20–21 Jan 2022
Birla Institute of Technology
Asia/Kolkata timezone

Identification of newer hits as potential FAK inhibitors using in-silico methods

Not scheduled
10m
Birla Institute of Technology

Birla Institute of Technology

Mesra, Ranchi 835 215, Jharkhand, India
Oral Presentation Pharmaceutical Chemistry Poster Presentations

Speaker

Sahaya Nadar (St. John Institute of Pharmacy and Research, Palghar)

Description

Focal adhesion kinase (FAK), a protein tyrosine kinase, has been overexpressed in cancer cells and plays a pivotal role in the proliferation of tumor malignancy. There is no FDA-approved and marketed the drug as FAK inhibitor for clinical use by far. This calls for a dire need to advance an area of active FAK inhibitors as possible anticancer entities. In the present study, applying appropriate filters in the ZINC database, 631 compounds were selected and virtually screened using Autodock Vina in PyRx 0.8. Further, Lipinski’s Rule of Five (Ro5) was applied on the best hits identified through molecular docking studies to find their drug-likeness using SwissADME. The compounds were further screened for their toxicity by Pro Tox II. Our analysis identified four hits, compounds ZINC95595125, ZINC43200601, ZINC40395224, and ZINC95593660, which exhibited an excellent binding score along with passing the ADMET evaluations making these ligands a primary choice to be tested experimentally. The identified hits displayed good crucial interaction with the FAK enzyme (PBD ID: 2ETM) and can be considered as potential leads. Further in-vitro and in-vivo anticancer activity against selected cell lines in which FAK are overexpressed can be carried out for these identified compounds.

Primary author

Sahaya Nadar (St. John Institute of Pharmacy and Research, Palghar)

Co-author

Tabassum Khan (Dr. Bhanuben Nanavati College of Pharmacy, Mumbai)

Presentation materials