochemical Society Country of Publication: England NLM ID: 7506897 Publication Model: Print Cited Medium: Internet ISSN: 1470-8752 (Electronic) Linking ISSN: 03005127 NLM ISO Abbreviation: Biochem Soc Trans Subsets: MEDLINE

MeSH-Schlagworte: Neoplasms*/therapy , Neoplasms*/immunology , Immunotherapy*/methods , Proteolysis*/drug effects, Humans ; Animals ; Proteolysis Targeting Chimera

Phosphorothioate-Modified DNA Aptamer-Based PROTACs for Targeted Degradation of Estrogen Receptor α.

Autoren: Watanabe D Terauchi H Osawa H et al.

Quelle: Bioconjugate chemistry [Bioconjug Chem] 2025 Oct 15; Vol. 36 (10), pp. 2172-2180. Date of Electronic Publication: 2025 Sep 09.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9010319 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4812 (Electronic) Linking ISSN: 10431802 NLM ISO Abbreviation: Bioconjug Chem Subsets: MEDLINE

MeSH-Schlagworte: Aptamers, Nucleotide*/chemistry , Aptamers, Nucleotide*/metabolism , Estrogen Receptor alpha*/metabolism , Proteolysis*/drug effects , Phosphorothioate Oligonucleotides*/chemistry , Phosphorothioate Oligonucleotides*/metabolism, Humans ; MCF-7 Cells ; Click Chemistry ; Proteolysis Targeting Chimera

Indolequinone-Based Hypoxia-Activated Proteolysis Targeting Chimeras Selectively Degrade BRD4 in Hypoxic Cancer Cells.

Autoren: Serafini M Twigger SA Delfas G et al.

Quelle: Journal of the American Chemical Society [J Am Chem Soc] 2025 Oct 08; Vol. 147 (40), pp. 36352-36364. Date of Electronic Publication: 2025 Sep 24.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: American Chemical Society Country of Publication: United States NLM ID: 7503056 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-5126 (Electronic) Linking ISSN: 00027863 NLM ISO Abbreviation: J Am Chem Soc Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Cell Cycle Proteins*/metabolism , Transcription Factors*/metabolism , Transcription Factors*/antagonists & inhibitors , Indolequinones*/chemistry , Indolequinones*/pharmacology, Humans ; Cell Line, Tumor ; Von Hippel-Lindau Tumor Suppressor Protein/metabolism ; Ubiquitin-Protein Ligases/metabolism ; Cell Hypoxia/drug effects ; Proteolysis Targeting Chimera ; Bromodomain Containing Proteins ; Adaptor Proteins, Signal Transducing

Advances in light-activated PROTACs and phototherapy-combined approaches for cancer treatment.

Autoren: Zhang W Li S Yuan H et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2026 Jan 15; Vol. 302 (Pt 1), pp. 118310. Date of Electronic Publication: 2025 Oct 26.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Neoplasms*/drug therapy , Neoplasms*/therapy , Neoplasms*/metabolism , Neoplasms*/pathology , Phototherapy* , Light* , Proteolysis*/drug effects , Proteolysis*/radiation effects , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry, Humans ; Animals ; Cell Proliferation/drug effects ; Molecular Structure ; Proteolysis Targeting Chimera

A double-edged sword of neo-substrate degradation in PROTACs.

Autoren: Song Z Duan C Wu M et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2026 Jan 05; Vol. 301, pp. 118253. Date of Electronic Publication: 2025 Oct 09.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Ubiquitin-Protein Ligases*/metabolism , Ubiquitin-Protein Ligases*/antagonists & inhibitors , Thalidomide*/pharmacology , Thalidomide*/chemistry, Humans ; Molecular Structure ; Animals ; Adaptor Proteins, Signal Transducing/metabolism ; Proteolysis Targeting Chimera

Mighty mini-PROTACs: an emerging class of degraders.

Autoren: Chen X Liao K Yuan J et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2026 Jan 05; Vol. 301, pp. 118202. Date of Electronic Publication: 2025 Oct 03.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Proteolysis*/drug effects , Proteasome Endopeptidase Complex*/metabolism, Humans ; Molecular Structure ; Ubiquitin-Protein Ligases/metabolism ; Ubiquitin/metabolism ; Proteolysis Targeting Chimera

Discovery of Potent Dual PROTAC Degraders Targeting BET-Kinase To Overcome FLT3 Inhibitor Resistance.

