John Cashman

Summary

Affiliation: Human BioMolecular Research Institute
Country: USA

Publications

  1. ncbi request reprint Human flavin-containing monooxygenase (form 3): polymorphisms and variations in chemical metabolism
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Pharmacogenomics 3:325-39. 2002
  2. ncbi request reprint Some distinctions between flavin-containing and cytochrome P450 monooxygenases
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Biochem Biophys Res Commun 338:599-604. 2005
  3. ncbi request reprint Quantitative analysis of FMO gene mRNA levels in human tissues
    Jun Zhang
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Drug Metab Dispos 34:19-26. 2006
  4. ncbi request reprint Potent Inhibition of Alcohol Self-Administration in Alcohol-Preferring Rats by a κ-Opioid Receptor Antagonist
    John R Cashman
    Human BioMolecular Research Institute, San Diego, California J R C and Behavioral Pharma, Inc, La Jolla, California M R A
    J Pharmacol Exp Ther 350:171-80. 2014
  5. pmc Immunodetection of serum albumin adducts as biomarkers for organophosphorus exposure
    Sigeng Chen
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 344:531-41. 2013
  6. pmc Identification of human butyrylcholinesterase organophosphate-resistant variants through a novel mammalian enzyme functional screen
    Jun Zhang
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 343:673-82. 2012
  7. doi request reprint Substituted heteroaromatic compounds: effect on nicotine self-administration in rats
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Psychopharmacology (Berl) 221:637-48. 2012
  8. doi request reprint Curcumins promote monocytic gene expression related to β-amyloid and superoxide dismutase clearance
    J R Cashman
    Human BioMolecular Research Institute, San Diego, Calif 92121, USA
    Neurodegener Dis 10:274-6. 2012
  9. pmc Transient trimethylaminuria related to menstruation
    Makiko Shimizu
    Laboratory of Drug Metabolism and Pharmacokinetics, Showa Pharmaceutical University, Machida, Tokyo 194 8543, Japan
    BMC Med Genet 8:2. 2007
  10. ncbi request reprint Human flavin-containing monooxygenases
    John R Cashman
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    Annu Rev Pharmacol Toxicol 46:65-100. 2006

Research Grants

  1. Biosensor for real-time chemical monitoring
    John Cashman; Fiscal Year: 2007
  2. New Opioids for Alcoholism
    John Cashman; Fiscal Year: 2006
  3. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2005
  4. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2004
  5. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2003
  6. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2002
  7. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2001
  8. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2000
  9. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2000
  10. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2000

