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Homework answers / question archive /   Enters mycobacterial cells in a concentration-dependent manner, binds to the beta-subunit of DNA-dependent RNA polymerase, forms a stable drug-enzyme complex, and suppresses RNA synthesis by inhibiting the elongation of messenger RNA

  Enters mycobacterial cells in a concentration-dependent manner, binds to the beta-subunit of DNA-dependent RNA polymerase, forms a stable drug-enzyme complex, and suppresses RNA synthesis by inhibiting the elongation of messenger RNA

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  1. Enters mycobacterial cells in a concentration-dependent manner, binds to the beta-subunit of DNA-dependent RNA polymerase, forms a stable drug-enzyme complex, and suppresses RNA synthesis by inhibiting the elongation of messenger RNA.
  2. Unclear, is thought to include 1) the inhibition of fatty acid synthase type I in replicating bacilli leading to interference with mycolic acid synthesis, 2) disruption of cellular membrane transport, and 3) reduction of intracellular pH.
  3. Diffuses into bacterial cells where it is activated by KatG (an oxidase/peroxidase encoded by the gene katG) to the nicotinoyl radical, which reacts with NAD+ of NADP+ to produce active adducts, the adducts interfere with the synthesis of mycolic acids by inhibiting NADH-dependent enoyl-ACP reductase, which is encoded by the gene inhA.
  4. inhibits arabinosyl transferase III, which is involved in cell-wall biosynthesis; this results in interference with the biosynthesis of the cell wall component arabinogalactan.
  5. target 50S ribosomal subunit on RNA, inhibiting peptidyl transferase.
  6. Inhibits DNA synthesis and supercoiling by targeting topoisomerase.
  7. blocks formation of the 70S initiation complex in peptide synthesis.
  8. Its an analogue of D-alanine that inhibits peptidoglycan synthesis by blocking the action of D-Alanine:D-Alanine ligase (Ddl), it also inhibits D-alanine racemase (Alr), which is involved in the conversion of L-Alanine to D-Alanine, which then serves as a substrate for Ddl.
  9. A structural analog of PABA and acts as a competitive inhibitor of dihydropteroate synthase (DHPS) in the bacterial folate pathway.
  10. Unknown, but may involve cellular membrane disruption, inhibition of mycobacterial phospholipase A2, inhibition of microbial potassium transport generation of hydrogen peroxide, and interference with bacterial electron transport systems.
  11. Inhibits protein synthesis by targeting the 30S ribosomal subunit.

 

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