#CTDDR2022: The 8th maha sangam for drug research

New Delhi: The 8th International Symposium on Current Trends in Drug Discovery Research held recently at CSIR-Central Drug Research Institute, Lucknow observed very important scientific sessions on “Biased GPCR Signaling: Road to Better Therapeutics and another session on Synthetic Biology and Medicinal Chemistry for Drug Discovery”

GPCRs couple to multiple intracellular signalling pathways and currently more than 50 per cent of approved medications target GPCRs: Dr. Bryan Roth

Dr. Bryan Roth, Michael Hooker Distinguished Professor, Director, NIMH Psychoactive Drug Screening Program delivered an interesting talk on Structural Insights into GPCRs: Accelerating Structure-Guided Drug Discovery. G protein-coupled receptors (GPCRs) are widely distributed in the human body and trigger cellular responses to a variety of extracellular stimuli. The diverse functions of GPCRs make these receptors key players in numerous physiological regulations and valuable drug targets for many diseases. Dr Bryan Roth discussed about psychedelic or hallucinogenic drugs such as LSD. His research leads to understand how these drugs work against anxiety and also about their side effects. He is the pioneer to solve the structures of receptors where these drugs bind. He is currently working to develop anti-depressant with non-psychedelic effect to develop safer treatment.

Schizophrenia is a serious mental disorder that affects a person’s ability to think, feel and behave clearly: Dr. Celine

Dr. Celine Valant from Drug Discovery Biology, Monash University, Australia is working on a drug xanomeline which has entered Phase III clinical trials for the treatment of schizophrenia. Schizophrenia is a serious mental disorder that affects a person’s ability to think, feel and behave clearly. If successful, xanomeline will be the first novel FDA-approved antipsychotic drug in almost 50 years. Her research is to understand the therapeutic action of xanomeline in schizophrenia.

Activation, signalling and regulation of GPCRs and ACRs have crucial role in therapeutic implications of human diseases Prof. Arun Shukla

Prof. Arun Shukla from IIT, Kanpur shed light on intrinsic bias at non-canonical seven transmembrane receptors. His elaborative talk was aimed to explore the structural basis of activation and signalling of selected non-canonical GPCRs and ultimately, leverage this information to improve therapeutic manipulation in human diseases. As these transmembrane receptors play significant role used in congestive heart failure, hypertension, asthma, allergies, schizophrenia, Parkinson’s disease and cancer.

Cathepsin S Inhibitors may be useful in treatment of Abdominal Aortic Aneurysm (AAA): Dr. Prabhakar

Later in session focused on Synthetic Biology and Medicinal Chemistry for Drug Discovery, Dr. Prabhakar K Jadhav from Minghui Pharmaceutical (Shanghai) Ltd, USA delivered a talk on “Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm (AAA)”. An abdominal aortic aneurysm can be life-threatening if it bursts. It is most common in older men and smokers. The enlargement of the aorta (the main blood vessel that delivers blood to the body), at the level of the abdomen usually happens during the disease. An AAA often grows slowly, without symptoms. As it grows, some people may notice a pulsating feeling near the navel. Pain in the back, stomach or side may be signs of impending rupture. Dr. Prabhakar in his talk showed how the Cathepsin S Inhibitors act in reducing the aorta for improving the Abdominal Aortic Aneurysm. Cathepsin S is a protein increased in human AAA lesions and plays a critical role in AAA. His team developed a highly potent and selective cathepsin S inhibitor which currently is in clinical trials. These novel inhibitors exhibit excellent in vitro and in vivo drug-like properties.

Beta-carboline derivatives has the potential for treating chronic pain: Dr Sanjay Batra

Dr. Sanjay Batra, CSIR-CDRI, Lucknow, shred his resent research on potential use of beta-carboline derivatives as agents for treating pain. Natural beta (β)-carbolines primarily influence brain functions but can also exhibit antioxidant effects. Synthetically designed β-carboline derivatives have recently been shown to have neuroprotective, cognitive enhancing and anti-cancer properties to add on this, Dr. Batra shared his recent research establishing the potential use of these derivatives for treatment of pain with their analgesic effects.

The CTDDR 2022 was concluded with the brain storming panel discussion by the stalwarts on “Challenges & Opportunities in Drug Discovery”

Prof. T.K. Chakraborty, IISc, Bengaluru, Dr. Murali Ramchandra, Aurigene Discovery Technologies, Bengaluru, Prof. Tapas. K. Kundu, JNCASR, Bengaluru and Dr. T. Rajamannar, SPARC, Baroda and Dr. D.S. Reddy, CSIR-CDRI, Lucknow were the panellist and Dr. Ram Vishwakarma, CSIR, Eminent Scientist, Chaired the panel discussion. As India has become the Pharmacy of the world but the status of drug discovery and development status is under development stage. There is an urgent need to improve the collaboration between Industry and Academia, not only nation wise but globally. Dr. Ram, emphasized to break the boundaries for making collaboration with the industry globally.

At the end of the session the valedictory function was organized and the young budding scientists were felicitated with best poster awards and best flash talk award. The symposium was concluded with the vote of thanks by Dr. P.N. Yadav and Dr. Dipankar Koley, the organizing secretory and co-organizing secretory.