Research

Medical Sciences

Title :

Identification and characterization of small molecules to block PD1/PDL1 pathway in immunotherapy

Area of Research :

Medical Sciences

Focus Area :

Cancer Immunotherapy, Drug Discovery

Principal Investigator :

Dr. Amit Awasthi, Translational Health Science and Technology Institute (THSTI), Faridabad, Haryana; Dr. Pranjal Gogoi, CSIR- North East Institute of Science and Technology (NEIST), Jorhat, Assam

Co-PI:

Dr. Shailendra Asthana, Translational Health Science and Technology Institute (THSTI), Faridabad, Haryana

Contact info :

Timeline Start Year :

2022

Timeline End Year :

2025

Total Budget (INR):

63,.3,552

Details

Executive Summary :

Blocking the interactions between programmed cell death protein 1 (PD-1) and its ligand, PD-L1, has emerged as a promising immunotherapy for treating cancer. Cancer immunotherapy harnesses the immune system to battle tumors: it directly targets the immune system rather than the tumors [3,4]. An immune checkpoint is a molecule in the immune system that either enhances (co-stimulatory molecules) or inhibits a signal [5,6]. The blockade of immune checkpoints can activate therapeutic antitumor immunity. There are currently several mAbs approved for the treatment of cancers as an effective target for cancer immunotherapy and clinical results have shown that anti-PD-1 therapy is superior to chemotherapy in the treatment of metastatic melanoma. There are some disadvantages to Ab-mediated immunotherapy too, like production cost, stability, and immunogenicity; therefore, low-molecular weight immune checkpoint inhibitors of PD-1/PD-L1 have become attractive targets in the drug discovery.

Equipments :

Achievements :

Indazole and triazole-based small molecules were shortlisted for synthesis. Compounds identified by targeting the binding site were evaluated in in-vitro assays. After completion of analysis Indian patent will file.All the synthesized compounds were characterized using NMR and HRMS analysis. Additionally, the purity of our synthesized compounds was evaluated using HPLC. Photophysical properties, including absorption, emission, and quantum yields, were also evaluated.

Outcome/Output:

1

Organizations involved