Autoren: Xiang Q Sun Y Hua H et al.

Quelle: Journal of medicinal chemistry [J Med Chem] 2025 Aug 28; Vol. 68 (16), pp. 17303-17322. Date of Electronic Publication: 2025 Aug 05.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Drug Discovery* , Drug Resistance, Neoplasm*/drug effects , fms-Like Tyrosine Kinase 3*/antagonists & inhibitors , fms-Like Tyrosine Kinase 3*/metabolism , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/chemical synthesis , Transcription Factors*/metabolism , Transcription Factors*/antagonists & inhibitors , Proteolysis Targeting Chimera*/chemical synthesis , Proteolysis Targeting Chimera*/chemistry , Proteolysis Targeting Chimera*/pharmacology, Animals ; Humans ; Mice ; Cell Cycle Proteins/metabolism ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Janus Kinase 2/metabolism ; Janus Kinase 2/antagonists & inhibitors ; Leukemia, Myeloid, Acute/drug therapy ; Proteolysis/drug effects ; Structure-Activity Relationship ; Xenograft Model Antitumor Assays ; Bromodomain Containing Proteins

HADDOCK-Guided modeling and molecular simulations of cereblon-based ternary complexes: Development of novel PROTACs for Ataxia telangiectasia and RAD3-Related (ATR) kinase.

Autoren: Sarnow AC Nassar H Alfayomy AM et al.

Quelle: Computers in biology and medicine [Comput Biol Med] 2025 Aug; Vol. 194, pp. 110570. Date of Electronic Publication: 2025 Jun 13.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Country of Publication: United States NLM ID: 1250250 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1879-0534 (Electronic) Linking ISSN: 00104825 NLM ISO Abbreviation: Comput Biol Med Subsets: MEDLINE

MeSH-Schlagworte: Molecular Dynamics Simulation* , Ubiquitin-Protein Ligases*/chemistry , Ubiquitin-Protein Ligases*/metabolism , Molecular Docking Simulation* , Proteolysis* , Adaptor Proteins, Signal Transducing*/chemistry , Adaptor Proteins, Signal Transducing*/metabolism , Ataxia Telangiectasia Mutated Proteins*/chemistry , Ataxia Telangiectasia Mutated Proteins*/metabolism, Humans ; Cell Cycle Proteins/chemistry ; Proteolysis Targeting Chimera

Advancements in Proteolysis Targeting Chimeras for Targeted Therapeutic Strategies in Alzheimer's Disease.

Autoren: Zhou Q Wang W Deng C

Quelle: Molecular neurobiology [Mol Neurobiol] 2025 Aug; Vol. 62 (8), pp. 9686-9709. Date of Electronic Publication: 2025 Mar 25.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Humana Press Country of Publication: United States NLM ID: 8900963 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1559-1182 (Electronic) Linking ISSN: 08937648 NLM ISO Abbreviation: Mol Neurobiol Subsets: MEDLINE

MeSH-Schlagworte: Alzheimer Disease*/metabolism , Alzheimer Disease*/drug therapy , Proteolysis*/drug effects , Molecular Targeted Therapy*/methods, Humans ; Animals ; tau Proteins/metabolism ; Amyloid beta-Peptides/metabolism ; Proteolysis Targeting Chimera

Data-Driven Generation of Conformational Ensembles and Ternary Complexes for PROTAC and Other Chimera Systems.

Autoren: Montisci F Friggeri L Burusco-Goni KK et al.

Quelle: Journal of chemical information and modeling [J Chem Inf Model] 2025 Sep 22; Vol. 65 (18), pp. 9541-9556. Date of Electronic Publication: 2025 Sep 05.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101230060 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1549-960X (Electronic) Linking ISSN: 15499596 NLM ISO Abbreviation: J Chem Inf Model Subsets: MEDLINE

MeSH-Schlagworte: Protein Conformation* , Proteolysis Targeting Chimera*/chemistry, Databases, Protein ; Models, Molecular ; Proteolysis ; Ubiquitin-Protein Ligases/chemistry