Experts and Doctors on enzyme inhibitors in United States

Summary

Locale: United States
Topic: enzyme inhibitors

Top Publications

  1. O Brien W, Xu G, Batta A, Tint G, Salen G, Dyer C, et al. Developmental sensitivity of associative learning to cholesterol synthesis inhibitors. Behav Brain Res. 2002;129:141-52 pubmed
    ..Thus, there is a developmental sensitivity to cholesterol synthesis blocking agents both in terms of their effects on brain sterols and new motor learning. ..
  2. Berti Mattera L, Wilkins P, Harwalkar S, Madhun Z, Almhanna K, Mattera R. Endothelins regulate arachidonic acid release and mitogen-activated protein kinase activity in Schwann cells. J Neurochem. 2000;75:2316-26 pubmed
    ..Regulation of these effectors may mediate the control of proliferation and differentiation of SC by ETs during peripheral nerve development and regeneration. ..
  3. Ahmad Z, Senior A. Mutagenesis of residue betaArg-246 in the phosphate-binding subdomain of catalytic sites of Escherichia coli F1-ATPase. J Biol Chem. 2004;279:31505-13 pubmed
    ..Phosphate protected against NBD-Cl inhibition in wild type but not in mutants. The results show that phosphate can bind in the betaE catalytic site of E. coli F(1) and that betaArg-246 is an important phosphate-binding residue. ..
  4. Klees R, Salasznyk R, Kingsley K, Williams W, Boskey A, Plopper G. Laminin-5 induces osteogenic gene expression in human mesenchymal stem cells through an ERK-dependent pathway. Mol Biol Cell. 2005;16:881-90 pubmed
    ..Addition of the ERK inhibitor PD98059 mitigates these effects. We conclude that contact with laminin-5 is sufficient to activate ERK and to stimulate osteogenic differentiation in hMSC. ..
  5. Aromolaran A, Zima A, Blatter L. Role of glycolytically generated ATP for CaMKII-mediated regulation of intracellular Ca2+ signaling in bovine vascular endothelial cells. Am J Physiol Cell Physiol. 2007;293:C106-18 pubmed
    ..In conclusion, CaMKII exerts a profound inhibition of ER Ca(2+) release in CPAE cells, which is mediated by glycolytically generated ATP, possibly through ATP-dependent phosphorylation of the IP(3)R...
  6. Radek K, Kovacs E, Gallo R, DiPietro L. Acute ethanol exposure disrupts VEGF receptor cell signaling in endothelial cells. Am J Physiol Heart Circ Physiol. 2008;295:H174-84 pubmed publisher
    ..Together, the data establish that acute ethanol exposure significantly impairs angiogenesis and suggest that this effect is mediated by changes in endothelial cell responsiveness to both VEGF and hypoxia...
  7. Salvador L, Taori K, Biggs J, Jakoncic J, Ostrov D, Paul V, et al. Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells. J Med Chem. 2013;56:1276-90 pubmed publisher
    ..Compound 1 exhibited activity comparable to the clinically approved elastase inhibitor sivelestat in short-term assays and demonstrated superior sustained activity in longer-term assays. ..
  8. Witherspoon M, Chen Q, Kopelovich L, Gross S, Lipkin S. Unbiased metabolite profiling indicates that a diminished thymidine pool is the underlying mechanism of colon cancer chemoprevention by alpha-difluoromethylornithine. Cancer Discov. 2013;3:1072-81 pubmed publisher
    ..This study identifies the fi rst shared mechanism for colorectal cancer chemoprevention and chemotherapy, suggesting a common metabolic target for both premalignant and malignant colon cells. ..
  9. Gulick A, Starai V, Horswill A, Homick K, Escalante Semerena J. The 1.75 A crystal structure of acetyl-CoA synthetase bound to adenosine-5'-propylphosphate and coenzyme A. Biochemistry. 2003;42:2866-73 pubmed publisher
    ..Additionally, we provide a structural explanation for the recently shown control of enzyme activity by acetylation of an active site lysine...

More Information

Publications182 found, 100 shown here

  1. Lodise T, Lomaestro B, Rodvold K, Danziger L, Drusano G. Pharmacodynamic profiling of piperacillin in the presence of tazobactam in patients through the use of population pharmacokinetic models and Monte Carlo simulation. Antimicrob Agents Chemother. 2004;48:4718-24 pubmed
    ..This study indicates that piperacillin-tazobactam should have utility for empirical therapy of hospital-onset infections. ..
  2. TURNER J, Thomas A, Reeves J, Hantash B. Calcineurin activation by slow calcium release from intracellular stores suppresses protein kinase C regulation of L-type calcium channels in L6 cells. Cell Calcium. 2009;46:242-7 pubmed publisher
    ..This study is the first to demonstrate that the regulation of L-type Ca(2+) channels in a myocyte model involves a balance between the differential Ca(2+) sensitivities and opposing actions of PKC and calcineurin. ..
  3. Kesanakurti D, Chetty C, Bhoopathi P, Lakka S, Gorantla B, Tsung A, et al. Suppression of MMP-2 attenuates TNF-? induced NF-?B activation and leads to JNK mediated cell death in glioma. PLoS ONE. 2011;6:e19341 pubmed publisher
    ..In summary, our study implies a role of MMP-2 in the regulation of TNF-? mediated constitutive NF-?B activation and Fas-mediated JNK mediated apoptosis in glioma xenograft cells in vitro and in vivo. ..
