Antifungal Flashcards
T or F: Fungi are eukaryotic organism
True, metabolic processes are homologous to humans
Which sites of action can we not utilize for Antifungal drugs?
Transcription and Translation
What agent affects the cell wall of fungi?
Echinocandins
What agent affects the plasma membrane ?
Polyenes
What agent affects the ER of Fungi? A-BIT
A- BIT
A- Allyamines
B- Benzylamines
I- Imadiazoles
T-Triazooles
Flucytosine inhibits what compound and how does Flucytosine enter the cell?
Flucytosine enters the cell as a prodrug through the cytosine deaminase transporter and inhibits Thymidylate synthase
T or F: Prodrugs enter the cell in their primary form, then convert.
True, Flucytosine is a prodrug.
Fungal Cell Walls contain all except? A. Chitin, B. 1,6 glucan C. 1,3 glucan D. Ergosterol E. All of the above
E. All of the above
Polyenes disrupt the plasma membrane, where would they bind to?
Bind to ergosterol and form pores which alter the fungal membrane permeability.
The affinity of amphotericin B is much higher for ergosterol than cholesterol, would the concentration of the drug cause effects on the host membrane.
At high concentrations, amphotericin B can alter the host cell membrane as well.
Targeting the bio components of ergosterols is a mechanism of action. One target squalene monooxygenase is targeted by?
Allylamine/benzylamines
Lanosterol is converted into ergosterol via which enzyme?
14-alpha sterol demethylase
What inhibits 14-alpha sterol demethylase?
Imidazole and triazoles
What is the target for cell wall synthesis inhibition with antifungals. ?
Beta (1,3) glucan synthase
Griseofulvin inhibits the target for cell division. What would also be affected if this target is affected?
Since it affects tubulin which is central for growth. Vacuole transport, and mitotic spindle fibers are affected.
T or False: Echinocandins are non-competitive inhibitors.
True, they don’t compete with the substrate but they do inhibit the enzyme.
T or F: Griseofulvin accumulates in keratin precursor cells.
True.
Flucytosine is converted into its active form called?
Fluorouracil
T or F: Fluorouracil is converted into 5-FdUMP
True
T or F: 5-FdUMP does not inhibit thymidylate synthase
False
T or F: Cytosine deaminase is found in a human cells?
False
What is involved in the biosynthesis of cholesterol?
Squalene epoxidase
Allyamines and Benzylamines can be found in the treatment of?
Hypercholesterolemia
Which enzyme has heme?
14-alpha sterol demethylase
T or F: Azoles decrease ergosterols
True
Mutation of P450 results in the resistance to which drug? A. Azoles B. Polyenes C. Fluorouracil D. Allyamines
A. Azoles
T or F: Griseofulvin binds to the tubulin and microtubulin
True
