Advances in Medicinal Chemistry Research

Course content

The course will be based on 3-4 major themes covering the objectives of the course. Hence, all subjects will be introduced in a theme driven interdisciplinary fashion. The themes will be illustrated by original scientific reports and may cover:

  • Target classes: receptors, transporters, enzymes, regulatory proteins
  • Target-ligand interactions
  • Structure – activity relationship (SAR) studies
  • Structure and ligand based drug design
  • Point of action and the prodrug concept
  • Peptidomimetics and protein based drugs
  • Drugability of lead compounds
  • Experimental methods in biological and biostructural chemistry
  • Basic and advanced medicinal chemistry concepts
  • 3D modeling of protein structure and ligand docking

As the course aims to highlight recent cutting edge research in medicinal/biostructural chemistry, themes vary but may cover: hypnotics, psychotropic drugs, immunomodulating agents, antiviral agents, neurotransmitters, chemotherapeutics, antineoplastics, drugs against neurodegenerative diseases and schizophrenia. During the course the students will cover three themes in groups of 4-5 persons. for each theme the groups will carry out literature search, write up a report and prepare a poster for oral presentation.

Education

MSc in Pharmaceutical Sciences - compulsory for line 1 and 2, MSc in Medicinal Chemistry - elective, Cand.Scient.Pharm. - elective, Cand.Pharm. - elective

 

Learning outcome

The original literature plays a pivotal role in the discovery of new drugs. In order to contribute to the process it is necessary to comprehend and to be able to communicate the content of primary research papers to others. The literature is the primary source of information in all steps of the drug discovery process including:

  • Biology of targets
  • Identification of interfering agents (drug candidates).
  • Optimization of interfering agents.

Importantly, the course aims at providing knowledge about the above-mentioned individual steps, while ensuring that the students do not consider each process isolated from the others. Hence, the students will have a collected understanding of biostructural/medicinal chemical aspects. Earlier courses provide in-depth insight to isolated techniques/theory. Rather, at this later time-point in the student’s education, an integrated view is acquired.
Drugs interfere with complex biological systems. In order to design targeted and specific drugs it is necessary to understand the system they interact with. Researchers will need to be able to quickly understand new techniques for the identification and optimization of biologics and small molecule compounds. The course objective is to train the students in acquiring the above-mentioned skills. They will work with original literature concerning particular indications. The indications may vary, and can include: cancer, diseases of the central nervous system, viral infections, neurodegenerative diseases, amyloid diseases.
 

At the end of the course, students will be able to:

Knowledge

  • Understand that particular cellular processes at the molecular level may lead to disease
  • Understand the content of original literature describing complex biological systems of relevance in drug research
  • Understand how the 3-dimensional structure of biological macromolecules plays a role for understanding the molecular basis of particular diseases, and for intervening with the disease progress
  • Understand the content of original literature describing the identification and optimization of small molecule compounds that can interfere with complex biological systems
  • Understand the content of original literature describing the impact of interfering with protein-protein interactions using designed biological macromolecules (biologics)
  • Understand how medicinal chemistry is an interdisciplinary field, building on basic scientific understanding of molecular and biological processes, exploiting detailed structural information and applying advanced chemistry for purposeful intervention

 


Skills

  • Choose experimental techniques and methods for use in the different stages in medicinal chemistry research
  • Compare and assess results obtained using different techniques and methods in medicinal chemistry research
  • Critically assess potentially conflicting reports in original literature
  • Select essential literature for a specific topic
  • Compare and assess the quality of 3D structural knowledge based on either experimental data or homology models

 

Competences

  • Collaborate and coordinate projects together with other professionals with expertise in medicinal chemistry related areas
  • Extract relevant and detailed information concerning a particular drug target from 3-D structural data files
  • Disseminate knowledge from the literature in a comparative and critical fashion
  • Translate relevant information from the basic understanding of the cellular biology behind diseases, via a molecular understanding of the relevant targets, to the relevance of chemical optimization of lead molecules for intervention.

 

 

 

 

•Lectures: 9
•Class lessons: 17

Reviews and original scientific papers available at the course website.

The teaching is arranged with the assumption that students have knowledge from basal courses in organic chemistry, physical chemistry, biochemistry, general pharmacology and medicinal chemistry.