  4. Zhang Y, Yang F, Kao Y, Kurilla M, Pompliano D, Dicker I. Homogenous assays for Escherichia coli DnaB-stimulated DnaG primase and DnaB helicase and their use in screening for chemical inhibitors. Anal Biochem. 2002;304:174-9 pubmed
    ..By this approach, specific primase inhibitors could be identified. ..
  5. Atkins C, Nozaki N, Shigeri Y, Soderling T. Cytoplasmic polyadenylation element binding protein-dependent protein synthesis is regulated by calcium/calmodulin-dependent protein kinase II. J Neurosci. 2004;24:5193-201 pubmed
    ..These results demonstrate that CPEB phosphorylation and translation are regulated by CaMKII activity and provide a possible mechanism for how dendritic protein synthesis in the hippocampus may be stimulated during synaptic plasticity. ..
  6. Pannu R, Won J, Khan M, Singh A, Singh I. A novel role of lactosylceramide in the regulation of lipopolysaccharide/interferon-gamma-mediated inducible nitric oxide synthase gene expression: implications for neuroinflammatory diseases. J Neurosci. 2004;24:5942-54 pubmed
    ..To our knowledge this is the first report of a role of LacCer in iNOS expression and the advantage of GSL depletion in attenuating post-SCI inflammation to improve the outcome of SCI. ..
  7. Samarakoon R, Higgins C, Higgins S, Kutz S, Higgins P. Plasminogen activator inhibitor type-1 gene expression and induced migration in TGF-beta1-stimulated smooth muscle cells is pp60(c-src)/MEK-dependent. J Cell Physiol. 2005;204:236-46 pubmed
    ..g., PAI-1], increased cell motility) are linked in the R22 vascular smooth muscle cell system, require pp60(c-src) kinase activity and MEK signaling and involve activation of an AG1478-sensitive (likely EGFR-dependent) pathway. ..
  8. Neviani P, Santhanam R, Trotta R, Notari M, Blaser B, Liu S, et al. The tumor suppressor PP2A is functionally inactivated in blast crisis CML through the inhibitory activity of the BCR/ABL-regulated SET protein. Cancer Cell. 2005;8:355-68 pubmed
    ..Thus, functional inactivation of PP2A is essential for BCR/ABL leukemogenesis and, perhaps, required for blastic transformation...
  9. Karmakar S, Banik N, Patel S, Ray S. Garlic compounds induced calpain and intrinsic caspase cascade for apoptosis in human malignant neuroblastoma SH-SY5Y cells. Apoptosis. 2007;12:671-84 pubmed
    ..Results strongly suggested that the garlic compounds DAS and DADS suppressed anti-apoptotic factors and activated calpain and intrinsic caspase cascade for apoptosis in SH-SY5Y cells. ..
  10. Trueblood K, Mohr S, Dubyak G. Purinergic regulation of high-glucose-induced caspase-1 activation in the rat retinal Müller cell line rMC-1. Am J Physiol Cell Physiol. 2011;301:C1213-23 pubmed publisher
  11. Zheng J, Wen Y, Song Y, Wang K, Chen D, Magness R. Activation of multiple signaling pathways is critical for fibroblast growth factor 2- and vascular endothelial growth factor-stimulated ovine fetoplacental endothelial cell proliferation. Biol Reprod. 2008;78:143-50 pubmed
  12. Zhang Z, Kelemen O, van Santen M, Yelton S, Wendlandt A, Sviripa V, et al. Synthesis and characterization of pseudocantharidins, novel phosphatase modulators that promote the inclusion of exon 7 into the SMN (survival of motoneuron) pre-mRNA. J Biol Chem. 2011;286:10126-36 pubmed publisher
    ..Our data show that subtle changes in similar compounds can turn a phosphatase inhibitor into an activator. These chemically related compounds influence alternative splicing by distinct mechanisms. ..
  13. Cao H, Hall J, Hille R. X-ray crystal structure of arsenite-inhibited xanthine oxidase: ?-sulfido,?-oxo double bridge between molybdenum and arsenic in the active site. J Am Chem Soc. 2011;133:12414-7 pubmed publisher
    ..The doubly bridged binding mode is in agreement with previous XAS data indicating that the catalytically essential sulfur is also essential for the high affinity of reduced xanthine oxidoreductase for arsenite...
  14. Zhang X, Gao M, Ha T, Kalbfleisch J, Williams D, Li C, et al. The toll-like receptor 9 agonist, CpG-oligodeoxynucleotide 1826, ameliorates cardiac dysfunction after trauma-hemorrhage. Shock. 2012;38:146-52 pubmed publisher
    ..The mechanisms involve activation of both PI3K/Akt and ERK signaling pathways. The TLR9 agonist, CpG-ODN 1826, may provide a novel treatment strategy for preventing or managing cardiac dysfunction and enhancing recovery in T-H patients. ..