Collaborators

Detail Information

Publications61

  1. ncbi request reprint Human flavin-containing monooxygenase (form 3): polymorphisms and variations in chemical metabolism
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Pharmacogenomics 3:325-39. 2002
    ..Heterogeneity in the relative frequencies of single and multiple site alleles, haplotypes and genotypes of the human FMO3 amongst various ethnic groups suggests population differences...
  2. ncbi request reprint Some distinctions between flavin-containing and cytochrome P450 monooxygenases
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Biochem Biophys Res Commun 338:599-604. 2005
    ..These properties may provide advantages in drug design, and by incorporating FMO detoxication pathways into drug candidates, more drug-like materials may emerge...
  3. ncbi request reprint Quantitative analysis of FMO gene mRNA levels in human tissues
    Jun Zhang
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Drug Metab Dispos 34:19-26. 2006
    ..e., FMO1 in kidney, FMO2 in lung, FMO3 and FMO5 in adult liver), FMO4 mRNA was observed more broadly at relatively comparable levels in liver, kidney, lung, and small intestine...
  4. ncbi request reprint Potent Inhibition of Alcohol Self-Administration in Alcohol-Preferring Rats by a κ-Opioid Receptor Antagonist
    John R Cashman
    Human BioMolecular Research Institute, San Diego, California J R C and Behavioral Pharma, Inc, La Jolla, California M R A
    J Pharmacol Exp Ther 350:171-80. 2014
    ..The results suggest that compound 5: is a potent drug-like κ-opioid receptor antagonist of utility in alcohol cessation medications development. ..
  5. pmc Immunodetection of serum albumin adducts as biomarkers for organophosphorus exposure
    Sigeng Chen
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 344:531-41. 2013
    ....
  6. pmc Identification of human butyrylcholinesterase organophosphate-resistant variants through a novel mammalian enzyme functional screen
    Jun Zhang
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 343:673-82. 2012
    ..The mammalian functional screening approach can serve as a cornerstone for further optimization and screening for OP-resistant hBChEs for potential therapeutic applications...
  7. doi request reprint Substituted heteroaromatic compounds: effect on nicotine self-administration in rats
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Psychopharmacology (Berl) 221:637-48. 2012
    ..e., human cytochrome P-450 2A6, hCYP 2A6) showed inhibition of smoking in humans. However, a comprehensive examination of hCYP 2A6 inhibitors to decrease nicotine self-administration in rats has not been reported...
  8. doi request reprint Curcumins promote monocytic gene expression related to β-amyloid and superoxide dismutase clearance
    J R Cashman
    Human BioMolecular Research Institute, San Diego, Calif 92121, USA
    Neurodegener Dis 10:274-6. 2012
    ..Recursive medicinal chemistry was applied to identify compounds that stimulate the innate immune system for use in the clearance of Aβ in AD and the reversal of neuroinflammation and defective SOD-1 accumulation in ALS...
  9. pmc Transient trimethylaminuria related to menstruation
    Makiko Shimizu
    Laboratory of Drug Metabolism and Pharmacokinetics, Showa Pharmaceutical University, Machida, Tokyo 194 8543, Japan
    BMC Med Genet 8:2. 2007
    ....
  10. ncbi request reprint Human flavin-containing monooxygenases
    John R Cashman
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    Annu Rev Pharmacol Toxicol 46:65-100. 2006
    ..Although exhaustive examples are not available, physiological factors can influence FMO function, and this may have implications for the clinical significance of FMO and a role in human disease...
  11. doi request reprint Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Bioorg Med Chem 17:6890-7. 2009
    ..e., (R)-15 and (S)-15) also inhibited PDE4D2 (i.e., K(i) values of 23 and 45 nM, respectively). Due to their synergistic functional activity, SNRI/PDE4 inhibitors may be effective in treating diseases such as depression...
  12. doi request reprint Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Bioorg Med Chem 17:337-43. 2009
    ..e., K(i) values of 106 and 253 nM, respectively). Due to the synergistic functional activity, PDE4 inhibitor/SSRIs may be effective in treating diseases such as depression...
  13. ncbi request reprint Role of flavin-containing monooxygenase in drug development
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Expert Opin Drug Metab Toxicol 4:1507-21. 2008
    ..However, I include discussion of these areas to stimulate further work and invite further discussion...
  14. pmc Immune defects in Alzheimer's disease: new medications development
    John R Cashman
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    BMC Neurosci 9:S13. 2008
    ..Bisdemethoxycurcumin appears to enhance immune function in mononuclear cells of AD patients and may provide a novel approach to AD immunotherapy...
  15. pmc Dual inhibitors of phosphodiesterase-4 and serotonin reuptake
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121, USA
    J Med Chem 52:1530-9. 2009
    ..On a molar basis, the antidepressant-like effect of the dual PDE4 inhibitor/SSRI 21 showed a 129-fold increase in in vivo efficacy compared to fluoxetine...
  16. ncbi request reprint Analysis of flavin-containing monooxygenase 3 genotype data in populations administered the anti-schizophrenia agent olanzapine
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Drug Metab Lett 2:100-14. 2008
    ..In female Asian American, allele frequency for FMO3 257 was significantly associated with diagnosis and in males, genotype frequency for FMO3 257 and diagnosis was significantly associated...
  17. pmc Inhibition of Bfl-1 with N-aryl maleimides
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, United States
