ProCite
RefWorks
Reference Manager
BibTeX
Zotero
EndNote
-
1.
Caffrey CR, 2007. Chemotherapy of schistosomiasis: present and future. Curr Opin Chem Biol 11: 433–439.
-
2.
Utzinger J, N'goran EK, Caffrey CR, Keiser J, 2011. From innovation to application: social-ecological context, diagnostics, drugs and integrated control of schistosomiasis. Acta Trop 120: S121–S137.
-
3.
Gryseels B, 2012. Schistosomiasis. Infect Dis Clin North Am 26: 383–397.
-
4.
Olliaro P, Delgado-Romero P, Keiser J, 2014. The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer). J Antimicrob Chemother 69: 863–870.
-
5.
Bernauer K, Link H, Stohler H, 1980. Antiandrogenic and schistosomicidal imidazolidine derivatives. US Patent 4,234,736.
-
6.
Forget E, Félix H, Notteghem MJ, Léger N, 1982. Appréciation de l'activité de dérivés schistosomicides en microscopie électronique. Bull Soc Pathol Exot 75: 192–200.
-
7.
Hansen JB, Hafliger O, 1983. Determination of the dissociation constant of a weak acid using a dissolution rate method. J Pharm Sci 72: 429–431.
-
8.
Link H, Stohler HR, 1984. 3-Arylhydantoine, eine substanzklasse mit schistosomizider wirkung. Eur J Med Chem 19: 261–265.
-
9.
Keiser J, Vargas M, Vennerstrom JL, 2010. Activity of antiandrogens against juvenile and adult Schistosoma mansoni in mice. J Antimicrob Chemother 65: 1991–1995.
-
10.
de Mendonça RL, Escrivá H, Bouton D, Laudet V, Pierce RJ, 2000. Hormones and nuclear receptors in schistosome development. Parasitol Today 16: 233–240.
-
11.
Battmann T, Bonfils A, Branche C, Humbert J, Goubet F, Teutsch G, Philibert D, 1994. Ru 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsuitism. J Steroid Biochem Molec Biol 48: 55–60.
-
12.
Mohler ML, Bohl CE, Jones A, Coss CC, Narayanan R, He Y, Hwang DJ, Dalton JT, Miller DD, 2009. Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. J Med Chem 52: 3597–3617.
-
13.
Féau C, Arnold LA, Kosinski A, Guy RK, 2009. A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors. J Biomol Screen 14: 43–48.
-
14.
Igawa T, Lin FF, Lee MS, Karan D, Batra SK, Lin MF, 2002. Establishment and characterization of androgen-independent human prostate cancer LNCaP cell model. Prostate 50: 222–235.
-
15.
Veldscholte J, Berrevoets CA, Ris-Stalpers C, Kuiper GG, Jenster G, Trapman J, Brinkmann AO, Mulder E, 1992. The androgen receptor in LNCaP cells contains a mutation in the ligand binding domain which affects steroid binding characteristics and response to antiandrogens. J Steroid Biochem Mol Biol 41: 665–669.
-
16.
Olea N, Sakabe K, Soto AM, Sonnenschein C, 1990. The proliferative effect of “anti-androgens” on the androgen-sensitive human prostate tumor cell line LNCaP. Endocrinology 126: 1457–1463.
-
17.
De Launoit Y, Veilleux R, Dufour M, Simard J, Labrie F, 1991. Characteristics of the biphasic action of androgens and the potent antiproliferative effects of the new pure antiestrogen EM-139 on cell cycle kinetic parameters in LNCaP human prostatic cancer cells. Cancer Res 51: 5165–5170.
-
18.
Veldscholte J, Berrevoets CA, Brinkmann AO, Grootegoed JA, Mulder E, 1992. Anti-androgens and the mutated androgen receptor of LNCaP cells: differential effects on binding affinity, heat-shock protein interaction, and transcription activation. Biochemistry 31: 2393–2399.
-
19.
Georget V, Térouanne B, Nicolas J-C, Sultan C, 2002. Mechanism of antiandrogen action: key role of hsp90 in conformational change and transcriptional activity of the androgen receptor. Biochemistry 41: 11824–11831.
-
20.
Fantappié MR, Galina A, de Medonca RL, Furtado DR, Secor WE, Colley DG, Corrêa-Oliveira R, Freeman G Jr, Tempone AJ, de Camargo LL, Rumjanek FD, 1999. Molecular characterization of a NADH ubiquinone oxidoreductase subunit 5 from Schistosoma mansoni and inhibition of mitochondrial respiratory chain function by testosterone. Mol Cell Biochem 202: 149–158.
-
21.
