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

Research output: Contribution to journalArticle

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 languageEnglish (US)
Pages (from-to)7293-7298
Number of pages6
JournalJournal of Medicinal Chemistry
Volume59
Issue number15
DOIs
StatePublished - Aug 11 2016

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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  • Cite this

    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