Title : G9a inhibition by CM-272: Developing a novel anti-tumoral strategy for castration-resistant prostate cancer using 2D and 3D in vitro models.

Pub. Date : 2022 Jun

PMID : 35483199






6 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 G9a inhibition by CM-272: Developing a novel anti-tumoral strategy for castration-resistant prostate cancer using 2D and 3D in vitro models. CM-272 euchromatic histone lysine methyltransferase 2 Homo sapiens
2 We disclose that, under the evaluated dose, CM-272 led to G9a activity inhibition, while not significantly affecting DNMT1 activity. CM-272 euchromatic histone lysine methyltransferase 2 Homo sapiens
3 Contrarily, PC3 cell viability impact was higher in G9a knockdown, compared with CM-272 treatment, suggesting an additional G9a function. CM-272 euchromatic histone lysine methyltransferase 2 Homo sapiens
4 Moreover, DU145 cells overexpressing catalytically functional G9a disclosed higher resistance to CM-272 treatment, reinforcing that the drug mechanism of action is dependent on G9a catalytic function. CM-272 euchromatic histone lysine methyltransferase 2 Homo sapiens
5 Moreover, DU145 cells overexpressing catalytically functional G9a disclosed higher resistance to CM-272 treatment, reinforcing that the drug mechanism of action is dependent on G9a catalytic function. CM-272 euchromatic histone lysine methyltransferase 2 Homo sapiens
6 We concluded that inhibition of G9a methyltransferase activity by CM-272 has anti-tumor effect in PCa cells, holding therapeutic potential against CRPC. CM-272 euchromatic histone lysine methyltransferase 2 Homo sapiens