  15. Borsch Haubold A, Bartoli F, Asselin J, Dudler T, Kramer R, Apitz Castro R, et al. Identification of the phosphorylation sites of cytosolic phospholipase A2 in agonist-stimulated human platelets and HeLa cells. J Biol Chem. 1998;273:4449-58 pubmed
  16. Sutters M, Yamaguchi T, Maser R, Magenheimer B, St John P, Abrahamson D, et al. Polycystin-1 transforms the cAMP growth-responsive phenotype of M-1 cells. Kidney Int. 2001;60:484-94 pubmed
    ..Expression of the polycystin-1 C-terminal tail disrupts normal cellular signaling and transforms the stably transfected M-1 cells to an abnormal PKD cell proliferation phenotype. ..
  17. Eckel Mahan K, Phan T, Han S, Wang H, Chan G, Scheiner Z, et al. Circadian oscillation of hippocampal MAPK activity and cAmp: implications for memory persistence. Nat Neurosci. 2008;11:1074-82 pubmed
    ..These data suggest that the persistence of long-term memories may depend on reactivation of the cAMP/MAPK/CREB transcriptional pathway in the hippocampus during the circadian cycle. ..
  18. Wang Y, Hu L, Yao R, Wang M, Crist K, Grubbs C, et al. Altered gene expression profile in chemically induced rat mammary adenocarcinomas and its modulation by an aromatase inhibitor. Oncogene. 2001;20:7710-21 pubmed
    ..In addition, the identified genes may become useful targets for drug development and potential biomarkers for monitoring treatment and prevention of breast cancer in humans. ..
  19. Eisenach J, Clark E, Charkoudian N, Dinenno F, Atkinson J, Fealey R, et al. Effects of chronic sympathectomy on vascular function in the human forearm. J Appl Physiol (1985). 2002;92:2019-25 pubmed
    ..The normal vasoconstrictor responses to tyramine indicate that there were viable sympathetic nerves in the forearm that were not engaged by LBNP. ..
  20. Sasser J, Ni X, Humphreys M, Baylis C. Increased renal phosphodiesterase-5 activity mediates the blunted natriuretic response to a nitric oxide donor in the pregnant rat. Am J Physiol Renal Physiol. 2010;299:F810-4 pubmed publisher
    ..Therefore, increased intrarenal PDE5 mediates the blunted natriuretic response to NO, and loss of responsiveness to the cGMP-dependent, natriuretic agents may contribute to volume expansion during pregnancy. ..
  21. Zhang B, Li S, Harbrecht B. Akt-mediated signaling is induced by cytokines and cyclic adenosine monophosphate and suppresses hepatocyte inducible nitric oxide synthase expression independent of MAPK P44/42. Biochim Biophys Acta. 2011;1813:73-9 pubmed publisher
    ..These data demonstrate that dbcAMP regulates hepatocyte iNOS expression through an Akt-mediated signaling mechanism that is independent of MAPK P44/42. ..
  22. Sakakima H, Khan M, Dhammu T, Shunmugavel A, Yoshida Y, Singh I, et al. Stimulation of functional recovery via the mechanisms of neurorepair by S-nitrosoglutathione and motor exercise in a rat model of transient cerebral ischemia and reperfusion. Restor Neurol Neurosci. 2012;30:383-96 pubmed publisher
    ..A combination of exercise and GSNO shows greater functional recovery. Improved recovery with GSNO, even administered 24 hours post-IR, demonstrates its clinical relevance. ..
  23. Smith V, Matthews C. Testing the role of chain connectivity on the stability and structure of dihydrofolate reductase from E. coli: fragment complementation and circular permutation reveal stable, alternatively folded forms. Protein Sci. 2001;10:116-28 pubmed
    ..These results show that changes in the backbone connectivity can produce alternatively folded forms and highlight the importance of protein-ligand interactions in stabilizing the active site architecture of DHFR. ..
  24. Xue C, Voss M, Nelson D, Duan J, Cherney R, Jacobson I, et al. Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. J Med Chem. 2001;44:2636-60 pubmed
    ..2 nM in the porcine TACE assay, and are broad-spectrum MMP inhibitors. Pharmacokinetic studies in beagle dogs revealed that SL422 and SP057 are orally bioavailable, with oral bioavailabilities of 11% and 23%, respectively. ..
  25. Yamamoto S, Yang G, Zablocki D, Liu J, Hong C, Kim S, et al. Activation of Mst1 causes dilated cardiomyopathy by stimulating apoptosis without compensatory ventricular myocyte hypertrophy. J Clin Invest. 2003;111:1463-74 pubmed
    ..These results show that Mst1 works as both an essential initiator of apoptosis and an inhibitor of hypertrophy in cardiac myocytes, resulting in a previously unrecognized form of cardiomyopathy. ..
  26. Padayatti P, Sheri A, Totir M, Helfand M, Carey M, Anderson V, et al. Rational design of a beta-lactamase inhibitor achieved via stabilization of the trans-enamine intermediate: 1.28 A crystal structure of wt SHV-1 complex with a penam sulfone. J Am Chem Soc. 2006;128:13235-42 pubmed
    ..Stabilizing the trans-enamine intermediate represents a novel strategy for the rational design of mechanism-based class A beta-lactamase inhibitors. ..
  27. Erickson D, Hollfelder S, Tenge J, Gohdes M, Burkhardt J, Krieter P. In vitro metabolism of the analgesic bicifadine in the mouse, rat, monkey, and human. Drug Metab Dispos. 2007;35:2232-41 pubmed
    ..Overall, the data indicate that the primary enzymes responsible for the primary metabolism of bicifadine in humans are MAO-B and CYP2D6...
