The main objective of this course is to familiarize students with the fundamental concepts of drug discovery and development. The course is intended for students who have a background in chemistry and interested in the process of drug discovery. The intended outcome is to train students on various aspects of new drug discovery/development, drug screening, target identification, lead discovery, optimization and the molecular basis of drug design and drug action.
Third year undergraduates of B.Sc. Chemistry; M.Sc. Chemistry students and doctoral students
Any student who has done basic organic chemistry and has some knowledge of biochemistry with an interest in drug discovery
Companies in the pharmaceutical sector may recognize and value this course.
ABOUT THE INSTRUCTOR
Prof. Harinath Chakrapani completed his undergraduate and post-graduate studies in Chemistry from Loyola College and Indian Institute of Technology Madras, respectively. He moved to Duke University, USA to pursue his doctoral studies and after post-doctoral research stints at Wake Forest University and the National Cancer Institute, USA, he joined IISER Pune in July 2009 and is currently Associate Professor. His research interests are in organic chemistry and chemical biology. His laboratory works on developing new tools to study effects of oxidative stress responses in cells and antibiotic resistance. He has over eight years of teaching experience at IISER Pune.
1. Join the course
Learners may pay the applicable fees and enrol to a course on offer in the portal and get access to all of its contents including assignments. Validity of enrolment, which includes access to the videos and other learning material and attempting the assignments, will be mentioned on the course. Learner has to complete the assignments and get the minimum required marks to be eligible for the certification exam within this period.
COURSE ENROLMENT FEE: The Fee for Enrolment is Rs. 3000 + GST
2. Watch Videos+Submit Assignments
After enrolling, learners can watch lectures and learn and follow it up with attempting/answering the assignments given.
3. Get qualified to register for exams
A learner can earn a certificate in the self paced course only by appearing for the online remote proctored exam and to register for this, the learner should get minimum required marks in the assignments as given below:
CRITERIA TO GET A CERTIFICATE
Assignment score = Score more than 50% in at least 9/12 assignments.
Exam score = 50% of the proctored certification exam score out of 100
Only the e-certificate will be made available. Hard copies will not be dispatched.”
4. Register for exams
The certification exam is conducted online with remote proctoring. Once a learner has become eligible to register for the certification exam, they can choose a slot convenient to them from what is available and pay the exam fee. Schedule of available slot dates/timings for these remote-proctored online examinations will be published and made available to the learners.
EXAM FEE: The remote proctoring exam is optional for a fee of Rs.1500 + GST. An additional fee of Rs.1500 will apply for a non-standard time slot.
5. Results and Certification
After the exam, based on the certification criteria of the course, results will be declared and learners will be notified of the same. A link to download the e-certificate will be shared with learners who pass the certification exam.
Week 1 : An overview of drugs and drug targets; structure of a cell; intermolecular binding forces; classification of drugs. Week 2 : Principles of enzyme structure, catalysis and inhibition in drug discovery: Enzyme mechanisms overview; enzyme catalysis and inhibition in drug discovery; reversible and irreversible inhibitors; transition-state inhibitors; case studies Week 3 : Principles of enzyme structure, catalysis and inhibition in drug discovery: Enzyme mechanisms overview; enzyme catalysis and inhibition in drug discovery; reversible and irreversible inhibitors; transition-state inhibitors; case studies,Receptors function and ligand binding interactions; Ion channel receptors; kinase-linked receptors; G-Protein coupled receptors, drug-receptor interaction; dose-response curves; case studies Week 4 : Receptors function and ligand binding interactions; Ion channel receptors; kinase-linked receptors; G-Protein coupled receptors, drug-receptor interaction; dose-response curves; case studies Week 5 : Nucleic acids structure and function; DNA Interactive agents and chemotherapy: DNA binding agents; intercalation and alkylation; DNA strand breakers; case studies Week 6 : Synthetic methods in medicinal chemistry: Combinatorial and parallel synthesis: solid phase techniques, mix and split method in combinatorial synthesis; dynamic combinatorial synthesis; solid phase synthesis; diversity-oriented synthesis. Week 7 : Lead discovery; Bioassays; drug targets; Lead Modification; optimization; pharmacophore; homologation; bioisostere; chain branching; Electronic effects; Lipophilicity; Structure-Activity Relationships; Quantiative-structure activity relationships (QSAR). Week 8 : Lead discovery; Bioassays; drug targets; Lead Modification; optimization; pharmacophore; homologation; bioisostere; chain branching; Electronic effects; Lipophilicity; Structure-Activity Relationships; Quantiative-structure activity relationships (QSAR). Week 9 : Drug metabolism and pharmacology: Analytical methods in metabolism; Phase I and Phase II transformations; Absorption, distribution, metabolism and excretion (ADME); bioavailability; pre-clinical and clinical development; therapeutic index and therapeutic window. Week 10 : Prodrugs and drug delivery systems: Use of prodrug systems; prodrugs for stability, solubility and slow release; overview of drug delivery Week 11 : Drug resistance mechanisms and synergism: Mechanisms of drug resistance; circumventing drug resistance; drug synergy Week 12 : Drug resistance mechanisms and synergism: Mechanisms of drug resistance; circumventing drug resistance; drug synergy
Books and References:
An Introduction to Medicinal Chemistry, Graham L. Patrick; Second Edition.The Organic Chemistry of Drug Design and Drug Action, Richard B. Silverman, Second EditionLehninger’s Principles of Biochemistry, Cox and Nelson, Fifth Edition (Reference).