Understand the phases and strategies of drug discovery and development. Consolidate fundamentals of organic chemistry and drug–target interactions relevant to rational drug design. Provide an overview of biotechnological drugs (antibodies, peptides/peptidomimetics, oligonucleotides/RNA-based). Comprehend the role and importance of those structural properties of biotechnological drugs which are important for the pharmacological activity and their potential therapeutic applications. Develop critical reading of primary literature and case studies.
Course Prerequisites
Basic organic chemistry, biochemistry, molecular biology and pharmacology (BSc level). Initial bridging sessions will be provided.
Teaching Methods
Frontal classes performed by informatic support (Slides).
Assessment Methods
The exam consists of a written test including exercises, multiple-choice questions, and open-ended questions. Practice sessions will be held during the course in preparation for the final exam.
Texts
All material used by the teacher during the lectures will be provided in the Kiro web site Scientific literature cited in the teaching material provided
Contents
Part 1 – Foundations and alignment. Overview of drug discovery and development. Organic chemistry refreshers: functional groups, scaffolds, relevant biomolecular classes. Biological targets and drug–target interactions; principles of ADME and drug-likeness. Part 2 – Rational Drug Design. Ligand-based drug design vs Structure-based drug design: SAR/QSAR, pharmacophores; target structures (PDB, AlphaFold). Part 3 – Biotechnological Drugs. Intro and classification of biotech drugs. Therapeutic antibodies (mono/bispecific, ADCs, glyco-engineered, nanobodies). Peptides and peptidomimetics: stability, rational design, chemical modifications; notes on recombinant proteins/growth factors. Therapeutic oligonucleotides and RNA-based drugs (antisense, siRNA, aptamers).
