title: l-Cystine Diamides as l-Cystine Crystallization Inhibitors for Cystinuria.
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.
authors.affiliation: Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey , 160 Frelinghuysen Road, Piscataway, New Jersey 08854, United States.
authors.forename: Longqin
authors.initials: L
authors.lastname: Hu
authors.affiliation: Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey , 160 Frelinghuysen Road, Piscataway, New Jersey 08854, United States.
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Yang
authors.affiliation: Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey , 160 Frelinghuysen Road, Piscataway, New Jersey 08854, United States.
authors.forename: Herve
authors.initials: H
authors.lastname: Aloysius
authors.affiliation: Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey , 160 Frelinghuysen Road, Piscataway, New Jersey 08854, United States.
authors.forename: Haifa
authors.initials: H
authors.lastname: Albanyan
authors.affiliation: Department of Genetics, Rutgers, The State University of New Jersey , Piscataway, New Jersey 08854, United States.
authors.forename: Min
authors.initials: M
authors.lastname: Yang
authors.affiliation: Dassault Systemes BioVIA Corp , San Diego, California 92121, United States.
authors.forename: Jian-Jie
authors.initials: JJ
authors.lastname: Liang
authors.affiliation: Molecular Design Institute, Department of Chemistry, New York University , New York, New York 10003, United States.
authors.forename: Anthony
authors.initials: A
authors.lastname: Yu
authors.affiliation: Molecular Design Institute, Department of Chemistry, New York University , New York, New York 10003, United States.
authors.forename: Alexander
authors.initials: A
authors.lastname: Shtukenberg
authors.affiliation: Molecular Design Institute, Department of Chemistry, New York University , New York, New York 10003, United States.
authors.forename: Laura N
authors.initials: LN
authors.lastname: Poloni
authors.affiliation: Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey , 160 Frelinghuysen Road, Piscataway, New Jersey 08854, United States.|High Performance and Research Computing, Office of Advanced Research Computing, Rutgers, The State University of New Jersey , Piscataway, New Jersey 08854, United States.
authors.forename: Vladyslav
authors.initials: V
authors.lastname: Kholodovych
authors.affiliation: Department of Genetics, Rutgers, The State University of New Jersey , Piscataway, New Jersey 08854, United States.
authors.forename: Jay A
authors.initials: JA
authors.lastname: Tischfield
authors.affiliation: Nephrology Division, NYU Langone Medical Center , New York, New York 10016, United States.
authors.forename: David S
authors.initials: DS
authors.lastname: Goldfarb
authors.affiliation: Molecular Design Institute, Department of Chemistry, New York University , New York, New York 10003, United States.
authors.forename: Michael D
authors.initials: MD
authors.lastname: Ward
authors.affiliation: Department of Genetics, Rutgers, The State University of New Jersey , Piscataway, New Jersey 08854, United States.
authors.forename: Amrik
authors.initials: A
authors.lastname: Sahota
mesh_terms: D000284:Administration, Oral; D026923:Amino Acid Transport Systems, Basic / Q000172:deficiency; D026921:Amino Acid Transport Systems, Neutral / Q000172:deficiency; D000818:Animals; D003553:Cystine / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*; D003555:Cystinuria / Q000188:drug therapy* / Q000235:genetics; D003958:Diamide / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*; D004195:Disease Models, Animal; D008297:Male; D051379:Mice; D018345:Mice, Knockout; D008958:Models, Molecular; D015394:Molecular Structure
chemical_list: D026923:Amino Acid Transport Systems, Basic; D026921:Amino Acid Transport Systems, Neutral; C489858:Slc3a1 protein, mouse; D003958:Diamide; D003553:Cystine