L -Cystine Diamides as l -Cystine Crystallization Inhibitors for Cystinuria

Longqin Hu; Yanhui Yang; Herve Aloysius; Haifa Albanyan; Min Yang; Jian Jie Liang; Anthony Yu; Alexander Shtukenberg; Laura N. Poloni; Vladyslav Kholodovych; Jay A. Tischfield; David S. Goldfarb; Michael D. Ward; Amrik Sahota

doi:10.1021/acs.jmedchem.6b00647

L -Cystine Diamides as l -Cystine Crystallization Inhibitors for Cystinuria

Longqin Hu, Yanhui Yang, Herve Aloysius, Haifa Albanyan, Min Yang, Jian Jie Liang, Anthony Yu, Alexander Shtukenberg, Laura N. Poloni, Vladyslav Kholodovych, Jay A. Tischfield, David S. Goldfarb, Michael D. Ward, Amrik Sahota

Chemistry

Research output: Contribution to journal › Article

Abstract

l-Cystine bismorpholide (1a) and l-cystine bis(N′-methylpiperazide) (1b) were seven and twenty-four times more effective than l-cystine dimethyl ester (CDME) in increasing the metastable supersaturation range of l-cystine, respectively, effectively inhibiting l-cystine crystallization. This behavior can be attributed to inhibition of crystal growth at microscopic length scale, as revealed by atomic force microscopy. Both 1a and 1b are more stable than CDME, and 1b was effective in vivo in a knockout mouse model of cystinuria.

Original language	English (US)
Pages (from-to)	7293-7298
Number of pages	6
Journal	Journal of Medicinal Chemistry
Volume	59
Issue number	15
DOIs	https://doi.org/10.1021/acs.jmedchem.6b00647
State	Published - Aug 11 2016

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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Hu, L., Yang, Y., Aloysius, H., Albanyan, H., Yang, M., Liang, J. J., Yu, A., Shtukenberg, A., Poloni, L. N., Kholodovych, V., Tischfield, J. A., Goldfarb, D. S., Ward, M. D., & Sahota, A. (2016). L -Cystine Diamides as l -Cystine Crystallization Inhibitors for Cystinuria. Journal of Medicinal Chemistry, 59(15), 7293-7298. https://doi.org/10.1021/acs.jmedchem.6b00647

L -Cystine Diamides as l -Cystine Crystallization Inhibitors for Cystinuria. / Hu, Longqin; Yang, Yanhui; Aloysius, Herve; Albanyan, Haifa; Yang, Min; Liang, Jian Jie; Yu, Anthony; Shtukenberg, Alexander; Poloni, Laura N.; Kholodovych, Vladyslav; Tischfield, Jay A.; Goldfarb, David S.; Ward, Michael D.; Sahota, Amrik.

In: Journal of Medicinal Chemistry, Vol. 59, No. 15, 11.08.2016, p. 7293-7298.

Research output: Contribution to journal › Article

Hu, Longqin ; Yang, Yanhui ; Aloysius, Herve ; Albanyan, Haifa ; Yang, Min ; Liang, Jian Jie ; Yu, Anthony ; Shtukenberg, Alexander ; Poloni, Laura N. ; Kholodovych, Vladyslav ; Tischfield, Jay A. ; Goldfarb, David S. ; Ward, Michael D. ; Sahota, Amrik. / L -Cystine Diamides as l -Cystine Crystallization Inhibitors for Cystinuria. In: Journal of Medicinal Chemistry. 2016 ; Vol. 59, No. 15. pp. 7293-7298.

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abstract = "l-Cystine bismorpholide (1a) and l-cystine bis(N′-methylpiperazide) (1b) were seven and twenty-four times more effective than l-cystine dimethyl ester (CDME) in increasing the metastable supersaturation range of l-cystine, respectively, effectively inhibiting l-cystine crystallization. This behavior can be attributed to inhibition of crystal growth at microscopic length scale, as revealed by atomic force microscopy. Both 1a and 1b are more stable than CDME, and 1b was effective in vivo in a knockout mouse model of cystinuria.",

author = "Longqin Hu and Yanhui Yang and Herve Aloysius and Haifa Albanyan and Min Yang and Liang, {Jian Jie} and Anthony Yu and Alexander Shtukenberg and Poloni, {Laura N.} and Vladyslav Kholodovych and Tischfield, {Jay A.} and Goldfarb, {David S.} and Ward, {Michael D.} and Amrik Sahota",

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AU - Hu, Longqin

AU - Yang, Yanhui

AU - Aloysius, Herve

AU - Albanyan, Haifa

AU - Yang, Min

AU - Liang, Jian Jie

AU - Yu, Anthony

AU - Shtukenberg, Alexander

AU - Poloni, Laura N.

AU - Kholodovych, Vladyslav

AU - Tischfield, Jay A.

AU - Goldfarb, David S.

AU - Ward, Michael D.

AU - Sahota, Amrik

PY - 2016/8/11

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AB - l-Cystine bismorpholide (1a) and l-cystine bis(N′-methylpiperazide) (1b) were seven and twenty-four times more effective than l-cystine dimethyl ester (CDME) in increasing the metastable supersaturation range of l-cystine, respectively, effectively inhibiting l-cystine crystallization. This behavior can be attributed to inhibition of crystal growth at microscopic length scale, as revealed by atomic force microscopy. Both 1a and 1b are more stable than CDME, and 1b was effective in vivo in a knockout mouse model of cystinuria.

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