Course: Principles of anticancer and antiviral drug development I.

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Course title Principles of anticancer and antiviral drug development I.
Course code UCH/645
Organizational form of instruction Lecture
Level of course Master
Year of study not specified
Frequency of the course In each academic year, in the summer semester.
Semester Summer
Number of ECTS credits 3
Language of instruction English
Status of course Compulsory-optional
Form of instruction unspecified
Work placements unspecified
Recommended optional programme components None
Course availability The course is available to visiting students
Lecturer(s)
  • Selinger Martin, RNDr. Ph.D.
  • De Clercq Erik, prof. Dr. Ph.D.
Course content
Contents of lectures: 1. Viruses. Viral structure, morphology and genome organization. ICTV and Baltimore classification. Viral genomes and replication strategies, viral evolution and genetic variability. 2. Immune System and Vaccines. Innate and adaptive immunity, pattern-recognition receptors, interferons, antigen presentation, B and T lymphocytes. Humoral and cellular responses. Live attenuated, inactivated, subunit, vector and mRNA vaccines; immunological memory. 3. Antiviral Drug Design I: Principles of antiviral drug research. Entry and Fusion Inhibitors - viral attachment/entry and host-cell receptors. Entry and fusion inhibitors and neutralizing antibodies. 4. Antiviral Drug Design II: Inhibitors of Viral Replication. Viral DNA and RNA polymerases. Antimetabolites and nucleoside/nucleotide analogues, including acyclic guanosine analogues and nucleoside phosphonates. Reverse transcriptase and integrase inhibitors (HIV). HCV NS5A/NS5B inhibitors. 5. Antiviral Drug Design III: Maturation & Release Inhibitors, Immune System Stimulation. Viral protein processing, maturation, assembly and release. HIV and HCV protease inhibitors, influenza neuraminidase inhibitors. Interferons, immunomodulatory approaches, combination therapy and antiviral resistance. 6. Cell Cycle, Cancer and Its Classification. Cell-cycle regulation, cyclins and CDKs, checkpoints and DNA damage responses. Oncogenes, tumor suppressors and apoptosis. Malignant transformation, hallmarks of cancer and tumor classification. 7. Oncogenic Viruses. Molecular mechanisms of viral oncogenesis, latency and cellular transformation. HPV, EBV, HBV, HCV, HTLV-1, KSHV and Merkel cell polyomavirus. Chronic inflammation and tumor immune evasion. 8. Cancer Therapy I: Surgery, Radiation and Hormonal Therapy. Treatment planning and curative, adjuvant and palliative approaches. Surgery, radiation-induced DNA damage and radiosensitivity. Hormone-dependent cancers, estrogen receptor targeting and androgen deprivation therapy. 9. Cancer Therapy II: Chemotherapy. Cytotoxic drugs: alkylating agents, platinum compounds, antimetabolites, antitumor antibiotics and plant alkaloids. Targeted therapy: tyrosine kinase and proteasome inhibitors, L-asparaginase. Toxicity, drug resistance and precision oncology. 10. Cancer Therapy III: Biological Therapy. Tumor-associated and tumor-specific antigens, monoclonal antibodies and checkpoint inhibitors (CTLA-4, PD-1/PD-L1). Cytokine therapy, cancer vaccines, hematopoietic stem cell transplantation and oncolytic viruses. Tumor immune evasion. 11. Adoptive Cell Therapy. Tumor microenvironment and principles of ACT. TIL, TCR-T and CAR-T therapies; CAR design, generations and signaling. Applications in hematological malignancies and solid tumors, cytokine release syndrome and other treatment-related toxicities.

Learning activities and teaching methods
Monologic (reading, lecture, briefing), Case studies
  • Preparation for exam - 20 hours per semester
  • Class attendance - 26 hours per semester
Learning outcomes
This course aims to provide students with an understanding of the fundamental principles of virology, immunology, and cancer biology, with particular emphasis on the mechanisms of action of antiviral and anticancer drugs. Upon successful completion of the course, students will be able to describe the mechanisms of action of major classes of antiviral and anticancer drugs, predict the consequences of alterations in viral replication and cancer-related signaling pathways, and explain the mechanisms underlying drug resistance in viruses and tumors. Furthermore, students will be able to compare conventional chemotherapy, targeted therapy, immunotherapy, and adoptive cell therapy, critically evaluate therapeutic strategies from a mechanistic perspective, and justify their clinical applications.
Upon successful completion of the course, students will be able to describe the mechanisms of action of major classes of antiviral and anticancer drugs, predict the consequences of alterations in viral replication and cancer-related signaling pathways, and explain the mechanisms underlying drug resistance in viruses and tumors. Furthermore, students will be able to compare conventional chemotherapy, targeted therapy, immunotherapy, and adoptive cell therapy, critically evaluate therapeutic strategies from a mechanistic perspective, and justify their clinical applications.
Prerequisites
knowledge of biochemistry, cellular and molecular biology, basics of biology

Assessment methods and criteria
Test

Students must correctly answer at least 60 % of test questions.
Recommended literature
  • R. B. Silverman: The Organic Chemistry of Drug Design and Drug Action, Academic Press, 2nd edition.


Study plans that include the course
Faculty Study plan (Version) Category of Branch/Specialization Recommended year of study Recommended semester