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Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor.
Bioorg Med Chem. 2013 Sep 1;21(17):5081-97. doi: 10.1016/j.bmc.2013.06.045. Epub 2013 Jul 1.
Bioorg Med Chem. 2013.
PMID: 23871442
Pharmacological inhibition to examine the role of DGAT1 in dietary lipid absorption in rodents and humans.
Maciejewski BS, LaPerle JL, Chen D, Ghosh A, Zavadoski WJ, McDonald TS, Manion TB, Mather D, Patterson TA, Hanna M, Watkins S, Gibbs EM, Calle RA, Steppan CM.
Maciejewski BS, et al. Among authors: laperle jl.
Am J Physiol Gastrointest Liver Physiol. 2013 Jun 1;304(11):G958-69. doi: 10.1152/ajpgi.00384.2012. Epub 2013 Apr 4.
Am J Physiol Gastrointest Liver Physiol. 2013.
PMID: 23558010
Free article.
Clinical Trial.
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Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d]pyrimidine core.
Dow RL, Andrews M, Aspnes GE, Balan G, Michael Gibbs E, Guzman-Perez A, Karki K, Laperle JL, Li JC, Litchfield J, Munchhof MJ, Perreault C, Patel L.
Dow RL, et al. Among authors: laperle jl.
Bioorg Med Chem Lett. 2011 Oct 15;21(20):6122-5. doi: 10.1016/j.bmcl.2011.08.028. Epub 2011 Aug 12.
Bioorg Med Chem Lett. 2011.
PMID: 21908190
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Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
Dow RL, Li JC, Pence MP, Gibbs EM, LaPerle JL, Litchfield J, Piotrowski DW, Munchhof MJ, Manion TB, Zavadoski WJ, Walker GS, McPherson RK, Tapley S, Sugarman E, Guzman-Perez A, DaSilva-Jardine P.
Dow RL, et al. Among authors: laperle jl.
ACS Med Chem Lett. 2011 Mar 18;2(5):407-12. doi: 10.1021/ml200051p. eCollection 2011 May 12.
ACS Med Chem Lett. 2011.
PMID: 24900321
Free PMC article.
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A comprehensive non-clinical evaluation of the CNS penetration potential of antimuscarinic agents for the treatment of overactive bladder.
Callegari E, Malhotra B, Bungay PJ, Webster R, Fenner KS, Kempshall S, LaPerle JL, Michel MC, Kay GG.
Callegari E, et al. Among authors: laperle jl.
Br J Clin Pharmacol. 2011 Aug;72(2):235-46. doi: 10.1111/j.1365-2125.2011.03961.x.
Br J Clin Pharmacol. 2011.
PMID: 21392072
Free PMC article.
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Renal clearance in drug discovery and development: molecular descriptors, drug transporters and disease state.
Feng B, LaPerle JL, Chang G, Varma MV.
Feng B, et al. Among authors: laperle jl.
Expert Opin Drug Metab Toxicol. 2010 Aug;6(8):939-52. doi: 10.1517/17425255.2010.482930.
Expert Opin Drug Metab Toxicol. 2010.
PMID: 20433402
Review.
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