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Academic Journal

Discovery of potent hypoxia-inducible factor-1α (HIF-1α) degraders by proteolysis targeting chimera (PROTAC).

  • Authors : Li Y; School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China; Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China.

Subjects: Hypoxia-Inducible Factor 1, alpha Subunit*/Hypoxia-Inducible Factor 1, alpha Subunit*/Hypoxia-Inducible Factor 1, alpha Subunit*/metabolism ; Hypoxia-Inducible Factor 1, alpha Subunit*/Hypoxia-Inducible Factor 1, alpha Subunit*/Hypoxia-Inducible Factor 1, alpha Subunit*/antagonists & inhibitors ; Proteolysis*/Proteolysis*/Proteolysis*/drug effects

  • Source: Bioorganic chemistry [Bioorg Chem] 2024 Dec; Vol. 153, pp. 107943. Date of Electronic Publication: 2024 Nov 04.Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN:

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Academic Journal

Development of miRNA-based PROTACs targeting Lin28 for breast cancer therapy.

  • Authors : Xu J; State Key Laboratory of Natural and Biomimetic Drugs, Chemical Biology Center and School of Pharmaceutical Sciences, Peking University, Xueyuan Rd, Beijing 100191, China.; Zhao X

Subjects: MicroRNAs*/MicroRNAs*/MicroRNAs*/genetics ; MicroRNAs*/MicroRNAs*/MicroRNAs*/metabolism ; RNA-Binding Proteins*/RNA-Binding Proteins*/RNA-Binding Proteins*/metabolism

  • Source: Science advances [Sci Adv] 2024 Sep 20; Vol. 10 (38), pp. eadp0334. Date of Electronic Publication: 2024 Sep 18.Publisher: American Association for the Advancement of Science Country of Publication: United States NLM ID: 101653440 Publication Model: Print-Electronic

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Academic Journal

Exploration of Hydrazide-Based HDAC8 PROTACs for the Treatment of Hematological Malignancies and Solid Tumors.

  • Authors : Zhao C; Department of Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy (GRIP), University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.; Zhang J

Subjects: Histone Deacetylases*/Histone Deacetylases*/Histone Deacetylases*/metabolism ; Histone Deacetylase Inhibitors*/Histone Deacetylase Inhibitors*/Histone Deacetylase Inhibitors*/pharmacology ; Histone Deacetylase Inhibitors*/Histone Deacetylase Inhibitors*/Histone Deacetylase Inhibitors*/chemistry

  • Source: Journal of medicinal chemistry [J Med Chem] 2024 Aug 22; Vol. 67 (16), pp. 14016-14039. Date of Electronic Publication: 2024 Aug 01.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

Discovery of KW0113 as a First and Effective PROTAC Degrader of DNMT1 Protein.

  • Authors : Wang H; School of Chemistry and Chemical Engineering, Nanchang University, Nanchang, 330031, China.; Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan, 528400, China.

Subjects: DNA (Cytosine-5-)-Methyltransferase 1*/DNA (Cytosine-5-)-Methyltransferase 1*/DNA (Cytosine-5-)-Methyltransferase 1*/antagonists & inhibitors ; DNA (Cytosine-5-)-Methyltransferase 1*/DNA (Cytosine-5-)-Methyltransferase 1*/DNA (Cytosine-5-)-Methyltransferase 1*/metabolism ; Proteolysis*/Proteolysis*/Proteolysis*/drug effects

  • Source: ChemMedChem [ChemMedChem] 2024 Dec 16; Vol. 19 (24), pp. e202400467. Date of Electronic Publication: 2024 Nov 07.Publisher: Wiley-VCH Country of Publication: Germany NLM ID: 101259013 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1860-7187

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Academic Journal

Discovery of novel penetrating peptides able to target human leukemia and lymphoma for enhanced PROTAC delivery.

  • Authors : Zhang Q; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, 710061, China.; Liu Y

Subjects: Leukemia*/Leukemia*/Leukemia*/drug therapy ; Leukemia*/Leukemia*/Leukemia*/pathology ; Leukemia*/Leukemia*/Leukemia*/metabolism

  • Source: European journal of medicinal chemistry [Eur J Med Chem] 2024 Nov 05; Vol. 277, pp. 116734. Date of Electronic Publication: 2024 Jul 31.Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

Discovery of Novel PROTAC SIRT6 Degraders with Potent Efficacy against Hepatocellular Carcinoma.

