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Questions and Answers
Who is the author of the study on the design of novel antifungal drugs?
Who is the author of the study on the design of novel antifungal drugs?
Dr. Frans Hochstenbach
The insulin hexamer contains two zinc ions, each coordinated by three ______ residues.
The insulin hexamer contains two zinc ions, each coordinated by three ______ residues.
His
Which of the following are current antifungals? (Select all that apply)
Which of the following are current antifungals? (Select all that apply)
- Nystatin (correct)
- Amphotericin B (correct)
- Miconazole (correct)
- Penicillin
What is amphotericin B used for?
What is amphotericin B used for?
Candicidin is currently in Phase I clinical trials.
Candicidin is currently in Phase I clinical trials.
Which ions can leak through the pore formed by amphotericin B? (Select all that apply)
Which ions can leak through the pore formed by amphotericin B? (Select all that apply)
Match the following antifungal drugs with their type:
Match the following antifungal drugs with their type:
Azoles are heterocycles of carbon and ______ atoms.
Azoles are heterocycles of carbon and ______ atoms.
What characteristic distinguishes miconazole from fluconazole?
What characteristic distinguishes miconazole from fluconazole?
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Study Notes
Transition Metals
- Transition metals are found in many biological processes
- Insulin hexamer contains two zinc ions, each coordinated by three His residues
- In manganese superoxide dismutase, the cofactor manganese is bound by three histidine side chains and one aspartate side chain.
Antifungal Drug Design
- Current antifungals include polyenes and azoles
- Polyenes include nystatin, amphotericin B, candicidin, SPK-843
Amphotericin B
- Amphotericin B is a polyene used for systemic fungal infections
- It forms a conducting pore in the plasma membrane of fungal cells
- The pore is formed by two rings of eight amphotericin B molecules linked hydrophobically to ergosterol
- The pore allows ions such as K+ and Mg2+ to leak out of the fungal cell, resulting in cell death
Candicidin
- Candicidin is a polyene in phase III clinical trials
- Candicidin is more soluble than amphotericin B
Azoles
- Azoles are heterocycles of carbon and nitrogen atoms
- Key examples include:
- Miconazole (diazole)
- Fluconazole (triazole)
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