    Bioorg Med Chem Lett 20:6560-4. 2010
    ..Inhibitors of Bfl-1 are potential development candidates for anti-cancer therapeutics...
  18. ncbi request reprint Dynamic medicinal chemistry in the elaboration of morphine-6-glucuronide analogs
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California, 92121
    Curr Top Med Chem 5:585-94. 2005
    ..Development of new pain medications for cancer and other diseases based on M6G could provide novel agents that could balance optimal analgesia with a decreased occurrence of adverse side effects...
  19. ncbi request reprint Effect of total parenteral nutrition and choline on hepatic flavin-containing and cytochrome P-450 monooxygenase activity in rats
    John R Cashman
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    Drug Metab Dispos 32:222-9. 2004
    ..The clinical relevance of these results is unknown but may be of significance for individuals receiving total parenteral nutrition and those afflicted with trimethylaminuria...
  20. ncbi request reprint Biochemical and clinical aspects of the human flavin-containing monooxygenase form 3 (FMO3) related to trimethylaminuria
    John R Cashman
    Human BioMolecular Research Institute, San Diego, CA, USA
    Curr Drug Metab 4:151-70. 2003
    ..The remarkable progress in the biochemical, genetic, clinical basis for understanding the trimethylaminuria condition is summarized and points to needs in the treatment of individuals suffering from trimethylaminuria...
  21. ncbi request reprint Interindividual differences of human flavin-containing monooxygenase 3: genetic polymorphisms and functional variation
    John R Cashman
    Human BioMolecular Research Institute, San Diego 92121, California
    Drug Metab Dispos 30:1043-52. 2002
    ..Human FMO3 may be another example of an environmental gene that participates in a protective mechanism to help humans ward off potentially toxic exposure of chemicals...
  22. ncbi request reprint The implications of polymorphisms in mammalian flavin-containing monooxygenases in drug discovery and development
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Drug Discov Today 9:574-81. 2004
    ..Examples of FMO allelic variation and splicing variants suggest that these genetic mutations could contribute to the interindividual and interethnic variability of FMO-mediated metabolism...
  23. ncbi request reprint The role of flavin-containing monooxygenases in drug metabolism and development
    John R Cashman
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92106, USA
    Curr Opin Drug Discov Devel 6:486-93. 2003
    ....
  24. ncbi request reprint Two new polymorphisms of the FMO3 gene in Caucasian and African-American populations: comparative genetic and functional studies
    Virginie Lattard
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Drug Metab Dispos 31:854-60. 2003
    ..Based on the functional activity of the variant FMO3 enzymes, it is likely that population differences exist for compounds primarily metabolized by FMO3...
  25. doi request reprint Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents
    Senait Ghirmai
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    J Med Chem 51:1913-24. 2008
    ..The ED 50 of inhibition of 10% ethanol self-administration in trained rats, using operant techniques for 11, was 0.5 mg/kg...
  26. ncbi request reprint Design, chemical synthesis, and biological evaluation of thiosaccharide analogues of morphine- and codeine-6-glucuronide
    James M MacDougall
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121 2804, USA
    J Med Chem 47:5809-15. 2004
    ..The in vivo antinociceptive activity of compound 5b was evaluated by the tail flick latency test, giving an ED50 of 2.5 mg/kg...
  27. pmc Novel variants of the human flavin-containing monooxygenase 3 (FMO3) gene associated with trimethylaminuria
    Meike S Motika
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Mol Genet Metab 97:128-35. 2009
    ..In another study, genotyping analysis of a 17 year old female revealed a mutation that caused a frame shift after K415 and resulted in a protein variant with only 486 amino acid residues that was associated with severe TMAu...
  28. pmc Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell-derived mesoderm
    Erik Willems
    Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Circ Res 109:360-4. 2011
    ..Although the initiating step of mesoderm formation is well characterized, the subsequent steps that promote for cardiac lineages are poorly understood and limit the yield of cardiomyocytes...
  29. pmc Design and synthesis of selective inhibitors of placental alkaline phosphatase
    Marion Lanier
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121 2804, USA
    Bioorg Med Chem 18:573-9. 2010
    ..These selective PLAP inhibitors will provide small molecule probes for the study of the pathophysiological role of PLAP...
  30. ncbi request reprint Functional activity of the mouse flavin-containing monooxygenase forms 1, 3, and 5
    Jun Zhang
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    J Biochem Mol Toxicol 21:206-15. 2007
    ..The results revealed unique features for mFMO5, suggesting possible impact on the functional significance of this abundantly expressed FMO5 isoform in both human and mouse liver...
  31. ncbi request reprint Synthesis and biological evaluation of some 6-arylamidomorphines as analogues of morphine-6-glucuronide
    James M MacDougall
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121 2804, USA
    Bioorg Med Chem 12:5983-90. 2004
    ..2-0.6 nM). Functional assays showed that compounds 10a-h acted as full mu opioid receptor agonists. The ED(50) of compound 10e.HCl as an analgesic was 12.6 mg/kg in the tail flick latency test in the rat...
  32. doi request reprint Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activation pathway
    Karl J Okolotowicz