  • Authors : Huang J; International Cancer Center, Guangdong Key Laboratory of Genome Instability and Human Disease Prevention, Marshall Laboratory of Biomedical Engineering, Department of Biochemistry and Molecular Biology, Health Science Centre School of Basic Medical Sciences, Shenzhen University, Shenzhen 518055, China.; Shenzhen University School of Pharmacy, Shenzhen University Medical School, Shenzhen 518055, China.

Subjects: Carcinoma, Hepatocellular*/Carcinoma, Hepatocellular*/Carcinoma, Hepatocellular*/drug therapy ; Carcinoma, Hepatocellular*/Carcinoma, Hepatocellular*/Carcinoma, Hepatocellular*/pathology ; Carcinoma, Hepatocellular*/Carcinoma, Hepatocellular*/Carcinoma, Hepatocellular*/metabolism

  • Source: Journal of medicinal chemistry [J Med Chem] 2024 Oct 10; Vol. 67 (19), pp. 17319-17349. Date of Electronic Publication: 2024 Sep 25.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

Discovery of novel EGFR-PROTACs capable of degradation of multiple EGFR-mutated proteins.

  • Authors : Du Y; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 211198, China.

Subjects: ErbB Receptors*/ErbB Receptors*/ErbB Receptors*/metabolism ; ErbB Receptors*/ErbB Receptors*/ErbB Receptors*/antagonists & inhibitors ; ErbB Receptors*/ErbB Receptors*/ErbB Receptors*/genetics

  • Source: European journal of medicinal chemistry [Eur J Med Chem] 2024 Jun 05; Vol. 272, pp. 116489. Date of Electronic Publication: 2024 May 16.Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer.

  • Authors : Chen W; Yunnan Key Laboratory of Animal Models and Human Disease Mechanisms, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650201, China; Kunming College of Life Sciences, University of Chinese Academy Sciences, Kunming 650204, China

Subjects: Breast Neoplasms*/Breast Neoplasms*/Breast Neoplasms*/drug therapy ; Breast Neoplasms*/Breast Neoplasms*/Breast Neoplasms*/pathology ; Breast Neoplasms*/Breast Neoplasms*/Breast Neoplasms*/metabolism

  • Source: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie [Biomed Pharmacother] 2024 Aug; Vol. 177, pp. 116972. Date of Electronic Publication: 2024 Jun 21.Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 8213295 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

Discovery of a potent and selective JAK1-targeting PROTAC degrader with anti-tumor activities.

  • Authors : Zhang X; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.; Wang W

Subjects: Janus Kinase 1*/Janus Kinase 1*/Janus Kinase 1*/antagonists & inhibitors ; Janus Kinase 1*/Janus Kinase 1*/Janus Kinase 1*/metabolism ; Antineoplastic Agents*/Antineoplastic Agents*/Antineoplastic Agents*/pharmacology

  • Source: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2024 Sep 01; Vol. 109, pp. 129838. Date of Electronic Publication: 2024 Jun 03.Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN:

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Academic Journal

PI3K PROTAC overcomes the lapatinib resistance in PIK3CA-mutant HER2 positive breast cancer.

  • Authors : Zhang H; Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, 650500, China; Medical School, Kunming University of Science and Technology, Kunming, 650500, China.

Subjects: Lapatinib*/Lapatinib*/Lapatinib*/pharmacology ; Breast Neoplasms*/Breast Neoplasms*/Breast Neoplasms*/drug therapy ; Breast Neoplasms*/Breast Neoplasms*/Breast Neoplasms*/genetics

  • Source: Cancer letters [Cancer Lett] 2024 Aug 28; Vol. 598, pp. 217112. Date of Electronic Publication: 2024 Jul 08.Publisher: Elsevier Science Ireland Country of Publication: Ireland NLM ID: 7600053 Publication Model: Print-Electronic Cited Medium: Internet ISSN:

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  • 1-10 of  4,052 results for ""Proteolysis""