Pharmacology Flashcards
Target identification
Finding element of the disease / process to alter
Hit generation
Making molecules that interact correctly with your target
Lead optimization
Testing / tweaking structures to find the best one
Preclinical development
Testing drug in cells or animals
Etoposide
Inhibits eukaryotic DNA topoisomerase II as a form of cancer chemotherapy
Ciprofloxacin
Antibiotic that inhibits bacterial DNA topoisomerase II (DNA gyrase)
Norfloxacin
Antibiotic that inhibits bacterial DNA topoisomerase II (DNA gyrase)
Rifampin
Bactericidal agent against tuberculosis that binds to the beta subunit of RNAP and blocks the DNA/RNA channel by preventing synthesis of the 2nd or 3rd phosphodiester bond via steric-occlusion.
Spinraza (Nusinersen)
Nucleotide analogue that binds directly after exon 7 in SMN2 in individuals w/ SMA –> tricks SMN2 into splicing in a manner that includes exon 7 to compensate for non functional SMN1 gene.
EXONDYS 51
Injection used to treat Duchenne’s by skipping exon 51 in the DMD gene, restoring the reading frame.
Streptomycin
Amino glycoside that interferes w/ base pairing between tRNA anticodon and mRNA codon.
Tetracycline
Binds to 30S subunit and inhibits binding of aminoacyl-tRNA to ribosome.
Chloramphenicol
Inhibits peptidyl transferase activity of the 50s ribosomal unit.
Erythromycin
Binds to 50S ribosomal subunit and interferes with translocation.
Puromycin
Causes premature chain termination by acting as an analog of aminoacyl-tRNA. Bind to A site and causes premature release of the peptide.