  28. Shi Y, Rehman H, Wright G, Zhong Z. Inhibition of inducible nitric oxide synthase prevents graft injury after transplantation of livers from rats after cardiac death. Liver Transpl. 2010;16:1267-77 pubmed publisher
    ..Inhibitors of iNOS are suggested as effective therapies to improve the outcome after transplantation of GCDD. ..
  29. Laclau M, Lu F, MacDonald M. Enzymes in pancreatic islets that use NADP(H) as a cofactor including evidence for a plasma membrane aldehyde reductase. Mol Cell Biochem. 2001;225:151-60 pubmed
    ..Reductases may be present in cytosol to protect the insulin cell from molecules that cause oxidative injury. ..
  30. Bankers Fulbright J, Kita H, Gleich G, O Grady S. Regulation of human eosinophil NADPH oxidase activity: a central role for PKCdelta. J Cell Physiol. 2001;189:306-15 pubmed
    ..Our results indicate that the G-protein-coupled LTB4 receptor and the IL-5 cytokine receptor converge on a common signaling pathway involving PI 3-kinase and PKCdelta to regulate NADPH oxidase activity in human eosinophils. ..
  31. Tran T, Uhl M, Ma J, Janssen L, Sriram V, Aulwurm S, et al. Inhibiting TGF-beta signaling restores immune surveillance in the SMA-560 glioma model. Neuro Oncol. 2007;9:259-70 pubmed
    ..Together, these results suggest that treatment with a TGF-betaRI inhibitor may be useful in the treatment of glioblastoma. ..
  32. Metzler W, Yanchunas J, Weigelt C, Kish K, Klei H, Xie D, et al. Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci. 2008;17:240-50 pubmed publisher
    ..Together with the previously published enzymatic data, the structural and binding data presented here strongly support a histidine-assisted covalent bond formation between S630 hydroxyl oxygen and the nitrile group of saxagliptin. ..
  33. Grassian A, Parker S, Davidson S, Divakaruni A, Green C, Zhang X, et al. IDH1 mutations alter citric acid cycle metabolism and increase dependence on oxidative mitochondrial metabolism. Cancer Res. 2014;74:3317-31 pubmed publisher
    ..Lastly, IDH1-mutant cells also grew poorly as subcutaneous xenografts within a hypoxic in vivo microenvironment. Together, our results suggest therapeutic opportunities to exploit the metabolic vulnerabilities specific to IDH1 mutation. ..
  34. Beebe S, White J, Blackmore P, Deng Y, Somers K, Schoenbach K. Diverse effects of nanosecond pulsed electric fields on cells and tissues. DNA Cell Biol. 2003;22:785-96 pubmed
    ..Potential applications for nsPEF include inducing apoptosis in cells and tumors, probing signal transduction mechanisms that determine cell fate, and enhancing gene expression...
  35. Lee K, Kang N, Rogozin E, Kim H, Cho Y, Bode A, et al. Myricetin is a novel natural inhibitor of neoplastic cell transformation and MEK1. Carcinogenesis. 2007;28:1918-27 pubmed
    ..Overall, these results indicated that myricetin has potent anticancer-promoting activity and mainly targets MEK signaling, which may contribute to the chemopreventive potential of several foods including red wines...
  36. McNally A, Macewan S, Anderson J. Foreign body-type multinucleated giant cell formation requires protein kinase C beta, delta, and zeta. Exp Mol Pathol. 2008;84:37-45 pubmed
    ..However, new evidence is provided that FBGC formation is supported by PKCbeta, PKCdelta, and PKCzeta in combined diacylglycerol-dependent (PKCbeta and PKCdelta) and -independent (PKCzeta) signaling pathways...
  37. Liles M, Williamson L, Rodbumrer J, Torsvik V, Goodman R, Handelsman J. Recovery, purification, and cloning of high-molecular-weight DNA from soil microorganisms. Appl Environ Microbiol. 2008;74:3302-5 pubmed publisher
    ..Nucleases that copurified with the metagenomic DNA were removed by incubating plugs with a high-salt and -formamide solution. This method was used to construct large-insert soil metagenomic libraries...
  38. Patterson M, Vecchio D, Jacklin E, Abel L, Chadha Boreham H, Luzy C, et al. Long-term miglustat therapy in children with Niemann-Pick disease type C. J Child Neurol. 2010;25:300-5 pubmed publisher
    ..Miglustat stabilized neurological disease progression in pediatric patients with Niemann-Pick disease type C, with comparable safety and tolerability to that observed in adults and juveniles...
  39. Sarkaria J, Tibbetts R, Busby E, Kennedy A, Hill D, Abraham R. Inhibition of phosphoinositide 3-kinase related kinases by the radiosensitizing agent wortmannin. Cancer Res. 1998;58:4375-82 pubmed
    ..These results identify wortmannin as an inhibitor of ATM activity and suggest that ATM and DNA-PK are relevant targets for the radiosensitizing effect of this drug in cancer cells. ..
  40. Coon S, Sundaram U. Unique regulation of anion/HCO3- exchangers by constitutive nitric oxide in rabbit small intestine. Am J Physiol Gastrointest Liver Physiol. 2003;285:G1084-90 pubmed
    ..These results indicate that cNO uniquely regulates the three BBM anion/HCO3- transporters in the rabbit small intestine. ..
