Targeting glioblastoma with HDAC inhibitors: insights into hydroxamic acid-based therapeutic strategies
Padmini Pai, Ipshita Das, Yashaswini Reddy, Babu Santhi Venkidesh, Poonam Bhandari, Manjunath Madalageri, Veeresh Sadashivanavar, Karkala Sreedhara Ranganath Pai, Pallavi Rao, Srinivas Oruganti, Manasa Gangadhar Shetty, Kapaettu Satyamoorthy, Babitha Kampa Sundara
TL;DR
This study explores a new hydroxamic acid compound that shows promise in treating glioblastoma by targeting epigenetic regulators and inducing cancer cell death.
Contribution
A novel hydroxamic acid-based HDAC inhibitor, compound 3B, is introduced with demonstrated antitumor efficacy in glioblastoma models.
Findings
Compound 3B inhibits glioma cell proliferation and induces G2/M phase cell cycle arrest.
It increases apoptosis and reduces colony formation in glioma cells.
In vivo models show strong antitumor activity of compound 3B.
Abstract
Epigenetic modifications play crucial roles in glioblastoma growth and aggressiveness, with key regulators including histone deacetylases (HDACs), histone acetyltransferases (HATs), and methyltransferases. Targeting these epigenetic alterations has emerged as a promising therapeutic strategy, utilizing DNA methyltransferase (DNMT) inhibitors, HDAC inhibitors (HDACis), and miRNA-based therapies. HDACis, whose effect on p53, p21, Bax, and Bcl-2, have gained significant interest because of their ability to restore the expression of tumor suppressor genes, thereby inducing apoptosis and overcoming therapeutic resistance. Our study demonstrated that a novel hydroxamic acid analogue, compound 3B, effectively inhibited glioma cell (C6) proliferation and exhibited potent anticancer activity. Compound 3B induced G2/M phase cell cycle arrest, increased apoptotic cell populations, and…
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Taxonomy
TopicsHistone Deacetylase Inhibitors Research · Epigenetics and DNA Methylation · Glioma Diagnosis and Treatment