Inhibitor enzimatic

Un inhibitor enzimatic este o moleculă care se leagă de o enzimă cu scopul de a descrește activitatea acesteia. Prin blocarea activității enzimatice, medicamentele care sunt inhibitori enzimatici pot distruge agenții patogeni^[1] sau pot corecta anumite dezechilibre metabolice.^[2]^[3] Aceeași idee este valorificată și în cazul pesticidelor. Totuși, nu toate moleculele care se leagă de enzime sunt inhibitori: există și compuși activatori enzimatici, care vor crește activitatea acestora.

[1]
Srinivasan B, Tonddast-Navaei S, Roy A, Zhou H, Skolnick J (septembrie 2018). „Chemical space of Escherichia coli dihydrofolate reductase inhibitors: New approaches for discovering novel drugs for old bugs”. Medicinal Research Reviews. doi:10.1002/med.21538. PMID 30192413.
[2]
Srinivasan B, Tonddast-Navaei S, Skolnick J (octombrie 2015). „Ligand binding studies, preliminary structure-activity relationship and detailed mechanistic characterization of 1-phenyl-6,6-dimethyl-1,3,5-triazine-2,4-diamine derivatives as inhibitors of Escherichia coli dihydrofolate reductase”. European Journal of Medicinal Chemistry. 103: 600–14. doi:10.1016/j.ejmech.2015.08.021. PMC 4610388 . PMID 26414808.
[3]
Srinivasan B, Skolnick J (mai 2015). „Insights into the slow-onset tight-binding inhibition of Escherichia coli dihydrofolate reductase: detailed mechanistic characterization of pyrrolo [3,2-f] quinazoline-1,3-diamine and its derivatives as novel tight-binding inhibitors”. The FEBS Journal. 282 (10): 1922–38. doi:10.1111/febs.13244. PMC 4445455 . PMID 25703118.

Antimetabolit
Farmacofor
Inhibiție competitivă

[:0-1] [1]
Srinivasan B, Tonddast-Navaei S, Roy A, Zhou H, Skolnick J (septembrie 2018). „Chemical space of Escherichia coli dihydrofolate reductase inhibitors: New approaches for discovering novel drugs for old bugs”. Medicinal Research Reviews. doi:10.1002/med.21538. PMID 30192413.

[:1-2] [2]
Srinivasan B, Tonddast-Navaei S, Skolnick J (octombrie 2015). „Ligand binding studies, preliminary structure-activity relationship and detailed mechanistic characterization of 1-phenyl-6,6-dimethyl-1,3,5-triazine-2,4-diamine derivatives as inhibitors of Escherichia coli dihydrofolate reductase”. European Journal of Medicinal Chemistry. 103: 600–14. doi:10.1016/j.ejmech.2015.08.021. PMC 4610388 . PMID 26414808.

[:2-3] [3]
Srinivasan B, Skolnick J (mai 2015). „Insights into the slow-onset tight-binding inhibition of Escherichia coli dihydrofolate reductase: detailed mechanistic characterization of pyrrolo [3,2-f] quinazoline-1,3-diamine and its derivatives as novel tight-binding inhibitors”. The FEBS Journal. 282 (10): 1922–38. doi:10.1111/febs.13244. PMC 4445455 . PMID 25703118.

[1]

[2]

[3]

Wikiwand in your browser!

Inhibitor enzimatic

Wikiwand in your browser!

Note

Vezi și