Research Areas
The research focus of the group is new drug discovery via employing natural product chemistry, rational drug design, and medicinal chemistry approaches followed by a detailed preclinical (in-vitro/ in-vivo) characterization of identified lead compounds.
"Kinase" Targeted Medicinal Chemistry
Small molecule-based drug discovery is among the most fascinating areas of research. Nature-derived small molecules ‘natural products’ have extensively served as starting points for the discovery of drugs for a variety of therapeutic indications. Many natural products, themselves have also become successful drugs and are in therapeutic use for many diseases. Our group is particularly interested in exploring the potential of natural products in discovering new preclinical leads through a target-based approach. Targeted drug design has been the focus in the modern era of drug discovery inherently because of the advances in disease biology. The post-translational modifications (PTMs) play a vital role in the functional diversity of the proteome and many biological pathways get activated via PTMs. Phosphorylation is one of the vital PTM that occurs in a large number of proteins and this event is carried out by kinases. Several pathways in cancer progression and metastasis are regulated by kinases as key players. Thus, targeting these pathways via small molecules has emerged as a vital therapeutic strategy in cancer drug discovery. On the other side, there is a perceived difficulty in selectively targeting a specific kinase without affecting several other kinases (overall, 519 kinases are encoded in the human genome), due to the conservation of the ATP binding pocket of most kinases. However, a desirable level of selectivity has been achieved by several candidates through rational drug design and many small molecules (>70) are in therapeutic use today.
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Our group is interested in exploring the natural products (NPs) or NP pharmacophores for medicinal chemistry targeted as kinases to discover potential leads for cancer drug discovery and preclinical development. The particular interest is to discover selective / isoform-selective kinase inhibitors as potential leads for preclinical development.
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Areas of our research:
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a) Targeting cyclin-dependent kinases to discover anticancer leads
b) Identifying isoform-selective PI3K-alpha inhibitors for cancer treatment
c) Discovering kinase inhibitors for cancer immunotherapy
d) Targeting kinases involved in viral replication as potential antiviral therapeutics
e) Targeting tau-kinases as potential anti-Alzheimer's therapeutics
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Achievements from translational research:​
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1. Investigational New Drug (IND) Application filed to Central Drugs Standard Control Organization (CDSCO) for a Small Molecule Lead, IIIM-290 to conduct Phase I/II Clinical Trial in Metastatic Pancreatic Cancer Patients. IND application approved.
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2. Investigational New Drug (IND) Application filed to Central Drugs Standard Control Organization (CDSCO) for a Phytopharmaceutical Lead, IIIM-160 (dual inhibitor of IL-6 and pain) to conduct Phase I Clinical Trial in Healthy Volunteers
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3. Nutraceutical lead, IIIM-141, a multi-targeted anti-Alzheimer's lead licensed to the industry
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4. Nutraceutical lead, IIIM-160, a dual inhibitor of IL-6/ pain for management of pain in rheumatoid arthritis licensed to the industry.
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Click here for our selected publications on kinase inhibitors.