Morales-Montor J, Mohamed F, Ghaleb AM, Baig S, Hallal-Calleros C, Damian RT, 2001. In vitro effects of hypothalamic-pituitary-adrenal axis (HPA) hormones on Schistosoma mansoni. J Parasitol 87: 1132–1139.
| Past two years | Past Year | Past 30 Days | |
|---|---|---|---|
| Abstract Views | 225 | 192 | 18 |
| Full Text Views | 332 | 13 | 1 |
| PDF Downloads | 93 | 8 | 1 |
Antischistosomal versus Antiandrogenic Properties of Aryl Hydantoin Ro 13-3978
Chunkai Wang
Chunkai Wang
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Chunkai Wang in
Current site
Google Scholar
PubMed
Search for other papers by Chunkai Wang in
Current site
Google Scholar
PubMed
Qingjie Zhao
Qingjie Zhao
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Qingjie Zhao in
Current site
Google Scholar
PubMed
Search for other papers by Qingjie Zhao in
Current site
Google Scholar
PubMed
Jaeki Min
Jaeki Min
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Jaeki Min in
Current site
Google Scholar
PubMed
Search for other papers by Jaeki Min in
Current site
Google Scholar
PubMed
Sakthivel Muniyan
Sakthivel Muniyan
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Sakthivel Muniyan in
Current site
Google Scholar
PubMed
Search for other papers by Sakthivel Muniyan in
Current site
Google Scholar
PubMed
Mireille Vargas
Mireille Vargas
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Mireille Vargas in
Current site
Google Scholar
PubMed
Search for other papers by Mireille Vargas in
Current site
Google Scholar
PubMed
Xiaofang Wang
Xiaofang Wang
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Xiaofang Wang in
Current site
Google Scholar
PubMed
Search for other papers by Xiaofang Wang in
Current site
Google Scholar
PubMed
Yuxiang Dong
Yuxiang Dong
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Yuxiang Dong in
Current site
Google Scholar
PubMed
Search for other papers by Yuxiang Dong in
Current site
Google Scholar
PubMed
R. Kiplin Guy
R. Kiplin Guy
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by R. Kiplin Guy in
Current site
Google Scholar
PubMed
Search for other papers by R. Kiplin Guy in
Current site
Google Scholar
PubMed
Ming-Fong Lin
Ming-Fong Lin
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Ming-Fong Lin in
Current site
Google Scholar
PubMed
Search for other papers by Ming-Fong Lin in
Current site
Google Scholar
PubMed
Jennifer Keiser
Jennifer Keiser
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Jennifer Keiser in
Current site
Google Scholar
PubMed
Search for other papers by Jennifer Keiser in
Current site
Google Scholar
PubMed
Jonathan L. Vennerstrom
Jonathan L. Vennerstrom
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, Nebraska; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, and University of Basel, Basel, Switzerland
Search for other papers by Jonathan L. Vennerstrom in
Current site
Google Scholar
PubMed
Search for other papers by Jonathan L. Vennerstrom in
Current site
Google Scholar
PubMed
In the early 1980s, the antischistosomal aryl hydantoin Ro 13-3978 (AH01), a close structural analogue of the androgen receptor antagonist nilutamide, was discovered. Administration of 100 mg/kg oral doses of AH01 to mice infected with adult and juvenile Schistosoma mansoni produced 95% and 64% total worm burden reductions, confirming its high activity against adult worms, and showing that AH01 is also effective against juvenile infections. AH01 had no measureable interaction with the androgen receptor in a ligand competition assay, but it did block dihydrotestosterone-induced cell proliferation in an androgen-dependent human prostate cancer cell line. For AH01, nilutamide, and three closely related aryl hydantoin derivatives, there was no correlation between antischistosomal activity and androgen receptor interaction.
Author Notes
Financial support: This investigation received financial support from the NIH (R21 AI097802-02) and the Swiss National Science Foundation (PPOOP3-135170 and 320030-149310).
Authors' addresses: Chunkai Wang, Xiaofang Wang, Yuxiang Dong, and Jonathan L. Vennerstrom, Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE, E-mails: chunkai.wang@unmc.edu, xiaofangwang@unmc.edu, ydong@unmc.edu, and jvenners@unmc.edu. Qingjie Zhao, Department of Pathology, University of Michigan, Ann Arbor, MI, E-mail: chemwo@gmail.com. Jaeki Min and R. Kiplin Guy, Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN, E-mails: jaeki.min@stjude.org and kip.guy@stjude.org. Sakthivel Muniyan and Ming-Fong Lin, Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, Omaha, NE, E-mails: s.muniyan@unmc.edu and mlin@unmc.edu. Mireille Vargas and Jennifer Keiser, Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland, E-mails: mireille.vargas@unibas.ch and jennifer.keiser@unibas.ch.
ProCite
RefWorks
Reference Manager
BibTeX
Zotero
EndNote
-
1.
Caffrey CR, 2007. Chemotherapy of schistosomiasis: present and future. Curr Opin Chem Biol 11: 433–439.
-
2.
