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Combined activity of the cancer metabolism inhibitor MPC-8640 and 5-fluorouracil in xenograft models

Autor: Orvelin Roman, Lori Fotheringham, Robert O. Carlson, Brita Brown, J. Scott Patton, Thomas B. Douce, Lynn DeMie, Vijay Baichwal, Chad Bradford, Leslie Reeves

Publikováno v: Journal of Clinical Oncology. 30:e13581-e13581

e13581 Background: Nicotinamide (Nam) phosphoribosyltransferase (Nampt) catalyzes the rate-limiting step in NAD biosynthesis from Nam. Nampt inhibition causes NAD depletion, inhibition of ATP synthesis and cell death. MPI-0487316 is a selective Nampt

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8f0e9fd9d2e47b49a12108ed4f4a3728
https://doi.org/10.1200/jco.2012.30.15_suppl.e13581

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Abstract 3233: Comparative in vitro and in vivo metabolism of MPC-3100, an oral HSP90 inhibitor, in rat, dog, monkey and human

Autor: J. Scott Patton, Leslie Reeves, Ashok C. Bajji, Vijay Baichwal, Daniel Wettstein, Chad Bradford, Richard Trovato, Se-Ho Kim, Lynn DeMie, Damon I. Papac, Rajendra P. Tangallapally, K Bulka, Orvelin Roman, Gary Mather, Benjamin Markovitz

Publikováno v: Cancer Research. 71:3233-3233

MPC-3100, an 8, 9-disubstituted purine, is an orally bioavailable HSP90 inhibitor currently in Phase 1 clinical development. The objectives of these studies were to compare the metabolism of MPC-3100 in preclinical species to select the species most

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::48cf8c9f85f0cfe58b9aab8f51362854
https://doi.org/10.1158/1538-7445.am2011-3233

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Abstract 3526: Coadministration of nicotinic acid with the Nampt inhibitor MPC-9528 enhances antitumor activity in Naprt deficient cancer cells in culture and in xenografts

Autor: Ryan T. Terry-Lorenzo, Damon I. Papac, Rosann Robinson, Tracey C. Fleischer, Daniel M. Cimbora, Lynn DeMie, Andrew D. Gassman, J. Jay Boniface, Vijay Baichwal, Thomas B. Douce, Ashley Peterson, Robert O. Carlson

Publikováno v: Cancer Research. 71:3526-3526

Background: The tumoricidal small molecule MPC-9528 is a picomolar inhibitor of nicotinamide phosphoribosyltransferase (Nampt). Nampt catalyzes the first and rate-limiting step in NAD synthesis from nicotinamide. Nicotinic acid phosphoribosyltransfer

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e67537febe6cb2a98883e170d50ad881
https://doi.org/10.1158/1538-7445.am2011-3526

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Abstract 4386: Administration of nicotinic acid reduces or prevents adverse effects of MPC-9528, a potent and selective Nampt inhibitor

Autor: Lynn DeMie, Gary Mather, Chad Bradford, Anna Costa, Lori Fotheringham, Valerie L. Belcher, Orvelin Roman

Publikováno v: Cancer Research. 71:4386-4386

Background: Inhibition of Nampt in cancer cell lines decreases NAD levels and induces cell death. We evaluate the potential toxicity of MPC-9528, a Nampt inhibitor, and investigate the effects of coadministration of nicotinic acid (NA), the substrate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f99e432922f9b73dcf5a31327633a356
https://doi.org/10.1158/1538-7445.am2011-4386

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Abstract 577: Basal NAD levels and Nampt expression correlate with in vitro and in vivo sensitivity of tumor cell lines to the Nampt inhibitor MPC-9528

Autor: Damon I. Papac, Ryan T. Terry-Lorenzo, Vijay Baichwal, Jeff S. Flick, Tracey C. Fleischer, Andrew D. Gassman, J. Jay Boniface, Ashley Peterson, Lynn DeMie, Jeremy P. Green, Robert O. Carlson, Rosann Robinson, Daniel M. Cimbora, Siavash Ghaffari

Publikováno v: Cancer Research. 71:577-577

Background: MPC-9528 is a potent and selective inhibitor of the NAD biosynthetic enzyme nicotinamide phosphoribosyltransferase (Nampt). Inhibition of Nampt by MPC-9528 causes depletion of cellular NAD followed by a decrease in ATP and cell death. Can

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e11d2dcf73c9518e51ab6eb7d198568d
https://doi.org/10.1158/1538-7445.am2011-577

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Abstract 3237: Evaluation of the pharmacokinetics and efficacy of a novel pro-drug of the HSP90 inhibitor, MPC-3100, designed with improved solubility

Autor: Leslie Reeves, Rajendra P. Tangallapally, Daniel P. Parker, Se-Ho Kim, Damon I. Papac, In Chul Kim, Brian Clemetson, Brian Hachey, Richard Trovato, Chad Bradford, J. Scott Patton, Vijay Baichwal, Ashok C. Bajji, Lynn DeMie, Daniel Wettstein, Christin Christensen

Publikováno v: Cancer Research. 71:3237-3237

MPC-3100 is a synthetic, orally bioavailable HSP90 inhibitor in clinical development. The low solubility of this compound requires a solubility enhancing agent to enable uniform oral bioavailability. A pro-drug of MPC-3100 with enhanced aqueous solub

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::425bdacb30bf4be8abc482c57c1e378a
https://doi.org/10.1158/1538-7445.am2011-3237

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Abstract LB-288: MPI-0486348: A novel inhibitor of nicotinamide phosphoribosyltransferase (Nampt) induces tumor regression in a preclinical model

Autor: Ryan T. Terry-Lorenzo, Kirill Ostanin, Mark A. Hess, J. Adam Willardsen, Jeffrey W. Lockman, Lynn DeMie, Chad Bradford, Jeremy P. Green, Vijay Baichwal, Leslie Reeves, Rena McKinnon, Damon I. Papac, Tracey C. Fleischer

Publikováno v: Cancer Research. 70:LB-288

Background: Nicotinamide phosphoribosyltransferase (Nampt) catalyzes the first step in the recycling of nicotinamide into NAD. Cancer cells develop dependence on Nampt due to increased energy requirements and the elevated activity of NAD consuming en

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1db1a28430397e235fafd1bb23d337f8
https://doi.org/10.1158/1538-7445.am10-lb-288

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