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Bioorg Med Chem 18:1918-24. 2010
    ..A library of analogs was synthesized and the structure-activity relationship and metabolic stability for the series is presented...
  33. ncbi request reprint Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide
    James M MacDougall
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121 2804, USA
    Bioorg Med Chem Lett 15:1583-6. 2005
    ..Compound 3 was also very stable at pH 2 and pH 7.4, suggesting that 3 possessed properties for sustained duration of action...
  34. ncbi request reprint Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors
    John L Stebbins
    Infectious and Inflammatory Disease Center, Burnham Institute for Medical Research, and University of California at San Diego, Division of Biological Sciences, 9500 Gilman Drive, La Jolla, California 92093, USA
    J Med Chem 50:6607-17. 2007
    ..Compared to FK506, the fragment-based FKBP12 inhibitors developed herein possess significant advantages as drug candidates...
  35. ncbi request reprint Inhibition of human liver microsomal (S)-nicotine oxidation by (-)-menthol and analogues
    James M MacDougall
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92126, USA
    Chem Res Toxicol 16:988-93. 2003
    ..This may be another example of self-medication to obtain the desired effect of nicotine...
  36. ncbi request reprint Deleterious mutations in the flavin-containing monooxygenase 3 (FMO3) gene causing trimethylaminuria
    Jun Zhang
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Pharmacogenetics 13:495-500. 2003
    ..The two deleterious mutations reported herein were rare mutations with estimated allelic frequencies of less than 1%...
  37. ncbi request reprint 5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6
    Travis T Denton
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121, USA
    J Med Chem 48:224-39. 2005
    ..We also found a number of compounds to be highly selective for the inhibition of human CYP2A6 versus the other human CYPs examined...
  38. ncbi request reprint Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization
    Jason K Yano
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121, USA
    J Med Chem 49:6987-7001. 2006
    ..The results suggest that inhibitors that compliment the active site features of CYP2A6 can exhibit significant selectivity for CYP2A6 relative to other human liver drug-metabolizing P450s...
  39. pmc Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation
    Senait Ghirmai
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Bioorg Med Chem 17:6671-81. 2009
    ..The inhibition of ethanol self-administration in rats trained to self-administer a 10% (w/v) ethanol solution, utilizing operant techniques showed 5-8 to have very potent efficacy (ED(50) values 19-50 microg/kg)...
  40. pmc A chemical biology approach to myocardial regeneration
    Erik Willems
    Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    J Cardiovasc Transl Res 4:340-50. 2011
    ....
  41. pmc Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells
    Erik Willems
    Muscle Development and Regeneration Program, Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Cell Stem Cell 11:242-52. 2012
    ..ITD-1 is a highly selective TGF-β inhibitor and reveals an unexpected role for TGF-β signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors...
  42. ncbi request reprint Nicotine-related alkaloids and metabolites as inhibitors of human cytochrome P-450 2A6
    Travis T Denton
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Biochem Pharmacol 67:751-6. 2004
    ..Our results indicate that the prominent nicotine-related alkaloid beta-nicotyrine present after smoking potently inhibits human CYP2A6...
  43. doi request reprint 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors
    Troy Voelker
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    Bioorg Med Chem 17:2047-68. 2009
    ..Acute administration of 32c (10mg/kg), or 32d (10mg/kg) ip tended to decrease the duration of mouse immobility in the FST although the effect was not statistically significant...
  44. ncbi request reprint Bivalent biogenic amine reuptake inhibitors
    Keith Fandrick
    Human BioMolecular Research Institute, 5310 Eastgate Mall, 92121, San Diego, CA, USA
    Bioorg Med Chem Lett 13:2151-4. 2003
    ..The bivalent ligand 4, comprised of linking an aryltropane by an octamethylene spacer showed high efficacy for the human dopamine transporter and had a discrimination ratio of 130...
  45. pmc Hepatic flavin-containing monooxygenase gene regulation in different mouse inflammation models
    Jun Zhang
    Human BioMolecular Research Institute, San Diego, California, USA
    Drug Metab Dispos 37:462-8. 2009
    ..Unlike cytochrome P450 regulation measured in the same mouse strains, Fmo3 expression was largely refractory to down-regulation in the DSS model of inflammatory colitis...
  46. pmc HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter
    Alice Kiselyuk
    Department of Bioengineering, University of California, San Diego, La Jolla, CA 92093, USA
    Chem Biol 19:806-18. 2012
    ..The discovery of bioactive modulators for HNF4α raises the possibility that diseases involving HNF4α, such as diabetes and cancer, might be amenable to pharmacologic intervention by modulation of HNF4α activity...
  47. pmc Chemical biology strategy reveals pathway-selective inhibitor of NF-kappaB activation induced by protein kinase C
    Ranxin Shi
    Sanford Burnham Medical Research Institute, La Jolla, San Diego, California 92037, USA
    ACS Chem Biol 5:287-99. 2010
    ..Altogether, as a selective chemical inhibitor of the NF-kappaB pathway induced by PKC, CID-2858522 serves as a powerful research tool and may reveal new paths toward therapeutically useful NF-kappaB inhibitors...