  41. Lang H, Schulte B, Schmiedt R. Ouabain induces apoptotic cell death in type I spiral ganglion neurons, but not type II neurons. J Assoc Res Otolaryngol. 2005;6:63-74 pubmed
    ..It is speculated that the high levels of calcineurin and NF-kappaB in type II SGNs, as compared with type I SGNs, may play protective roles in enhancing the survival of type II neurons exposed to ouabain. ..
  42. Lothrop A, Ruggles E, Hondal R. No selenium required: reactions catalyzed by mammalian thioredoxin reductase that are independent of a selenocysteine residue. Biochemistry. 2009;48:6213-23 pubmed publisher
    ..7 in the full-length mammalian enzyme (83-142 nM), but surprisingly the truncated enzyme showed much stronger inhibition (25 nM). This contrasts with auranofin, where the absence of Sec more strongly perturbed inhibition...
  43. Bush K, Fisher J. Epidemiological expansion, structural studies, and clinical challenges of new ?-lactamases from gram-negative bacteria. Annu Rev Microbiol. 2011;65:455-78 pubmed publisher
    ..Combination therapy will likely be required to counteract the continuing evolution of these insidious enzymes in multidrug-resistant pathogens. ..
  44. La Favor J, Anderson E, Dawkins J, Hickner R, Wingard C. Exercise prevents Western diet-associated erectile dysfunction and coronary artery endothelial dysfunction: response to acute apocynin and sepiapterin treatment. Am J Physiol Regul Integr Comp Physiol. 2013;305:R423-34 pubmed publisher
    ..Furthermore, exercise training may be a practical means of preventing diet-induced ED and CAD development. ..
  45. Finney J, Moon H, Ronnebaum T, Lantz M, Mure M. Human copper-dependent amine oxidases. Arch Biochem Biophys. 2014;546:19-32 pubmed publisher
    ..Consequently, there is a critical need to understand the functions of these proteins at the molecular level, so that strategies targeting these enzymes can be developed to combat human diseases. ..
  46. Huang C, Bode A, Chen N, Ma W, Li J, Nomura M, et al. Transactivation of AP-1 in AP-1-luciferase reporter transgenic mice by arsenite and arsenate. Anticancer Res. 2001;21:261-7 pubmed
    ..Furthermore, both arsenite and arsenate could induce transactivation of AP-1 in AP-1-luciferase reporter transgenic mice. ..
  47. Margolis P, Hackbarth C, Lopez S, Maniar M, Wang W, Yuan Z, et al. Resistance of Streptococcus pneumoniae to deformylase inhibitors is due to mutations in defB. Antimicrob Agents Chemother. 2001;45:2432-5 pubmed
    ..pneumoniae ATCC 49619 harbor mutations in defB but not in fmt. Reintroduction of the mutated defB gene into wild-type S. pneumoniae R6x recreates the resistance phenotype. The altered enzyme displays decreased sensitivity to actinonin...
  48. O Grady M, Raha D, Hanson B, Bunting M, Hanson G. Combining RNA interference and kinase inhibitors against cell signalling components involved in cancer. BMC Cancer. 2005;5:125 pubmed
  49. Kunos C, Radivoyevitch T, Abdul Karim F, Fanning J, Abulafia O, Bonebrake A, et al. Ribonucleotide reductase inhibition restores platinum-sensitivity in platinum-resistant ovarian cancer: a Gynecologic Oncology Group Study. J Transl Med. 2012;10:79 pubmed publisher
    ..The potent ribonucleotide reductase (RNR) inhibitor 3-aminopyridine-2-carboxyaldehyde-thiosemicarbazone (3-AP) was tested as a chemosensitizer for restored cisplatin-mediated cytotoxicity in platinum-resistant ovarian cancer...
  50. Mak A, Pehar M, Nixon A, Williams R, Uetrecht A, Puglielli L, et al. Post-translational regulation of CD133 by ATase1/ATase2-mediated lysine acetylation. J Mol Biol. 2014;426:2175-82 pubmed publisher
    ..Taken together, we suggest that lysine acetylation on predicted extracellular residues plays a key role in expression and trafficking of CD133 protein to the cell surface and can be targeted to disrupt CD133 regulation and function. ..
  51. Slim R, Hammock B, Toborek M, Robertson L, Newman J, Morisseau C, et al. The role of methyl-linoleic acid epoxide and diol metabolites in the amplified toxicity of linoleic acid and polychlorinated biphenyls to vascular endothelial cells. Toxicol Appl Pharmacol. 2001;171:184-93 pubmed
    ..These findings have implications in understanding interactive mechanisms of how dietary fats can modulate dysfunction of the vascular endothelium mediated by certain environmental contaminants. ..
  52. Grunewald G, Dahanukar V, Criscione K. Effects of a 3-alkyl-, 4-hydroxy- and/or 8-aromatic-substituent on the phenylethanolamine N-methyltransferase inhibitor potency and alpha2-adrenoceptor affinity of 2,3,4,5-tetrahydro-1H-2-benzazepines. Bioorg Med Chem. 2001;9:1957-65 pubmed
    ..Compound 3 is the most selective (PNMT/alpha2) and one of the more potent at PNMT compounds yet reported in the benzazepine series, and should have sufficient lipophilicity to penetrate the blood-brain barrier (CLogP = 1.8). ..
