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Patrick An Introduction to Medicinal Chemistry 3/e Chapter 7 NUCLEIC ACIDS AS DRUG TARGETS

Patrick An Introduction to Medicinal Chemistry 3/e Chapter 7 NUCLEIC ACIDS AS DRUG TARGETS Part 3: Section 7.3 (Drugs acting on RNA). Contents Part 3: Section 7.3 (Drugs acting on RNA) 4. Drugs Acting On rRNA - Antibiotics 5. Drugs Acting On mRNA - Antisense Therapy (2 slides)

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Patrick An Introduction to Medicinal Chemistry 3/e Chapter 7 NUCLEIC ACIDS AS DRUG TARGETS

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  1. Patrick An Introduction to Medicinal Chemistry 3/e Chapter 7 NUCLEIC ACIDS AS DRUG TARGETS Part 3: Section 7.3 (Drugs acting on RNA)

  2. Contents Part 3: Section 7.3 (Drugs acting on RNA) 4. Drugs Acting On rRNA - Antibiotics 5. Drugs Acting On mRNA - Antisense Therapy (2 slides) 6. Drugs related to nucleic acid building blocks - Examples: Antiviral agents (2 slides) - Examples [7 slides]

  3. 4. DRUGS ACTING ON rRNA Antibiotics Streptomycin Chloramphenicol (vs typhoid) Rifamycins Chlortetracycline (Aureomycin) Erythromycin

  4. Protein synthesis 5. DRUGS ACTING ON mRNA Antisense Therapy

  5. 5. DRUGS ACTING ON mRNA Antisense Therapy • Advantages • Same effect as an enzyme inhibitor or receptor antagonist • Highly specific where the oligonucleotide is 17 nucleotides or more • Smaller dose levels required compared to inhibitors or antagonists • Potentially less side effects • Disadvantages • ‘Exposed’ sections of mRNA must be targeted • Instability and polarity of oligonucleotides (pharmacokinetics) • Short lifetime of oligonucleotides and poor absorption across cell membranes

  6. Azidothymidine (AZT) (Zidovudine;Retrovir) Chain terminating group 6. Drugs related to nucleic acid building blocks Examples: Antiviral agents • Enzyme inhibitor • AZT is phosphorylated to a triphosphate in the body • Triphosphate has two mechanisms of action • - inhibits a viral enzyme (reverse transcriptase) • - added to growing DNA chain and acts as chain terminator

  7. Chain terminating group Chain terminating group Acyclovir (Zovirax) Famciclovir (Famvir) 6. Drugs related to nucleic acid building blocks Examples: Antiviral agents Notes: Same mechanisms of action as AZT Used vs herpes simplex and shingles

  8. 6. Drugs related to nucleic acid building blocks Examples: Antisense nucleotides - see earlier Uracil mustard - see earlier

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