  48. ncbi request reprint Human and plant flavin-containing monooxygenase N-oxygenation of amines: detoxication vs. bioactivation
    John R Cashman
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    Drug Metab Rev 34:513-21. 2002
    ..However, study of the Arabidopsis FMO-like enzyme may provide considerable insight into the possible role of mammalian FMOs in biogenic amine metabolism...
  49. ncbi request reprint Investigation of structure and function of a catalytically efficient variant of the human flavin-containing monooxygenase form 3
    Tímea Borbás
    Human BioMolecular Research Institute, San Diego, CA 92121, USA
    Drug Metab Dispos 34:1995-2002. 2006
    ..A molecular model of human FMO3 was also constructed to help explain the results. The increase in catalytic efficiency observed for Pro360 in human FMO3 was also observed when the His of FMO1 was replaced by Pro at loci 360...
  50. ncbi request reprint Syntheses of 3-carbomethoxy-4-(aryl)piperidines and in vitro and in vivo pharmacological evaluation: identification of inhibitors of the human dopamine transporter
    Xianqi Feng
    Human BioMolecular Research Institute, 5310 Eastgate Mall, CA 92121, San Diego, USA
    Bioorg Med Chem 11:775-80. 2003
    ..The conclusion is that substantial portions of the cocaine structure can be dissected away to provide compounds with significant binding and reuptake inhibition of the human dopamine transporter...
  51. ncbi request reprint Flavin-containing monooxygenase 3 and human disease
    Meike S Motika
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA
    Expert Opin Drug Metab Toxicol 3:831-45. 2007
    ....
  52. pmc Chemical synthesis of two series of nerve agent model compounds and their stereoselective interaction with human acetylcholinesterase and human butyrylcholinesterase
    Nora H Barakat
    Human BioMolecular Research Institute, San Diego, California 92121, USA
    Chem Res Toxicol 22:1669-79. 2009
    ..The potential of and limitations for using these model compounds in the development of biological therapeutics against nerve agent toxicity are also discussed...
  53. ncbi request reprint Alternative processing events in human FMO genes
    Virginie Lattard
    Human BioMolecular Research Institute, San Diego, California, USA
    Mol Pharmacol 65:1517-25. 2004
    ..It is not clear whether these FMO splice variants can oxygenate other substrates, including those that remain to be discovered...
  54. pmc Direct detection of the hydrolysis of nerve agent model compounds using a fluorescent probe
    Xueying Zheng
    Human BioMolecular Research Institute, San Diego, CA 92121, United States
    Chem Biol Interact 187:330-4. 2010
    ....
  55. pmc Nerve agent analogues that produce authentic soman, sarin, tabun, and cyclohexyl methylphosphonate-modified human butyrylcholinesterase
    Cynthia Gilley
    Human BioMolecular Research Institute, San Diego, California 92121, USA
    Chem Res Toxicol 22:1680-8. 2009
    ..However, the soman and sarin thiomethyl compounds yielded two types of adducts, one of which was thiomethyl phosphonate, a modification not found after treatment with authentic soman and sarin...
  56. ncbi request reprint Stop codon mutations in the flavin-containing monooxygenase 3 (FMO3) gene responsible for trimethylaminuria in a Japanese population
    Hiroshi Yamazaki
    Laboratory of Drug Metabolism and Pharmacokinetics, Showa Pharmaceutical University, Machida, Tokyo 194 8543, Japan
    Mol Genet Metab 90:58-63. 2007
    ..The results suggest that individuals homozygous for either of the nonsense mutations, Arg500Stop and/or Cys197Stop alleles, in the FMO3 gene can possess abnormal TMA N-oxygenation...
  57. ncbi request reprint Effect of genetic variants of the human flavin-containing monooxygenase 3 on N- and S-oxygenation activities
    Makiko Shimizu
    Showa Pharmaceutical University, 3 3165 Higashi tamagawa Gakuen, Machida, Tokyo 194 8543, Japan
    Drug Metab Dispos 35:328-30. 2007
    ..Genetic polymorphism in the human FMO3 gene might lead to unexpected changes of catalytic efficiency for N- and S-oxygenation of xenobiotics and endogenous materials...
  58. ncbi request reprint Effects of the dietary supplements, activated charcoal and copper chlorophyllin, on urinary excretion of trimethylamine in Japanese trimethylaminuria patients
    Hiroshi Yamazaki
    Laboratory of Drug Metabolism, Graduate School of Pharmaceutical Sciences, Hokkaido University, N12W6, Kita ku, Sapporo 060 0812, Japan
    Life Sci 74:2739-47. 2004
    ..several weeks) than those observed for activated charcoal. The results suggest that the daily intake of charcoal and/or copper chlorophyllin may be of significant use in improving the quality of life of individuals suffering from TMAU...
  59. ncbi request reprint Mild trimethylaminuria observed in a Japanese cohort with liver damage
    Hiroshi Yamazaki
    Am J Med 118:803-5. 2005
  60. pmc Curcuminoids inhibit multiple human cytochromes P450, UDP-glucuronosyltransferase, and sulfotransferase enzymes, whereas piperine is a relatively selective CYP3A4 inhibitor
    Laurie P Volak
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    Drug Metab Dispos 36:1594-605. 2008
    ..Based on these data and expected tissue concentrations of inhibitors, we predict that a p.o. administered curcuminoid/piperine combination is most likely to inhibit CYP3A, CYP2C9, UGT, and SULT metabolism within the intestinal mucosa...
  61. ncbi request reprint Genetic and environmental influences on therapeutic and toxicity outcomes: studies with CYP2A6
    Soisungwan Satarug
    National Research Centre for Environmental Toxicology, The University of Queensland, Brisbane, Queensland, Australia
    Curr Clin Pharmacol 1:291-309. 2006
    ..The results indicate that the phenotype of CYP2A6 enzyme in liver is an outcome of interactions between the CYP2A6 gene, cadmium, nicotine and possibly its metabolites...

