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

• During the past years several total syntheses of PF1022A and manifold structure-activity relationships have been established [6].

Anatomical context of PF 1022

• Next, we examined the effects of PF1022A on larval A. cantonensis migrating into the central nervous system (CNS) of rats [7].
• We examined the effects of PF1022A, newly developing in Japan, on adult Angiostrongylus cantonensis in the pulmonary arteries of rats [7].

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].

References