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Drug Discovery: basic principles

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Drug Discovery: basic principles

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Academic year 2021/2022

Course ID
BIO0170B Pds 306-TB
Teacher
Prof.ssa Sonja Visentin (Lecturer)
Degree course
[0101M21] Molecular Biotechnology
Year
2nd year
Teaching period
To be defined
Type
Related or integrative
Credits/Recognition
5
Credits 24 CFU plan
5
Course disciplinary sector (SSD)
CHIM/08 - chimica farmaceutica
Delivery
Formal authority
Language
English
Attendance
Obligatory
Type of examination
Written and oral
Type of learning unit
modulo
Modular course
PHARMACOLOGY AND DRUG THERAPIES (BIO0170 Pds 306-TB)
Prerequisites
Elements of organic chemistry and biochemistry.
Propedeutic for
This teaching is a point of arrival. It is not propaedeutical.
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Sommario del corso

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Course objectives

The main objective of the course is to provide students with the basics of drug discovery and understanding the relationship between the chemical structure of molecules and their pharmacological activity. Moreover, the course prefigures to provide the student with a highly professionalized competence of business and national pharmaceutical research centers, on the different aspects of instrumental analysis in the different phases of the discovery, development and production process  of the pharmaceutical industry.

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Results of learning outcomes

At the end of the course, students should be able to have learned the various stages that make up the pipeline of drug discovery and understand the chemical and physical properties of the molecules in the pharmaceutical field

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Program

  • Introduction to drug discovery ; identification of the target and the ligand ; virtual screening ; drug discovery based on fragments ; transformations of lead ; isosterism and bioisosterism ; Introduction to QSAR ; synthesis of peptides and SPPS ; Combinatorial Approach to Drug Discovery ; example of study.
  • Physico-chemical properties of molecules and their influence on the interaction between drugs and their targets :
  • type of bond and their strength, intermolecular forces, ionization, lipophilicity
  • Relevance of the structures of proteins and DNA drug-receptor interaction
  • Principles of Pharmacodynamics Pharmacokinetics ( ADMET )
  • Molecular Descriptors involved in the determination of the ADME profile of potential drugs
  • Principles of Pharmacodynamics Pharmacokinetics ( ADMET )
  • Structure- activity relationship and drug design
  • Drug Discovery for biotechnological drugs
  • Nanotechnology for drug delivery
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Course delivery

The course will be delivered through frontal lectures using the Moodle platform

Lessons: 40 hours

After the recent emergency situation, the teaching will be made compatible with an integrated learning environment in e-learning mode, suitable for face-to-face situations, those in which teaching is provided entirely online and forms of blended teaching.

Depending on the changing situations, the platform course will welcome: lesson materials (video recordings and / or audio presentations); exercises to be carried out online, but also face-to-face; in-depth teaching materials that can be discussed through a forum and / or in the classroom during the lesson-debate. The objective of the learning environment is to create continuity between the different teaching moments and between the different situations (remote activities and face-to-face activities).

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Learning assessment methods

The exam is divided in  two parts:

  • writing a scientific article about a drug assigned to each candidate at least 15 days before the examination date, using a track provided by the teacher (max 27/30)
  • Oral exam on the program

The unit of measure: thirty/30

Depending on the recent emergency situation, the exam may be in oral remote (webex) mode.

Suggested readings and bibliography

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Burger's Medicinal Chemistry and Drug Discover

Author: Donald Abraham and David Rotella

Publisher: Wiley
ISBN: 978-0-470-27815-4

Pharmaceutical Analysis
Author: David Watson
Publisher: Elsevier
ISBN: 9780702051296



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Notes

The teaching activity may vary according to the limitations imposed by the current health crisis. In any case, the remote mode is ensured throughout the academic year

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