Research Grants15

  1. Biosensor for real-time chemical monitoring
    John Cashman; Fiscal Year: 2007
    ..The final sensitive and selective product will be of use in a rapid screening format of physiological fluids for OP exposure. ..
  2. New Opioids for Alcoholism
    John Cashman; Fiscal Year: 2006
    ..The potential commercial application of the work is that the research could lead to a 'blockbuster' drug product. ..
  3. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2005
    ..Such fundamental information will be useful in the development of safer drugs, the prevention of adverse drug reactions and the protection of humans from disease. ..
  4. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2004
    ..Such fundamental information will be useful in the development of safer drugs, the prevention of adverse drug reactions and the protection of humans from disease. ..
  5. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2003
    ..Such fundamental information will be useful in the development of safer drugs, the prevention of adverse drug reactions and the protection of humans from disease. ..
  6. Amine N-Oxygenation by FMO3 and FMO4
    John Cashman; Fiscal Year: 2002
    ..Such fundamental information will be useful in the development of safer drugs, the prevention of adverse drug reactions and the protection of humans from disease. ..
  7. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2001
    ..The study will provide an understanding of the structural and pharmaceutical properties of hDAT antagonists. The work will lead to new insight into the preparation of human medications necessary in the cessation of cocaine abuse. ..
  8. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2000
    ..The study will provide an understanding of the structural and pharmaceutical properties of hDAT antagonists. The work will lead to new insight into the preparation of human medications necessary in the cessation of cocaine abuse. ..
  9. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2000
    ..The study will provide an understanding of the structural and pharmaceutical properties of hDAT antagonists. The work will lead to new insight into the preparation of human medications necessary in the cessation of cocaine abuse. ..
  10. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2000
    ..The study will provide an understanding of the structural and pharmaceutical properties of hDAT antagonists. The work will lead to new insight into the preparation of human medications necessary in the cessation of cocaine abuse. ..
  11. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 1999
    ..The study will provide an understanding of the structural and pharmaceutical properties of hDAT antagonists. The work will lead to new insight into the preparation of human medications necessary in the cessation of cocaine abuse. ..
  12. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 1999
    ..The study will provide an understanding of the structural and pharmaceutical properties of hDAT antagonists. The work will lead to new insight into the preparation of human medications necessary in the cessation of cocaine abuse. ..