Biosynthetic Enzyme

Inhibitor

Specificity

Clinical Trial/ Drug

GlcNAc-T

Jawsamycin

Antifungal: fungicidal

• Effective against Fusarium spp., Scedosporium spp., and Mucorales fungi.

• Not effective against Candida albicans or Cryptococcus neoformans

No

Gpi12

Nonsubstrate analog:

Salicylic hydroxamic acid (SHAM), a Zn⁺⁺ binder

Substrate analogs:

GlcNCONH₂-β-PI and GlcNCONH₂-(2-O-octyl)-PI (suicide inhibitors)

GalNCONH₂-PI and GlcNCONH₂-β-PI (suicide inhibitors)

Antiprotozoan parasite (Trypanosoma brucei)

• Tested in cell-free system only

Antiprotozoan parasite (T. brucei)

• Tested in cell-free system only

Antiprotozoan parasite (Plasmodium falciparum)

• Tested in cell-free system only

No

No

No

Gwt1

Patented lead molecule (identity not publicly available)

APX001/E1211

(N-phosphonooxymethyl prodrug that is processed into its active form, APX001A/ E1210, by the action of alkaline phosphatase in the host)

Aminopyrifen

(2-aminonicotinate)

Gepinacin

(monocarboxylic amide)

Antimalarial

Antifungal: Fungistatic

• Effective against Candida spp., as well as invasive mold infections caused by Aspergillus spp., Scedosporium spp., Fusarium spp., or other rare molds

Antifungal: fungicidal

• Inhibits growth of Neospora crassa. Useful against several plant fungal pathogens.

Antifungal: fungistatic

• Acts against Candida spp., Aspergillus spp.

Lead optimization

Phase II clinical trial (Fosmanogepix/ Manogepix)

Pesticide under development (code AKD-5195)

No

MT-I

L‐myo‐inositol-1-phosphate

Antiprotozoan parasite

• Tested only in a cell-free system (T. brucei)

No

Mcd4

YW3548/ M743

(a terpene lactone from C. simplex) and M720 (a derivative of M743)

Antifungal: fungistatic

• Specificity demonstrated for Candida spp. and Aspergillus spp.

• Protozoan parasites are not inhibited by it since they lack the step/ enzyme being targeted.

• Mammalian GPI-MT1 mediated by PIG-N is also inhibited.

No