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. 2002 Mar;66(1):21–38. doi: 10.1128/MMBR.66.1.21-38.2002

TABLE 1.

Drug disruption of cytoskeletal elements in the Apicomplexa

Drug and cytoskeletal element (drug mechanism) Concn Action Comments
Actin microfilaments
    Cytochalasin D (disrupter)a 0.1-0.2 μM Inhibits actin-based gliding motility (extracellular) and invasion Inhibits gliding motility in extracellular parasites; use resistant host cells to avoid host cell effects.
    Latrunculin (disrupter)b 10 nM-5 μM Inhibits motility and invasion Will also show host cell actin effects.
    Jasplakinolide (stabilizer)c 50 nM-2 μM Filament polymerization inhibits gliding and invasion Acts on extracellular parasites; will also act on host cell actin in intracellular settings.
Microtubules
    Oryzalin (disrupter)d Also other dinitroanilines such as trifluralin, ethafluralin
        Subpellicular microtubules 0.5 μM Parasites lack apical polarity No effect on extracellular parasites; no effect on host cell microtubules, but intracellular parasites are affected.
        Spindle microtubules 2.5 μM Parasites are incapable of replication As for subpellicular microtubules.
    Colchicine (disrupter)e
        Subpellicular microtubules 10 μM-1 mM Parasites lack apical polarity No drug effect on extracellular parasites; use resistant host cells to avoid host cell disruption (no microtubules in RBCs).
        Spindle microtubules 5-10 mM Parasites are incapable of replication As for subpellicular microtubules.
    Colcemid (disrupter)f 50 μM Inhibits intracellular growth No cell biological observations accompany study.
    Vinblastine (disrupter)g 15-100 nM Inhibits intracellular growth No cell biological observations accompany study.
    Vincristine (disrupter)h 7 nM Inhibits intracellular growth No cell biological observations accompany study.
    Tubulozole (disrupter)i 10 μM Parasites are killed May inhibit parasite protein synthesis rather than microtubules
    Taxol (stabilizer)j 0.1-0.5 μM Parasites are incapable of budding No drug effect on extracellular parasites; host cell microtubules will also be affected (no microtubules in RBCs).
    Docetaxel/taxotere (stabilizer)k 10 nm-50 μM Parasites are incapable of replication No drug effect on extracellular parasites; host cell microtubules will also be affected (no microtubules in RBCs).
    Epithalone A (stabilizer)l 0.1-0.5 μM Parasites are incapable of budding No drug effect on extracellular parasites; host cell microtubules will also be affected (no microtubules in RBCs).
Myosin
    BDM (ATPase inhibitor)m 20-40 mM Inhibits actin-based gliding motility (extracellular) and invasion Will also act on host cell myosins (not present in red cells).
    KT5926 (LC kinase inhibitor)n 1-5 μM Inhibits actin-based gliding motility (extracellular) and invasion Most probably inhibits secretion of TRAP family adhesins rather than myosin.
a

Data from references 8, 25, 28, 35, 37, 39, 54, 56, 57, 64, 69, 85, 103, 104, 129, 131, 140, 143-145, 148, 152, 156, 163, and 170.

b

Data from reference 145.

c

Data from references 123, 145, and 147.

d

Data from references 11, 17, 22, 59, 78, 96, 110, 145, and 164.

e

Data from references 15, 23, 59, 85, 131, 156, 173, 185, 188, and 189.

f

Data from reference 16.

g

Data from references 16, 35, 120, 131, 156, 174, 188, and 189.

h

Data from references 35 and 174.

i

Data from references 16, 35, and 36.

j

Data from references 59, 69, 85, 144, 145, 159, and 168.

k

Data from references 137 and 159.

l

Data from reference 168.

m

Data from references 37, 56, 57, 64, and 119.

n

Data from reference 37.