Amit Shard

Design and Synthesis of Novel Quinazolinone-Based Pyruvate Kinase M2 Activators as Selective Inhibitors of Oral Cancer Cells

Bhagyashri Rathod, Swarali Joshi, Siddulu Regu, K.V.N.S. Manikanta, Hansal Kumar, S. Dubey, et al.

Also available via: RELX Group (Netherlands)

Novel imidazopyrimidines-based molecules induce tetramerization of tumor pyruvate kinase M2 and exhibit potent antiproliferative profile

Sagarkumar Patel, Christoph Globisch, Priyanka Pulugu, Prasoon Kumar, Alok Jain, Amit Shard

Discovery of novel and potent lead molecules for the specific therapeutic targets by de novo drug design is still in infancy. Here, we disclose the unprecedented development of imidazopyri(mi)dine-based tumor pyruvate kinase M2 (PKM2) modulators by subsequent link and grow strate…Read more

Also available via: Elsevier BV

Discovery of boronic acid-based potent activators of tumor pyruvate kinase M2 and development of gastroretentive nanoformulation for oral dosing

Rajkumar Patle, Shital Shinde, Sagarkumar Patel, Rahul Maheshwari, Heena Jariyal, Akshay Srivastava, et al.

Also available via: Elsevier BV

Pyruvate kinase M2 in chronic inflammations: a potpourri of crucial protein–protein interactions

Sagarkumar Patel, Anwesha Das, Payal Meshram, Ayushi Sharma, Arnab Chowdhury, Heena Jariyal, et al.

Chronic inflammation (CI) is a primary contributing factor involved in multiple diseases like cancer, stroke, diabetes, Alzheimer's disease, allergy, asthma, autoimmune diseases, coeliac disease, glomerulonephritis, sepsis, hepatitis, inflammatory bowel disease, reperfusion injur…Read more

Also available via: Springer Science+Business Media

Metabolite profiling of IMID‐2, a novel anticancer molecule of piperazine derivative: <i>In silico</i> prediction, <i>in vitro</i> and <i>in vivo</i> metabolite characterization using UPLC–QTOF–MS/MS

Niraj Kumar Panday, Disha Thakkar, Sagarkumar Patel, Amit Shard, Pinaki Sengupta

IMID-2, a newly identified piperazine-based anticancer molecule, has been shown to be cytotoxic against various cancer cell lines. The primary aim of this research was to identify and characterize possible metabolites of the molecule formed during biotransformation. A metabolite…Read more

Also available via: Wiley

Tumor pyruvate kinase M2 modulators: a comprehensive account of activators and inhibitors as anticancer agents

Bhagyashri Rathod, Shivam Chak, Sagarkumar Patel, Amit Shard

Pyruvate kinase M2 (PKM2) catalyzes the conversion of phosphoenolpyruvate (PEP) to pyruvate. It plays a central role in the metabolic reprogramming of cancer cells and is expressed in most human tumors. It is essential in indiscriminate proliferation, survival, and tackling apopt…Read more

Also available via: Royal Society of Chemistry