  53. Khundmiri S, Metzler M, Ameen M, Amin V, Rane M, Delamere N. Ouabain induces cell proliferation through calcium-dependent phosphorylation of Akt (protein kinase B) in opossum kidney proximal tubule cells. Am J Physiol Cell Physiol. 2006;291:C1247-57 pubmed
    ..Taken together, the results point to a role for CCE and Akt phosphorylation, in response to low concentrations of ouabain, that increase the rate of cell proliferation without inhibiting Na(+)-K(+)-ATPase-mediated ion transport...
  54. Drawz S, Bethel C, Doppalapudi V, Sheri A, Pagadala S, Hujer A, et al. Penicillin sulfone inhibitors of class D beta-lactamases. Antimicrob Agents Chemother. 2010;54:1414-24 pubmed publisher
    ..By exploiting conserved structural and mechanistic features, JDB/LN-1-255 is a promising lead compound in the quest for effective inhibitors of OXA-type beta-lactamases. ..
  55. Herman S, Gordon A, Wagner A, Heerema N, Zhao W, Flynn J, et al. Phosphatidylinositol 3-kinase-? inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood. 2010;116:2078-88 pubmed publisher
    ..Collectively, these studies provide rationale for the clinical development of CAL-101 as a first-in-class targeted therapy for CLL and related B-cell lymphoproliferative disorders. ..
  56. Paintlia A, Paintlia M, Singh A, Singh I. Modulation of Rho-Rock signaling pathway protects oligodendrocytes against cytokine toxicity via PPAR-?-dependent mechanism. Glia. 2013;61:1500-1517 pubmed publisher
  57. Knight J, Luo W, O Dell A, Yalavarthi S, Zhao W, Subramanian V, et al. Peptidylarginine deiminase inhibition reduces vascular damage and modulates innate immune responses in murine models of atherosclerosis. Circ Res. 2014;114:947-56 pubmed publisher
    ..These results support a role for aberrant NET formation in the pathogenesis of atherosclerosis through modulation of innate immune responses. ..
  58. Lombardo L, Lee F, Chen P, Norris D, Barrish J, Behnia K, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004;47:6658-61 pubmed
    ..On the basis of its robust in vivo activity and favorable pharmacokinetic profile, 13 was selected for additional characterization for oncology indications. ..
  59. Newcomer S, Taylor J, Bowles D, Laughlin M. Endothelium-dependent and -independent relaxation in the forelimb and hindlimb vasculatures of swine. Comp Biochem Physiol A Mol Integr Physiol. 2007;148:292-300 pubmed
    ..The current results of this investigation suggest that the forelimb and hindlimb vasculatures of swine have relatively similar vasorelaxation responses to both endothelium-dependent and -independent vasodilators. ..
  60. Gentry E, Henderson B, Arrant A, Gearing M, Feng Y, Riddle N, et al. Rho Kinase Inhibition as a Therapeutic for Progressive Supranuclear Palsy and Corticobasal Degeneration. J Neurosci. 2016;36:1316-23 pubmed publisher
    ..Our study correlates bona fide changes in PSP and CBD brains with cellular models, identifies drug targets, and tests the therapeutic in vivo. ..
  61. Fero M, Rivkin M, Tasch M, Porter P, Carow C, Firpo E, et al. A syndrome of multiorgan hyperplasia with features of gigantism, tumorigenesis, and female sterility in p27(Kip1)-deficient mice. Cell. 1996;85:733-44 pubmed
    ..The absence of p27 also caused an ovulatory defect and female sterility. Maturation of secondary ovarian follicles into corpora lutea, which express high levels of p27, was markedly impaired...
  62. Xiao H, Yin T, Wang X, Uchida T, Chung J, White M, et al. Specificity of interleukin-2 receptor gamma chain superfamily cytokines is mediated by insulin receptor substrate-dependent pathway. J Biol Chem. 2002;277:8091-8 pubmed
    ..These data suggest that IRS-dependent signaling pathways work by recruiting different signaling molecules to determine specificity of IL-2R gamma superfamily cytokines. ..
  63. Konduri S, Srivenugopal K, Yanamandra N, Dinh D, Olivero W, Gujrati M, et al. Promoter methylation and silencing of the tissue factor pathway inhibitor-2 (TFPI-2), a gene encoding an inhibitor of matrix metalloproteinases in human glioma cells. Oncogene. 2003;22:4509-16 pubmed
    ..These studies establish that TFPI-2 is transcriptionally silenced through promoter methylation in SNB19 cells. ..
  64. Lai J, Yu C, Moser C, Aderca I, Han T, Garvey T, et al. SULF1 inhibits tumor growth and potentiates the effects of histone deacetylase inhibitors in hepatocellular carcinoma. Gastroenterology. 2006;130:2130-44 pubmed
    ..The interaction between SULF1 and apicidin was confirmed in vivo in Huh7 and Hep3B xenografts. These results show that SULF1 promotes histone H4 acetylation, potentiates the effects of HDAC inhibitors, and inhibits HCC tumorigenesis. ..
  65. Foster J, Carmines P, Pollock J. PP2B-dependent NO production in the medullary thick ascending limb during diabetes. Am J Physiol Renal Physiol. 2009;297:F471-80 pubmed publisher
    ..In conclusion, while NO bioavailability in mTALs is reduced during diabetes, free radical scavenging with tempol unmasks increased NO production that involves PP2B-dependent activation of NOS1 and NOS2...
