Artikel ; Online: CYP1B1: A Promising Target in Cancer Drug Discovery.
Anti-cancer agents in medicinal chemistry
2023 Band 23, Heft 9, Seite(n) 981–988
Abstract: CYP1B1 plays an essential role in cancer's pathogenesis since it activates procarcinogens. Significantly, this enzyme catalyzes the hydroxylation of 17β-estradiol, leading to carcinogenic metabolites involved in carcinogenesis and cancer progression. ... ...
Abstract | CYP1B1 plays an essential role in cancer's pathogenesis since it activates procarcinogens. Significantly, this enzyme catalyzes the hydroxylation of 17β-estradiol, leading to carcinogenic metabolites involved in carcinogenesis and cancer progression. Therefore, the inhibition of CYP1B1 activity is considered a therapeutic target for chemotherapy. In addition, CYP1B1 is overexpressed in hormone-dependent cancer cells and could be related to resistance to anticancer drugs. However, the activity of CYP1B1 in the tumor microenvironment can metabolize and activate prodrugs in cancer cells, providing more selectivity and being useful for chemoprevention or chemotherapy strategies. Furthermore, due to its importance in anticancer drug design, recent studies have reported using computational methods to understand the intermolecular interactions between possible ligands and CYP1B1. Therefore, in this perspective, we highlight recent findings in developing CYP1B1 inhibitors (flavonoids, trans-stilbenes, estradiol derivatives, and carbazoles) and CYP1B1-activated prodrugs (a chalcone DMU-135 and an oxime DMAKO-20). Finally, we have analyzed their possible molecular interactions with this enzymatic target by molecular docking, which can help to design new active substances. |
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Mesh-Begriff(e) | Humans ; Cytochrome P-450 CYP1A1/metabolism ; Molecular Docking Simulation ; Prodrugs/pharmacology ; Cytochrome P-450 CYP1B1 ; Antineoplastic Agents/pharmacology ; Neoplasms/drug therapy ; Carcinogenesis ; Drug Discovery ; Estradiol ; Tumor Microenvironment |
Chemische Substanzen | Cytochrome P-450 CYP1A1 (EC 1.14.14.1) ; Prodrugs ; Cytochrome P-450 CYP1B1 (EC 1.14.14.1) ; Antineoplastic Agents ; Estradiol (4TI98Z838E) ; CYP1B1 protein, human (EC 1.14.14.1) |
Sprache | Englisch |
Erscheinungsdatum | 2023-01-09 |
Erscheinungsland | Netherlands |
Dokumenttyp | Journal Article ; Research Support, Non-U.S. Gov't |
ZDB-ID | 2217610-X |
ISSN | 1875-5992 ; 1871-5206 |
ISSN (online) | 1875-5992 |
ISSN | 1871-5206 |
DOI | 10.2174/1871520623666230119103914 |
Datenquelle | MEDical Literature Analysis and Retrieval System OnLINE |
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