Proteolysis Targeting Chimera

Bifunctional molecules that are designed to recruit E3 UBIQUITIN LIGASE to a specific target protein. Proteolysis targeting chimera consist of a target protein ligand connected via a linker to an E3 ligand. They promote association of E3 with specific target proteins tagged for degradation via the PROTEASOME.

Also Known As:

Cereblon Based Small Molecule Compounds; Chimeras, Proteolysis Targeting; IAP Based PROTACs; MDM2 Protein Based PROTACs; Phospho Dependent PROTACs; Targeting Chimeras, Proteolysis; VHL Based PROTACs; Cereblon-Based Small-Molecule Compounds; IAP-Based PROTACs; MDM2 Protein-Based PROTACs; PROTAC Proteolysis Targeting Chimera; PROTACs; Phospho-Dependent PROTACs; PhosphoPROTACs; Proteolysis Targeting Chimeras; VHL-Based PROTACs

Networked: 364 relevant articles (25 outcomes, 45 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Specialty Uses of Chemicals
  - Laboratory Chemicals: 1
    - Indicators and Reagents: 59418
      - Cross-Linking Reagents: 45
        Proteolysis Targeting Chimera: 364

Experts

1.	Zheng, Guangrong: 10 articles (01/2022 - 01/2020)
2.	Zhou, Daohong: 9 articles (01/2022 - 01/2020)
3.	Khan, Sajid: 8 articles (01/2022 - 01/2020)
4.	Zhang, Xuan: 8 articles (01/2022 - 01/2020)
5.	Zhang, Peiyi: 7 articles (01/2022 - 01/2020)
6.	Liu, Jing: 6 articles (11/2022 - 12/2020)
7.	Wei, Wenyi: 6 articles (11/2022 - 12/2020)
8.	Ocaña, Alberto: 6 articles (01/2022 - 08/2019)
9.	Thummuri, Dinesh: 5 articles (01/2022 - 01/2020)
10.	Wang, Shaomeng: 5 articles (12/2021 - 08/2018)

Related Diseases

1.	Neoplasms (Cancer) 01/01/2023 - "Benefiting from the GSH-scavenging ability to amply the c-Myc-related ferroptosis and cell cycle arrest, this ARV@PDSA Nano-PROTACs strategy shows superior anti-tumor efficacy with a low dose administration and good biocompatibility in vivo. " 10/01/2022 - "Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations." 01/01/2022 - "PROTACs specific for a number of known cancer targets have been developed in the last 5 years, which present new options for remission in patients with previously untreatable malignancies and provide a foundation for future-generation compounds. " 01/01/2020 - "PROTACs have been developed to degrade a variety of cancer targets with unprecedented efficacy against a multitude of tumor types. " 11/13/2023 - "This technology is emerging as an exciting new avenue for therapeutic development, with several PROTACs currently undergoing clinical trials targeting cancer. "
2.	Breast Neoplasms (Breast Cancer) 11/08/2023 - "This study provides a potentially valuable strategy for breast cancer treatment using tumor microenvironment-responsive PROTACs." 01/01/2022 - "PROTACs: A Hope for Breast Cancer Patients?" 01/01/2021 - "Proteolysis-targeting chimeras and their implications in breast cancer." 10/19/2020 - "Controlled Delivery of BET-PROTACs: In Vitro Evaluation of MZ1-Loaded Polymeric Antibody Conjugated Nanoparticles in Breast Cancer." 12/01/2020 - "Proteolysis-targeting chimeras in breast cancer therapy."
3.	Hematologic Neoplasms (Hematological Malignancy) 01/01/2022 - "More PROTACs will enter clinical trials soon, benefiting patients with hematologic malignancies." 01/01/2021 - "Preclinical Studies of PROTACs in Hematological Malignancies." 01/01/2020 - "These studies provide "proof of principle" that targeting CDK6 with PROTACs that inhibit its enzymatic activity and promote its degradation represents an effective strategy to exploit the "CDK6 dependence" of Ph+ ALL and, perhaps, of other hematologic malignancies. " 01/01/2023 - "In this review, we provide a comprehensive summary of the recent advances in the development of PROTACs as therapeutic strategies in diverse hematological malignancies. " 01/01/2023 - "PROTACs: Walking through hematological malignancies."
4.	Prostatic Neoplasms (Prostate Cancer) 10/28/2022 - "Overall, this study reports a previously unappreciated requirement for EZH2TAD for mediating EZH2's non-canonical (co-)activator recruitment and gene activation functions in prostate cancer and suggests EZH2-targeting PROTACs as a potentially attractive therapeutic for the treatment of aggressive prostate cancer that rely on the circuits wired by EZH2 and AR." 04/25/2023 - "The present review highlights an overview of PROTACs in prostate cancer and their superiority over conventional inhibitors. " 04/25/2023 - "PROTACs in the Management of Prostate Cancer." 01/01/2023 - "PROTACs for prostate cancer." 01/01/2022 - "The destructive power of PROTACs could tackle prostate cancer."
5.	Hypoxia (Hypoxemia) 01/01/2023 - "Bioactivity studies showed that these hypoxia-responsive PROTACs exhibited excellent hypoxic responsiveness and ERα degradation activity under hypoxic conditions, and thus improved the toxic effects of the active PROTAC in normal cells. " 12/14/2022 - "Hypoxia deactivates epigenetic feedbacks via enzyme-derived clicking proteolysis-targeting chimeras." 01/01/2022 - "We categorize these activatable PROTACs according to their activation mechanism contributed by different stimuli, including reduction-activatable, hypoxia-activatable, and enzyme-activatable PROTACs and photo-caged or photo-switchable PROTACs. " 11/30/2021 - "Here we report the identification of a kind of hypoxia-activated proteolysis targeting chimera (ha-PROTAC) by introducing the hypoxia-activated leaving group (1-methyl-2-nitro-1H-imidazol-5-yl)methyl or 4-nitrobenzyl into the structure of an EGFRDel19-based PROTAC. " 07/05/2010 - "The ER-targeting PROTACs are composed of an estradiol on one end and a hypoxia-inducing factor 1alpha (HIF-1alpha)-derived synthetic pentapeptide on the other. "

Related Drugs and Biologics

1.	snake venom protein C activator
2.	Proteolysis Targeting Chimera
3.	Proteins (Proteins, Gene)
4.	Ubiquitin-Protein Ligases (Ubiquitin-Protein Ligase)
5.	Peptides (Polypeptides)
6.	ARV-825
7.	Phosphates (Orthophosphate)
8.	Phosphoric Monoester Hydrolases (Phosphatases)
9.	Fluorine
10.	Ligands

Related Therapies and Procedures

1.	Therapeutics
2.	Immunotherapy
3.	Vascularized Composite Allotransplantation
4.	Injections
5.	Drug Therapy (Chemotherapy)