  66. Jaiswal A, Banerjee S, Panda H, Bulkin C, Izumi T, Sarkar F, et al. A novel inhibitor of DNA polymerase beta enhances the ability of temozolomide to impair the growth of colon cancer cells. Mol Cancer Res. 2009;7:1973-83 pubmed publisher
    ..Our findings provide the "proof-of-concept" for the development of highly specific and thus safer structure-based inhibitors for the prevention of tumor progression and/or treatment of colorectal cancer. ..
  67. Kundu S, Roome T, Bhattacharjee A, Carnevale K, Yakubenko V, Zhang R, et al. Metabolic products of soluble epoxide hydrolase are essential for monocyte chemotaxis to MCP-1 in vitro and in vivo. J Lipid Res. 2013;54:436-47 pubmed publisher
    ..Their effectiveness, often attributed to increasing EET levels, is probably influenced by the impairment of DHET formation and inhibition of chemotaxis. ..
  68. Pathak M, Dhawan D, Lindner D, Borden E, Farver C, Yi T. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther. 2002;1:1255-64 pubmed
    ..These observations suggest the potential of pentamidine in anticancer therapies and may provide a basis for developing novel PTPase-targeted therapeutics. ..
  69. Yang L, Xie S, Jamaluddin M, Altuwaijri S, Ni J, Kim E, et al. Induction of androgen receptor expression by phosphatidylinositol 3-kinase/Akt downstream substrate, FOXO3a, and their roles in apoptosis of LNCaP prostate cancer cells. J Biol Chem. 2005;280:33558-65 pubmed
    ..Together, our data provide the first model to explain how PI3K/Akt and AR can cooperate to control LNCaP cell growth and death under normal conditions. ..
  70. Kuritzky L. Noninvasive management of lower urinary tract symptoms and sexual dysfunction associated with benign prostatic hyperplasia in the primary care setting. Compr Ther. 2005;31:194-208 pubmed
  71. Ostrov D, Hernandez Prada J, Corsino P, Finton K, Le N, Rowe T. Discovery of novel DNA gyrase inhibitors by high-throughput virtual screening. Antimicrob Agents Chemother. 2007;51:3688-98 pubmed
    ..coli DNA gyrase. These compounds are structurally unrelated to previously identified gyrase inhibitors and represent potential scaffolds for the optimization of novel antibacterial agents that act on fluoroquinolone-resistant strains. ..
  72. Moser L, Schultz Cherry S. Suppression of astrovirus replication by an ERK1/2 inhibitor. J Virol. 2008;82:7475-82 pubmed publisher
    ..These data support a role for ERK1/2 in a postattachment step, although the precise mechanism remains under investigation. ..
  73. Fallon M, MacDonald M. Beta-cell alpha-ketoglutarate hydroxylases may acutely participate in insulin secretion. Metabolism. 2008;57:1148-54 pubmed publisher
    ..It is possible that an increase in mitochondrially generated alpha-ketoglutarate derived from insulin secretagogue carbon and translocated to the cytosol may be part of the signal for insulin secretion. ..
  74. Chen X, Fu W, Tung C, Ward N. Angiopoietin-1 induces neurite outgrowth of PC12 cells in a Tie2-independent, beta1-integrin-dependent manner. Neurosci Res. 2009;64:348-54 pubmed publisher
    ..Our results suggest that Ang1 induces neurite outgrowth in PC12 cells in a Tie2-independent, beta1-integrin-FAK-PI3K-Akt-dependent manner and that NGF and Ang1 mediate neurite outgrowth via two independent signaling mechanisms. ..
  75. McManus M, Murphy M, Franklin J. The mitochondria-targeted antioxidant MitoQ prevents loss of spatial memory retention and early neuropathology in a transgenic mouse model of Alzheimer's disease. J Neurosci. 2011;31:15703-15 pubmed publisher
  76. Matsuoka Y, Yang J. Selective inhibition of extracellular signal-regulated kinases 1/2 blocks nerve growth factor to brain-derived neurotrophic factor signaling and suppresses the development of and reverses already established pain behavior in rats. Neuroscience. 2012;206:224-36 pubmed publisher
    ..Our results suggest the possible use of AZD6244, already in human clinical trials as an anticancer agent, for the treatment of pathological pain. ..
  77. Liu Q, Rehman H, Shi Y, Krishnasamy Y, Lemasters J, Smith C, et al. Inhibition of sphingosine kinase-2 suppresses inflammation and attenuates graft injury after liver transplantation in rats. PLoS ONE. 2012;7:e41834 pubmed publisher
    ..In conclusion, SK2 plays an important role in hepatic inflammation responses and graft injury after cold storage/transplantation and represents a new therapeutic target for liver graft failure. ..
  78. Wolf B, Weisbrode S. Safety evaluation of an extract from Salacia oblonga. Food Chem Toxicol. 2003;41:867-74 pubmed
  79. Blagoveshchenskaya A, Cheong F, Rohde H, Glover G, Knödler A, Nicolson T, et al. Integration of Golgi trafficking and growth factor signaling by the lipid phosphatase SAC1. J Cell Biol. 2008;180:803-12 pubmed publisher
    ..Inhibition of p38 MAPK abolishes growth factor-induced Golgi-to-ER shuttling of SAC1 and slows secretion. These results suggest direct roles for p38 MAPK and SAC1 in transmitting growth signals to the secretory machinery. ..
