The anthelmintic praziquantel is a human serotoninergic G-protein-coupled receptor ligand

Nature Communications

Volumn 8, Issue 1, 2017, Pages

  Chan, John D ^a   Cupit, Pauline M ^b   Gunaratne, Gihan S ^a   McCorvy, John D ^c   Yang, Yang ^a   Stoltz, Kristen ^d   Webb, Thomas R ^e   Dosa, Peter I ^d   Roth, Bryan L ^c,f   Abagyan, Ruben ^b   Cunningham, Charles ^g   Marchant, Jonathan S ^a,h,i  

^a UNIVERSITY OF MINNESOTA   (United States)

^b UNIVERSITY OF CALIFORNIA SAN DIEGO   (United States)

^c UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^d UNIVERSITY OF MINNESOTA   (United States)

^e SRI INTERNATIONAL   (United States)

^f University of North Carolina   (United States)

^g UNIVERSITY OF NEW MEXICO   (United States)

^h UNIVERSITY OF MINNESOTA MEDICAL SCHOOL   (United States)

ⁱ MEDICAL COLLEGE OF WISCONSIN   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

G PROTEIN COUPLED RECEPTOR; PRAZIQUANTEL; SEROTONIN 2B RECEPTOR; ANTHELMINTIC AGENT; SEROTONIN 2 AGONIST;

CONCENTRATION (COMPOSITION); DRUG PRESCRIBING; INFECTIOUS DISEASE; LIGAND; MOLECULAR ANALYSIS; PARASITE; PARASITIC DISEASE; PROTEIN;

ADULT; ANTIHELMINTHIC THERAPY; ARTICLE; BLOOD VESSEL TONE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DISABILITY-ADJUSTED LIFE YEAR; DISEASE BURDEN; ENANTIOMER; HEK293 CELL LINE; HUMAN; HYDROGEN BOND; IMMUNE RESPONSE; IMMUNOMODULATION; LARVAL STAGE; MESENTERY BLOOD VESSEL; POLYPHARMACOLOGY; SCHISTOSOMIASIS; STEREOISOMERISM; WORLD HEALTH ORGANIZATION; ANIMAL; CELL LINE; COMPUTER SIMULATION; DRUG EFFECT; FEMALE; MESENTERIC ARTERY; MESENTERIC VEIN; METABOLISM; MOUSE; MYOGRAPHY; PARTIAL AGONISM; SCHISTOSOMA MANSONI; SCHISTOSOMIASIS MANSONI; VASOCONSTRICTION;

SCHISTOSOMATIDAE;

ANIMALS; ANTHELMINTICS; CELL LINE; COMPUTER SIMULATION; DRUG PARTIAL AGONISM; FEMALE; HUMANS; MESENTERIC ARTERIES; MESENTERIC VEINS; MICE; MYOGRAPHY; PRAZIQUANTEL; RECEPTOR, SEROTONIN, 5-HT2B; SCHISTOSOMA MANSONI; SCHISTOSOMIASIS MANSONI; SEROTONIN 5-HT2 RECEPTOR AGONISTS; VASOCONSTRICTION;

EID: 85037138864     PISSN: None     EISSN: 20411723     Source Type: Journal    
DOI: 10.1038/s41467-017-02084-0     Document Type: Article

References (35)

