PEPTIDE DRUGS
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- Versione italiana
- Academic year
- 2022/2023
- Teacher
- DELIA PRETI
- Credits
- 6
- Didactic period
- Secondo Semestre
- SSD
- CHIM/08
Training objectives
- Biologically active peptides have attracted a growing interest in the pharmaceutical industry, resulting in the recent marketing of a number of peptide/protein drugs. In addition, an increasing series of peptide/protein drugs is currently being evaluated in advanced clinical trials. The main objective of the course is to provide students with the KNOWLEDGE of the theoretical basis needed to understand the chemistry, the pharmacodynamics/pharmacokinetic features and the growing application potential of peptide/protein medicines divided into therapeutic classes. Of particular relevance for the professional practice, the course will stimulate the acquirement of SKILLS in the recognition and description, with appropriate language, of the structural and pharmacodynamic aspects of the different drug classes and their therapeutic uses.
Prerequisites
- Basic notions from the courses of general chemistry, organic chemistry, molecular biology, animal biology and anatomy. In particular, the ability to recognize a functional group and the relative chemical reactivity is recommended. In addition, knowledge of: the concept of chirality, the structural parameters affecting the solubility of a molecule, the chemico-physical parameters governing the interaction between atoms and functional groups. Finally, notions concerning the structure and physiology of animal cells, the anatomical location of cells and tissues, the processes of transcription and translation of DNA in gene expression.
Course programme
- The course will be given as lectures for a total of 36 hours during which the following topics will be addressed.
PART 1: GENERAL (10 hours)
Critical analysis of the recent market expansion of peptide/protein drugs. Structure and general properties of amino acids and peptides. Basic notions about peptide synthesis: protecting groups in peptide synthesis; methods of activation for peptide coupling; liquid synthesis; solid phase synthesis. Peptide drugs vs. "traditional medicines": strengths, weaknesses, perspectives. Pharmacokinetic (absorption, distribution and elimination) of peptide drugs. Peptidomimetics: definition; concept of bioactive conformation; concept of conformational restriction; conformational analysis in peptide systems. Design of a peptidomimetic: non-natural amino acids, cyclic peptides, peptide bond isosteres. General overview of the main therapeutic indications of peptide drugs currently in the market or in advanced clinical trials.
PART 2A: PEPTIDE/PEPTIDOMIMETIC drugs (18 hours)
Peptides used in oncology: Synthetic analogues of GnRH; Synthetic analogues of somatostatin; Synthetic analogues of GH; Proteasome inhibitors; Inhibitors of the enzyme histone deacetylase. Peptides used for the treatment of metabolic disorders: Insulin and fast acting and long acting synthetic analogues; Glucagon and amylin (outline); GLP-1 analogues. Peptides used for the treatment of cardiovascular disorders: Antithrombotics; Antiplatelet agents. Peptides with various therapeutic indications: Peptide drugs used as analgesics; Peptide drugs used for the prevention of organ rejection; Peptide drugs used for the treatment of multiple sclerosis.
PART 2B: MONOCLONAL ANTIBODY (8 hours)
Monoclonal antibodies: clinical use in anticancer therapy (rituximab, trastuzumab), rejection prophylaxis (basiliximab, daclizumab), in the treatment of rheumatoid arthritis (infliximab, certolizumab), psoriasis (efalizumab), asthma (Omalizumab) and viral infections (palivizumab) . Didactic methods
- Video-recorded lectures for a total of 36 hours.
Learning assessment procedures
- The written exam consists of 31 questions to be answered in 40 minutes. The use of own notes, books or multimedia supports is not allowed. The questions will be formulated with multiple choice answeres (5 options for each question) relating to all the training objectives defined above. Each correct answer will be assigned a score of 1, for a total of 31 points, equal to a maximum grade of 30/30 cum laude. There will be no penalty for incorrect or missing answers.
Reference texts
- Specific topics can be explored on the following texts:
1) V. Santagada, G. Caliendo. "Peptidi e Peptidomimetici". PICCIN
2) Peptide Chemistry and Drug Design edited by Ben M. Dunn Ph.D, Wiley (DOI:10.1002/9781118995303).
3) Foye's. Principi di chimica farmaceutica. Editore: Piccin-Nuova Libraria. Edizione 2014, capitolo "Biotecnologie farmaceutiche".
4) Gasco, Gualtieri, Melchiorre. Chimica Farmaceutica. Casa editrice Ambrosiana. Capitolo "Farmaci Biotecnologici".
