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Chemical Compound Review

CHEMBL186158     (3S,6R,9S,12R,15S,18R,21S,24R) -6,18...

Synonyms: AG-K-68892, KST-1A1700, KST-1A1701, AC1Q6FHK, LS-57680, ...
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Disease relevance of PF 1022

  • The 24-membered cyclooctadepsipeptide (CODP) PF1022A, the active metabolite of the fungus imperfectus Mycelia sterilia (Rosellinia sp.) isolated from the plant Camellia japonica in Japan, is described as a powerful broad-spectrum anthelmintic natural product with low toxicity in animals [1].

High impact information on PF 1022

  • Latrophilin-like receptor from the parasitic nematode Haemonchus contortus as target for the anthelmintic depsipeptide PF1022A [2].
  • PF1022A or emodepside also bind to this 54 kDa aminoterminal region of HC110R and interact with the functional responses of alpha-latrotoxin [3].
  • Using a PF1022A-ligand immunoscreening of a cDNA library from Haemonchus contortus a cDNA clone of 3569 base pairs could be identified [3].
  • To enhance the bioavailability of PF1022A (cyclo(D-lactyl-L-N-methylleucyl-D-3-phenyllactyl-L-N-met hylleucyl-D-lactyl-L-N-methylleucyl-D-3-phenyllactyl-L-N- methylleucyl)), a newly developed antinematode drug, we examined whether the new drug has polymorphism or not [4].
  • These results suggest that selectivity against adult females in vivo could be attributable to non-neuropharmacological mechanisms and that PF1022A does not pass through the blood-brain barrier in host animals [5].

Biological context of PF 1022


Anatomical context of PF 1022


Associations of PF 1022 with other chemical compounds

  • We examined the effect of PF1022A, one of the gabergic anthelmintics newly developed in Japan, on gamma-aminobutyric acid (GABA) receptors using a radioligand binding technique in isolated membrane preparations of the nematode Ascaris suum [8].

Analytical, diagnostic and therapeutic context of PF 1022

  • By examining physicochemical properties of these forms by various methods including X-ray powder diffractometry and differential scanning calorimetry, it became apparent that PF1022A had one amorphous (form alpha) and three crystalline polymorphic forms, form I, form II and form III [4].


  1. Influence of the cyclooctadepsipeptides PF1022A and PF1022E as natural products on the design of semi-synthetic anthelmintics such as emodepside. Jeschke, R., Iinuma, K., Harder, A., Schindler, M., Murakami, T. Parasitol. Res. (2005) [Pubmed]
  2. Latrophilin-like receptor from the parasitic nematode Haemonchus contortus as target for the anthelmintic depsipeptide PF1022A. Saeger, B., Schmitt-Wrede, H.P., Dehnhardt, M., Benten, W.P., Krücken, J., Harder, A., Von Samson-Himmelstjerna, G., Wiegand, H., Wunderlich, F. FASEB J. (2001) [Pubmed]
  3. Cyclooctadepsipeptides--an anthelmintically active class of compounds exhibiting a novel mode of action. Harder, A., Schmitt-Wrede, H.P., Krücken, J., Marinovski, P., Wunderlich, F., Willson, J., Amliwala, K., Holden-Dye, L., Walker, R. Int. J. Antimicrob. Agents (2003) [Pubmed]
  4. Effects of amorphous and polymorphs of PF1022A, a new antinematode drug, on Angiostrongylus costaricensis in mice. Kachi, S., Terada, M., Hashimoto, H. Jpn. J. Pharmacol. (1998) [Pubmed]
  5. Influence of PF1022A on the motility of Angiostrongylus cantonensis in vitro. Kachi, S., Terada, M., Hashimoto, H. Parasitol. Res. (1997) [Pubmed]
  6. PF1022A and related cyclodepsipeptides - a novel class of anthelmintics. Scherkenbeck, J., Jeschke, P., Harder, A. Current topics in medicinal chemistry. (2002) [Pubmed]
  7. Effects of PF1022A on adult Angiostrongylus cantonensis in the pulmonary arteries and larvae migrating into the central nervous system of rats. Kachi, S., Ishih, A., Terada, M. Parasitol. Res. (1995) [Pubmed]
  8. Characterization of subtypes of gamma-aminobutyric acid receptors in an Ascaris muscle preparation by binding assay and binding of PF1022A, a new anthelmintic, on the receptors. Chen, W., Terada, M., Cheng, J.T. Parasitol. Res. (1996) [Pubmed]
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