2. Academic Validation
  3. Targeting TRAIL

Targeting TRAIL

  • Bioorg Med Chem Lett. 2019 Sep 15;29(18):2527-2534. doi: 10.1016/j.bmcl.2019.07.053.
George Nicolae Daniel Ion 1,  George Mihai Nitulescu 2,  Costin Ioan Popescu 3
Affiliations

Affiliations

  • 1 Carol Davila University of Medicine and Pharmacy, Traian Vuia 6, Bucharest 020956, Romania.
  • 2 Carol Davila University of Medicine and Pharmacy, Traian Vuia 6, Bucharest 020956, Romania. Electronic address: george.nitulescu@umfcd.ro.
  • 3 Institute of Biochemistry of the Romanian Academy, Splaiul Independentei 296, Bucharest 600031, Romania.
PMID: 31383590 DOI: 10.1016/j.bmcl.2019.07.053
Abstract

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), also known as Apo2L, has been investigated in the past decade for its promising Anticancer activity due to its ability to selectively induce Apoptosis in tumoral cells by binding to TRAIL receptors (TRAIL-R). Macromolecules such as agonistic monoclonal Antibodies and recombinant TRAIL have not proven efficacious in clinical studies, therefore several small molecules acting as TRAIL-R agonists are emerging in the scientific literature. In this work we focus on systemizing these drug molecules described in the past years, in order to better understand and predict the requirements for a novel anti-tumoral therapy based on the TRAIL-R-induced apoptotic mechanism.

Keywords

Anti-tumoral; Apoptosis; Cancer; Death receptor; TRAIL.

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