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 remains one of the most fascinating and impactful areas of research. Natural products—small molecules derived from nature—have historically served as crucial starting points for drug discovery across a variety of therapeutic indications. Many natural products have themselves evolved into successful drugs and continue to play a significant role in treating a wide range of diseases.
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Our group is particularly interested in leveraging the potential of natural products to discover new preclinical leads using a target-based approach. The focus on targeted drug design has become prominent in the modern era of drug discovery, largely driven by major advances in understanding disease biology. Among the mechanisms of interest are post-translational modifications (PTMs), which play a pivotal role in expanding the functional diversity of the proteome and regulating key biological pathways. Phosphorylation, one of the most critical PTMs, is mediated by kinases and occurs in a vast number of proteins. Kinases regulate several signaling pathways that drive cancer progression and metastasis, making them prime targets for cancer drug discovery. However, selectively targeting a specific kinase without affecting others has been a significant challenge, mainly due to the high conservation of the ATP-binding pocket across the human kinome (comprising 519 kinases).
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Despite these challenges, rational drug design efforts have successfully achieved desirable levels of kinase selectivity. Today, more than 70 small-molecule kinase inhibitors have been approved for therapeutic use, underscoring the viability and importance of this strategy. The research within our group is focused on exploring natural products (NPs) and NP-derived pharmacophores for medicinal chemistry efforts targeting kinases, with the aim of discovering potential leads for cancer drug discovery and preclinical development. We are particularly interested in identifying selective or isoform-selective kinase inhibitors as promising candidates for further preclinical advancement.
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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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Translational Outcomes:​
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​IND's filed:
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. Investigational New Drug (IND) Application filed to Central Drugs Standard Control Organization (CDSCO) for a Phytopharmaceutical Lead, IIIM-141 (a multitargeted lead for Alzheimeir's disease) to conduct Phase I Clinical Trial in Healthy Volunteers
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Products Out-licensed:
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4. Nutraceutical lead, IIIM-141, a multi-targeted anti-Alzheimer's lead licensed to the industry
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5. 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.
