Therapeutic natural compounds enzastaurin and palbociclib inhibit | 60650
Journal of Cell Science & Therapy

Journal of Cell Science & Therapy
Open Access

ISSN: 2157-7013

Therapeutic natural compounds enzastaurin and palbociclib inhibit MASTL kinase activity preventing breast cancer cell proliferation

Global Conference on Cell and Gene Therapy - July 04, 2022 | Webinar

July 04, 2022 | Webinar

Gauri Misra

National Institute of Biologicals, India

Scientific Tracks Abstracts: J Cell Sci Therapy

Abstract :

The present study is focused on the identification of new MASTL inhibitors from natural sources. The Enzastaurin and Palbociclib were some of the leads obtained from our previous in silico work that are from natural source and have been validated as MASTL kinase inhibitors using in vitro kinase assay in the present study. These compounds will be less toxic to the normal cells. The development of new anticncer drugs has been recently recieving a lot of attention and Microtubuleassociated serine/threonine kinase-like (MASTL) remains to be one such attractive target that also regulates mitotic progression. In this study, novel inhibitory molecules were screened against MASTL kinase, a protein involved in cell proliferation in breast cancer. Enzastaurin and Palbociclib, being natural source-derived drugs were selectively used to identify their role as MASTL kinase inhibitors. Human breast cancer (MCF-7) cells were used to evaluate the cytotoxic activity, kinase activity, and other cell-based assays of Enzastaurin and Palbociclib. Cytotoxicity in MCF-7 cells was caused by the potential natural compounds in a dose- and time-dependent manner. Further analysis by Annexin V and PI staining indicated that both drugs are potent inducers of apoptosis. Enzastaurin induced G2/M phase arrest, while Palbociclib caused G1 arrest. MASTL kinase activity was significantly abrogated with both the compounds showing EC50 values of 17.13 μM and 10.51 μM, respectively. In this study, we have validated naturally derived compounds Enzastaurin and Palbociclib as novel MASTL kinase inhibitors with significant antitumor effect as potential therapeutic leads against breast cancer using cell based studies.

Biography :

Gauri Misra is currently working as a Scientist Grade II at the prestigious National Institute of Biologicals which is an apex autonomus institute under the administrative control of Ministry of Health and Family welfare, Government of India. Here, she leads the COVID-19 Kit testing laboratory and the Molecular Diagnostics Laboratory. She is the pioneer for initiating a number of research projects and funds. She has been the recipient of many awards including the Eli-Lilly Asia Outstanding Thesis Award (first prize) in 2009 and best oral presentation award at the “National Seminar on Crystallography-37”. She was selected as visiting Scientist under the INSA bilateral exchange program to visit the Israel Structural Proteomics Center situated at Weizmann Institute of Science, Rehovot, Israel, in 2014. She is serving as reviewer for various prestigious international journals. Furthermore, she is member of many scientific societies including the Indian Biophysical Society, Indian Science Congress Association and Indian Crystallographic Association. Till date, she has authored and co-authored 21 research articles in peer-reviewed journals of impact, 05 International books and 06 book chapters. She has been invited as a speaker at various prestigious institutions to share her knowledge.