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Full-Text Articles in Medicinal and Pharmaceutical Chemistry

Failure To Ubiquitinate C-Met Leads To Hyperactivation Of Mtor Signaling In A Mouse Model Of Autosomal Dominant Polycystic Kidney Disease, Shan Qin, Mary Taglienti, Surya M. Nauli, Leah Contrino, Ayumi Takakura, Jing Zhou, Jordan A. Kreidberg Oct 2010

Failure To Ubiquitinate C-Met Leads To Hyperactivation Of Mtor Signaling In A Mouse Model Of Autosomal Dominant Polycystic Kidney Disease, Shan Qin, Mary Taglienti, Surya M. Nauli, Leah Contrino, Ayumi Takakura, Jing Zhou, Jordan A. Kreidberg

Pharmacy Faculty Articles and Research

Autosomal dominant polycystic kidney disease (ADPKD) is a common inherited disorder that is caused by mutations at two loci, polycystin 1 (PKD1) and polycystin 2 (PKD2). It is characterized by the formation of multiple cysts in the kidneys that can lead to chronic renal failure. Previous studies have suggested a role for hyperactivation of mammalian target of rapamycin (mTOR) in cystogenesis, but the etiology of mTOR hyperactivation has not been fully elucidated. In this report we have shown that mTOR is hyperactivated. in Pkd1-null mouse cells due to failure of the HGF receptor c-Met to be properly ubiquitinated and subsequently …


Development Of Cytarabine Prodrugs And Delivery Systems For Leukemia Treatment, Bhupender S. Chhikara, Keykavous Parang Jan 2010

Development Of Cytarabine Prodrugs And Delivery Systems For Leukemia Treatment, Bhupender S. Chhikara, Keykavous Parang

Pharmacy Faculty Articles and Research

Importance of the field: Cytarabine is a polar nucleoside drug used for the treatment of myeloid leukemia and non-Hodgkin’s lymphoma. The drug has a short plasma half-life, low stability, and limited bioavailability. Overdosing of patients with continuous infusions may lead to side effects. Thus, various prodrug strategies and delivery systems have been extensively explored to enhance the half-life, stability, and delivery of cytarabine. Among the recent cytarabine prodrugs, amino acid conjugate ValCytarabine and fatty acid derivative CP-4055 (in phase 3 trials) have been investigated for the treatment of leukemia and solid tumors, respectively. Alternatively, delivery systems of cytarabine have …