Table 3.
List of small molecule inhibitors for eukaryotic RNA MTases. The ‘design strategy’ column describes the basic method for inhibitor design, while ‘evaluation method’ roughly lists the experiments conducted in the associated references. CADD = computer aided drug design, i.s. = in silico; i.vt. = in vitro; i.c. = in cellulo; i.vv. = in vivo
Type | Organism | Enzyme/Modification/RNA species | Design strategy | Evaluation method | References |
---|---|---|---|---|---|
Eukaryotes (single cell) | Fungi, Encephalitozoon cuniculi | Ecm1/ m7G/ mRNA cap | SAH analogue | i.vt., i.c. | (197,198) |
Nucleotide analogue | i.vt. | (114) | |||
Fungi C. albicans | CCM1/ m7G/ mRNA cap | Natural products | i.c. | (194) | |
Yeast S. cerevisiae | ABD1 (S.c.)/ m7G/ mRNA cap | Natural products | i.c. | (194) | |
Leishmania infantum | Cmt1/ m7G/ mRNA cap | SAH analogue | i.vt. | (195) | |
Trypanosoma brucei | Cmt1/ m7G/ mRNA cap | SAH analogue | i.vt. | (196) | |
Eukaryotes (multiple cell) | Human, H. sapiens | METTL3-METTL14/ m6A/ mRNA internal | CADD | i.s., i.vt., i.c. | (223) |
SAH analogue | i.vt. | (166) | |||
i.s., i.vt. | (221) | ||||
i.s., i.vt., i.c. | (222) | ||||
i.vt., i.c. | (299) | ||||
Non SAH analogue | i.s., i.vt., i.c., i.vv. | (126) | |||
i.vt., i.c. | (216,224,300) |