  80. Moreb J, Baker H, Chang L, Amaya M, Lopez M, Ostmark B, et al. ALDH isozymes downregulation affects cell growth, cell motility and gene expression in lung cancer cells. Mol Cancer. 2008;7:87 pubmed publisher
    ..Aldehyde dehydrogenase isozymes ALDH1A1 and ALDH3A1 are highly expressed in non small cell lung cancer. Neither the mechanisms nor the biologic significance for such over expression have been studied...
  81. Son Y, Lee S, Kim S, Jang Y, Chun J, Lee J. Acteoside inhibits melanogenesis in B16F10 cells through ERK activation and tyrosinase down-regulation. J Pharm Pharmacol. 2011;63:1309-19 pubmed publisher
    ..Acteoside decreased tyrosinase activity and melanin biosynthesis in B16F10 cells by activating ERK signalling, which down-regulated MITF, tyrosinase and TRP-1 production. ..
  82. Yan L, Yan C, Qian K, Su H, Kofsky Wofford S, Lee W, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014;57:2611-22 pubmed publisher
    ..Furthermore, cellular studies revealed that 1 is cell membrane permeable and effectively inhibits intracellular PRMT1 activity and blocks cell proliferation in leukemia cell lines with different genetic lesions. ..
  83. Sy S, Tang B, Pastrakuljic A, Roberts E, Kalow W. Detailed characterization of experimentally derived human hepatic CYP1A1 activity and expression using differential inhibition of ethoxyresorufin O-deethylation by fluvoxamine. Eur J Clin Pharmacol. 2001;57:377-86 pubmed
    ..To characterize the distribution of mathematically derived human hepatic CYP1A1 activity using differential inhibition of ethoxyresorufin O-deethylation (EROD) by fluvoxamine...
  84. Ankenman R, Salvatore M. Low dose alpha-methyl-para-tyrosine (AMPT) in the treatment of dystonia and dyskinesia. J Neuropsychiatry Clin Neurosci. 2007;19:65-9 pubmed
    ..The authors propose that a special utility of AMPT in tardive disorders may be related to a downregulation of tyrosine hydroxylase activity that may be increased by neuroleptic-induced effects on tyrosine hydroxylase phosphorylation. ..
  85. Drawz S, Bonomo R. Three decades of beta-lactamase inhibitors. Clin Microbiol Rev. 2010;23:160-201 pubmed publisher
    ..The goal for the next 3 decades will be to design inhibitors that will be effective for more than a single class of beta-lactamases. ..
  86. Sekeres M, List A, Cuthbertson D, Paquette R, Ganetzky R, Ganetsky R, et al. Phase I combination trial of lenalidomide and azacitidine in patients with higher-risk myelodysplastic syndromes. J Clin Oncol. 2010;28:2253-8 pubmed publisher
    ..The combination of lenalidomide and azacitidine is well tolerated with encouraging clinical activity. The go-forward dose is azacitidine 75 mg/m(2) on days 1 through 5 and lenalidomide 10 mg on days 1 through 21. ..
  87. Ochsner U, Sun X, Jarvis T, Critchley I, Janjic N. Aminoacyl-tRNA synthetases: essential and still promising targets for new anti-infective agents. Expert Opin Investig Drugs. 2007;16:573-93 pubmed
    ..This review provides an update on the present strategies to develop novel aaRS inhibitors as anti-infective drugs. ..
  88. Totir M, Helfand M, Carey M, Sheri A, Buynak J, Bonomo R, et al. Sulbactam forms only minimal amounts of irreversible acrylate-enzyme with SHV-1 beta-lactamase. Biochemistry. 2007;46:8980-7 pubmed
  89. Naydenov N, Harris G, Brown B, Schaefer K, Das S, Fisher P, et al. Loss of soluble N-ethylmaleimide-sensitive factor attachment protein ? (?SNAP) induces epithelial cell apoptosis via down-regulation of Bcl-2 expression and disruption of the Golgi. J Biol Chem. 2012;287:5928-41 pubmed publisher
    ..These results reveal a novel role for ?SNAP in promoting epithelial cell survival by unique mechanisms involving regulation of Bcl-2 expression and Golgi biogenesis. ..
  90. Chang K, Ponder J, Labarbera D, Petrash J. Aldose reductase inhibition prevents endotoxin-induced inflammatory responses in retinal microglia. Invest Ophthalmol Vis Sci. 2014;55:2853-61 pubmed publisher
    ..These results demonstrate that the action of AR contributes to the activation of RMG. Inhibition of AR may be a therapeutic strategy to reduce inflammation associated with activation of RMG in disease. ..
  91. Malathi K, Paranjape J, Ganapathi R, Silverman R. HPC1/RNASEL mediates apoptosis of prostate cancer cells treated with 2',5'-oligoadenylates, topoisomerase I inhibitors, and tumor necrosis factor-related apoptosis-inducing ligand. Cancer Res. 2004;64:9144-51 pubmed
    ..These findings indicate that RNase L integrates and amplifies apoptotic signals generated during treatment of prostate cancer cells with 2-5A, Topo I inhibitors, and TRAIL. ..
  92. Clark B, Li J. Janus kinase 2 signaling in the angiotensin II-dependent activation of StAR expression. Endocr Res. 2004;30:685-93 pubmed