ECTS
See exam description
Type of assessment
Continuous assessment
A course certificate in SLVKM0381U - Advances in Medicinal Chemistry Research is completed based on a continuous assessment. To qualify for assessment, the student must have submitted and approved three written reports and participated in oral presentations of the subjects, based on poster presentations.
Marking scale
passed/not passed
Censorship form
No external censorship
Criteria for exam assessment

To obtain a course certificate, the student must be able to:

 

Knowledge

  • Ability to understand and present the content of original literature describing identification and optimization of small molecule compounds that can interfere with complex biological systems.
  • Ability to understand and present the content of original literature describing the impact of interfering with protein-protein interactions using designed biological macromolecules.
  • Ability to understand and present the content of original literature describing complex biological systems of relevance in drug research.
  • Demonstrate a comprehensive collected understanding and knowledge of biostructural/​​medicinal-chemical aspects in the drug discovery process.
  • Understand that particular cellular processes at the molecular level may lead to disease
  • Understand the content of original literature describing complex biological systems of relevance in drug research
  • Understand how the 3-dimensional structure of biological macromolecules plays a role for understanding the molecular basis of particular diseases, and for intervening with the disease progress
  • Understand the content of original literature describing the impact of interfering with protein-protein interactions using designed biological macromolecules (biologics)


Skills

  • Choose experimental techniques and methods for use in the different stages in medicinal chemistry research
  • Compare and assess results obtained using different techniques and methods in medicinal chemistry research
  • Critically assess potentially conflicting reports in original literature
  • Select essential literature for a specific topic
  • Compare and assess the quality of 3D structural knowledge based on either experimental data or homology models

 

Competences

  • Collaborate and coordinate projects together with other professionals with expertise in medicinal chemistry related areas
  • Extract relevant and detailed information concerning a particular drug target from 3-D structural data files
  • Disseminate knowledge from the literature in a comparative and critical fashion
  • Translate relevant information from the basic understanding of the cellular biology behind diseases, via a molecular understanding of the relevant targets, to the relevance of chemical optimization of lead molecules for intervention.
ECTS
See exam description
Type of assessment
Oral examination, 25 min
Examination is based on a poster presentation, submitted by the student.
The exam is without preparation time.
The oral examination consists of a 25 minutes session in total; 20 min. student presentation and questioning by examiner followed by 5 min. evaluation.
Aid
Without aids

Except the poster presentation, which is drawn as the exam subject.

Marking scale
7-point grading scale
Censorship form
No external censorship
Criteria for exam assessment

To achieve the grade 12 the student must be able to:

 

Knowledge

  • Ability to understand and present the content of original literature describing identification and optimization of small molecule compounds that can interfere with complex biological systems.
  • Ability to understand and present the content of original literature describing the impact of interfering with protein-protein interactions using designed biological macromolecules.
  • Ability to understand and present the content of original literature describing complex biological systems of relevance in drug research.
  • Demonstrate a comprehensive collected understanding and knowledge of biostructural/​​medicinal-chemical aspects in the drug discovery process.
  • Understand that particular cellular processes at the molecular level may lead to disease
  • Understand the content of original literature describing complex biological systems of relevance in drug research
  • Understand how the 3-dimensional structure of biological macromolecules plays a role for understanding the molecular basis of particular diseases, and for intervening with the disease progress
  • Understand the content of original literature describing the impact of interfering with protein-protein interactions using designed biological macromolecules (biologics)


Skills

  • Choose experimental techniques and methods for use in the different stages in medicinal chemistry research
  • Compare and assess results obtained using different techniques and methods in medicinal chemistry research
  • Critically assess potentially conflicting reports in original literature
  • Select essential literature for a specific topic
  • Compare and assess the quality of 3D structural knowledge based on either experimental data or homology models

 

Competences

  • Collaborate and coordinate projects together with other professionals with expertise in medicinal chemistry related areas
  • Extract relevant and detailed information concerning a particular drug target from 3-D structural data files
  • Disseminate knowledge from the literature in a comparative and critical fashion
  • Translate relevant information from the basic understanding of the cellular biology behind diseases, via a molecular understanding of the relevant targets, to the relevance of chemical optimization of lead molecules for intervention
  • Category
  • Hours
  • Lectures
  • 26
  • Project work
  • 88
  • Preparation
  • 91,5
  • Exam
  • 0,5
  • English
  • 206,0