1. Hotez, P. J., et al. Helminth infections: The great neglected tropical diseases. J. Clin. Invest. 118, 1311-1321 (2008).
2. Ross, A. G. P., et al. Schistosomiasis. NEJM 346, 1212-1220 (2002).
3. Wilson, R. A., Coulson, P. S. Schistosoma mansoni: Dynamics of migration through the vascular system of the mouse. Parasitology 92, 83-100 (1986).
4. Hotez, P. J., Fenwick, A. Schistosomiasis in Africa: An emerging tragedy in our new global health decade. PLoS Negl. Trop. Dis. 3, e485 (2009).
5. Hotez, P. J., Engels, D., Fenwick, A., Savioli, L. Africa is desperate for praziquantel. Lancet 376, 496-498 (2010).
6. Doenhoff, M. J., et al. Praziquantel: Its use in control of schistosomiasis in sub-Saharan Africa, current research needs. Parasitology 136, 1825-1835 (2009).
7. Melman, S. D., et al. Reduced susceptibility to praziquantel among naturally occurring Kenyan isolates of Schistosoma mansoni. PLoS Negl. Trop. Dis. 3, e504 (2009).
8. Bergquist, R., Utzinger, J., Keiser, J. Controlling schistosomiasis with praziquantel: How much longer without a viable alternative? Infect. Dis. Poverty 6, 74 (2017).
9. Chan, J. D., et al. Ergot alkaloids (Re)generate new leads as antiparasitics. PLoS Negl. Trop. Dis. 9, e0004063 (2015).
10. Bottegoni, G., Kufareva, I., Totrov, M., Abagyan, R. Four-dimensional docking: A fast, accurate account of discrete receptor flexibility in ligand docking. J. Med. Chem. 52, 397-406 (2009).
11. Kufareva, I., Ilatovskiy, A. V., Abagyan, R. Pocketome: An encyclopedia of small-molecule binding sites in 4D. Nucleic Acids Res. 40, D535-540 (2012).
12. Roth, B. L., et al. Salvinorin A: A potent naturally occurring nonnitrogenous kappa opioid selective agonist. Proc. Natl Acad. Sci. USA 99, 11934-11939 (2002).
13. Woelfle, M., et al. Resolution of praziquantel. PLoS Negl. Trop. Dis. 5, e1260 (2011).
14. Chubb, J. M., Bennett, J. L., Akera, T., Brody, T. M. Effects of praziquantel, a new anthelmintic, on electromechanical properties of isolated rat atria. J. Pharmacol. Exp. Ther. 207, 284-293 (1978).
15. Jim, K., Triggle, D. J. Actions of praziquantel, 1-methyladenine in guinea-Pig Ileal longitudinal muscle. Can. J. Physiol. Pharmacol. 57, 1460-1462 (1979).
16. Meyer, T., et al. Taste, a new incentive to switch to (R)-praziquantel in schistosomiasis treatment. PLoS Negl. Trop. Dis. 3, e357 (2009).
17. Zamanian, M., et al. The repertoire of G protein-coupled receptors in the human parasite Schistosoma mansoni, the model organism Schmidtea mediterranea. BMC Genom. 12, 596 (2011).
18. Chan, J. D., et al. A miniaturized screen of a Schistosoma mansoni serotonergic G protein-coupled receptor identifies novel classes of parasite-selective inhibitors. PLoS Pathog. 12, e1005651 (2016).
19. Angelucci, F., et al. The anti-schistosomal drug praziquantel is an adenosine antagonist. Parasitology 134, 1215-1221 (2007).
20. Meister, I., et al. Activity of praziquantel enantiomers, main metabolites against Schistosoma mansoni. Antimicrob. Agents Chemother. 58, 5466-5472 (2014).
21. Buttle, G. A., Khayyal, M. T. Rapid hepatic shift of worms in mice infected with Schistosoma mansoni after a single injection of tartar emetic. Nature 194, 780-781 (1962).
22. Vanhoutte, P. M. Serotonin, the vascular wall. Int. J. Cardiol. 14, 189-203 (1987).
23. Watts, S. W., Morrison, S. F., Davis, R. P., Barman, S. M. Serotonin, blood pressure regulation. Pharmacol. Rev. 64, 359-388 (2012).
24. Olliaro, P., Delgado-Romero, P., Keiser, J. The little we know about the pharmacokinetics, pharmacodynamics of praziquantel (racemate, R-enantiomer). J. Antimicrob. Chemother. 69, 863-870 (2014).
25. Botros, S. S., El-Din, S. H., El-Lakkany, N. M., Sabra, A. N., Ebeid, F. A. Drugmetabolizing enzymes, praziquantel bioavailability in mice harboring Schistosoma mansoni isolates of different drug susceptibilities. J. Parasitol. 92, 1344-1349 (2006).
26. Silva, C. L., Morel, N., Lenzi, H. L., Noel, F. Increased reactivity to 5-hydroxytryptamine of portal veins from mice infected with Schistosoma mansoni. Comp. Biochem. Physiol. A. Mol. Integr. Physiol. 120, 417-423 (1998).
27. Sarin, S. K., Mosca, P., Sabba, C., Groszmann, R. J. Hyperdynamic circulation in a chronic murine schistosomiasis model of portal hypertension. Hepatology 13, 581-584 (1991).
28. Ebrahimkhani, M. R., et al. Stimulating healthy tissue regeneration by targeting the 5-HT(2)B receptor in chronic liver disease. Nat. Med. 17, 1668-1673 (2011).
29. Anthony, B., Allen, J. T., Li, Y. S., McManus, D. P. Hepatic stellate cells, parasite-induced liver fibrosis. Parasites Vectors 3, 60 (2010).
30. Wacker, D., et al. Crystal structure of an LSD-bound human serotonin receptor. Cell 168, 377-389 (2017). e312.
31. Chen, Y. C., Totrov, M., Abagyan, R. Docking to multiple pockets or ligand fields for screening, activity prediction, scaffold hopping. Future Med. Chem. 6, 1741-1755 (2014).
32. Totrov, M. Atomic property fields: Generalized 3D pharmacophoric potential for automated ligand superposition, pharmacophore elucidation, 3D QSAR. Chem. Biol. Drug Des. 71, 15-27 (2008).
33. Gaulton, A., et al. The ChEMBL database in 2017. Nucleic Acids Res. 45, D945-D954 (2017).
34. Halpern, W., Mulvany, M. J. Tension responses to small length changes of vascular smooth muscle cells [proceedings]. J. Physiol. 265, 21P-23P (1977).
35. Warshaw, D. M., Mulvany, M. J., Halpern, W. Mechanical, morphological properties of arterial resistance vessels in young, old spontaneously hypertensive rats. Circ. Res. 45, 250-259 (1979).