Utzinger J, N'goran EK, Caffrey CR, Keiser J, 2011. From innovation to application: social-ecological context, diagnostics, drugs and integrated control of schistosomiasis. Acta Trop 120: S121–S137.
-
3.
Gryseels B, 2012. Schistosomiasis. Infect Dis Clin North Am 26: 383–397.
-
4.
Olliaro P, Delgado-Romero P, Keiser J, 2014. The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer). J Antimicrob Chemother 69: 863–870.
-
5.
Bernauer K, Link H, Stohler H, 1980. Antiandrogenic and schistosomicidal imidazolidine derivatives. US Patent 4,234,736.
-
6.
Forget E, Félix H, Notteghem MJ, Léger N, 1982. Appréciation de l'activité de dérivés schistosomicides en microscopie électronique. Bull Soc Pathol Exot 75: 192–200.
-
7.
Hansen JB, Hafliger O, 1983. Determination of the dissociation constant of a weak acid using a dissolution rate method. J Pharm Sci 72: 429–431.
-
8.
Link H, Stohler HR, 1984. 3-Arylhydantoine, eine substanzklasse mit schistosomizider wirkung. Eur J Med Chem 19: 261–265.
-
9.
Keiser J, Vargas M, Vennerstrom JL, 2010. Activity of antiandrogens against juvenile and adult Schistosoma mansoni in mice. J Antimicrob Chemother 65: 1991–1995.
-
10.
de Mendonça RL, Escrivá H, Bouton D, Laudet V, Pierce RJ, 2000. Hormones and nuclear receptors in schistosome development. Parasitol Today 16: 233–240.
-
11.
Battmann T, Bonfils A, Branche C, Humbert J, Goubet F, Teutsch G, Philibert D, 1994. Ru 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsuitism. J Steroid Biochem Molec Biol 48: 55–60.
-
12.
Mohler ML, Bohl CE, Jones A, Coss CC, Narayanan R, He Y, Hwang DJ, Dalton JT, Miller DD, 2009. Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. J Med Chem 52: 3597–3617.
-
13.
Féau C, Arnold LA, Kosinski A, Guy RK, 2009. A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors. J Biomol Screen 14: 43–48.
-
14.
Igawa T, Lin FF, Lee MS, Karan D, Batra SK, Lin MF, 2002. Establishment and characterization of androgen-independent human prostate cancer LNCaP cell model. Prostate 50: 222–235.
-
15.
Veldscholte J, Berrevoets CA, Ris-Stalpers C, Kuiper GG, Jenster G, Trapman J, Brinkmann AO, Mulder E, 1992. The androgen receptor in LNCaP cells contains a mutation in the ligand binding domain which affects steroid binding characteristics and response to antiandrogens. J Steroid Biochem Mol Biol 41: 665–669.
-
16.
Olea N, Sakabe K, Soto AM, Sonnenschein C, 1990. The proliferative effect of “anti-androgens” on the androgen-sensitive human prostate tumor cell line LNCaP. Endocrinology 126: 1457–1463.
-
17.
De Launoit Y, Veilleux R, Dufour M, Simard J, Labrie F, 1991. Characteristics of the biphasic action of androgens and the potent antiproliferative effects of the new pure antiestrogen EM-139 on cell cycle kinetic parameters in LNCaP human prostatic cancer cells. Cancer Res 51: 5165–5170.
-
18.
Veldscholte J, Berrevoets CA, Brinkmann AO, Grootegoed JA, Mulder E, 1992. Anti-androgens and the mutated androgen receptor of LNCaP cells: differential effects on binding affinity, heat-shock protein interaction, and transcription activation. Biochemistry 31: 2393–2399.
-
19.
Georget V, Térouanne B, Nicolas J-C, Sultan C, 2002. Mechanism of antiandrogen action: key role of hsp90 in conformational change and transcriptional activity of the androgen receptor. Biochemistry 41: 11824–11831.
-
20.
Fantappié MR, Galina A, de Medonca RL, Furtado DR, Secor WE, Colley DG, Corrêa-Oliveira R, Freeman G Jr, Tempone AJ, de Camargo LL, Rumjanek FD, 1999. Molecular characterization of a NADH ubiquinone oxidoreductase subunit 5 from Schistosoma mansoni and inhibition of mitochondrial respiratory chain function by testosterone. Mol Cell Biochem 202: 149–158.
-
21.
Morales-Montor J, Mohamed F, Ghaleb AM, Baig S, Hallal-Calleros C, Damian RT, 2001. In vitro effects of hypothalamic-pituitary-adrenal axis (HPA) hormones on Schistosoma mansoni. J Parasitol 87: 1132–1139.
| Past two years | Past Year | Past 30 Days | |
|---|---|---|---|
| Abstract Views | 225 | 192 | 18 |
| Full Text Views | 332 | 13 | 1 |
| PDF Downloads | 93 | 8 | 1 |