Experts and Doctors on enzyme inhibitors in United States


Locale: United States
Topic: enzyme inhibitors

Top Publications

  1. Hong Y, Roy R, Ambros V. Developmental regulation of a cyclin-dependent kinase inhibitor controls postembryonic cell cycle progression in Caenorhabditis elegans. Development. 1998;125:3585-97 pubmed
    ..In vulva precursor cells (VPCs), a pathway of heterochronic genes acts via cki-1 to maintain VPCs in G1 during the L2 stage. ..
  2. Peluffo R, Arguello J, Lingrel J, Berlin J. Electrogenic sodium-sodium exchange carried out by Na,K-ATPase containing the amino acid substitution Glu779Ala. J Gen Physiol. 2000;116:61-73 pubmed
    ..M. Argüello, and J.R. Berlin. 2000. J. Gen. Physiol. 116:47-59). This model showed that alterations in the kinetics of extracellular ion-dependent reactions alone could explain the effects of Glu779Ala substitution on the Na,K-ATPase. ..
  3. Liu J, Kern J. Neuregulin-1 activates the JAK-STAT pathway and regulates lung epithelial cell proliferation. Am J Respir Cell Mol Biol. 2002;27:306-13 pubmed
    ..This pathway plays an important role in NRG-1-stimulated proliferation of pulmonary epithelial cells. ..
  4. DiPetrillo K, Wood S, Kostrubsky V, Chatfield K, Bement J, Wrighton S, et al. Effect of caffeine on acetaminophen hepatotoxicity in cultured hepatocytes treated with ethanol and isopentanol. Toxicol Appl Pharmacol. 2002;185:91-7 pubmed
    ..The results indicate that CYP3A is responsible for the caffeine-mediated stimulation of APAP toxicity. Our results suggest that caffeine may be an additional risk factor for developing alcohol-mediated APAP hepatotoxicity. ..
  5. Tian G, Ghanekar S, Aharony D, Shenvi A, Jacobs R, Liu X, et al. The mechanism of gamma-secretase: multiple inhibitor binding sites for transition state analogs and small molecule inhibitors. J Biol Chem. 2003;278:28968-75 pubmed
    ..These findings provide useful insights into the catalytic and regulatory mechanisms of gamma-secretase that may facilitate the design of novel gamma-secretase inhibitors. ..
  6. Knappenberger K, Tian G, Ye X, Sobotka Briner C, Ghanekar S, Greenberg B, et al. Mechanism of gamma-secretase cleavage activation: is gamma-secretase regulated through autoinhibition involving the presenilin-1 exon 9 loop?. Biochemistry. 2004;43:6208-18 pubmed
    ..It is possible that the DeltaE9 mutation causes Alzheimer's disease because cleavage activation of gamma-secretase is no longer necessary, alleviating constraints on Abeta formation. ..
  7. Yoo H, Kumagai A, Shevchenko A, Shevchenko A, Dunphy W. Adaptation of a DNA replication checkpoint response depends upon inactivation of Claspin by the Polo-like kinase. Cell. 2004;117:575-88 pubmed
    ..These results indicate that the Plx1-dependent inactivation of Claspin results in termination of a DNA replication checkpoint response. ..
  8. Van Dross R, Yao S, Asad S, Westlake G, Mays D, Barquero L, et al. Constitutively active K-cyclin/cdk6 kinase in Kaposi sarcoma-associated herpesvirus-infected cells. J Natl Cancer Inst. 2005;97:656-66 pubmed
    ..The constitutive activation of K-cyclin/cdk complexes in KSHV-infected cells appears to result from the extended half-life of K-cyclin and may explain its role in Kaposi sarcoma. ..
  9. Yu C, Yezierski R. Activation of the ERK1/2 signaling cascade by excitotoxic spinal cord injury. Brain Res Mol Brain Res. 2005;138:244-55 pubmed
    ..Blockade of this intracellular kinase cascade prevented the onset of injury-induced pain behavior. ..

More Information

Publications323 found, 100 shown here

  1. Li S, Fang C, Aberle N, Ren B, Ceylan Isik A, Ren J. Inhibition of PI-3 kinase/Akt/mTOR, but not calcineurin signaling, reverses insulin-like growth factor I-induced protection against glucose toxicity in cardiomyocyte contractile function. J Endocrinol. 2005;186:491-503 pubmed
    ..Collectively, our data suggest that IGF-1 may provide cardiac protection against glucose in part through a PI-3 kinase/Akt/mTOR/ p70s6k-dependent and calcineurin-independent pathway. ..
  2. Schmidt L, Ballman K, Tindall D. Inhibition of fatty acid synthase activity in prostate cancer cells by dutasteride. Prostate. 2007;67:1111-20 pubmed
    ..This is the first study to examine the effects of clinically relevant levels of dutasteride on prostate cancer cells at the molecular level and specifically, demonstrating the inhibition of FASN in these cells. ..
  3. Dong F, Ren J. Fidarestat improves cardiomyocyte contractile function in db/db diabetic obese mice through a histone deacetylase Sir2-dependent mechanism. J Hypertens. 2007;25:2138-47 pubmed
    ..Collectively, these results suggest that fidarestat may protect against cardiomyocyte dysfunction in db/db mice through a Sir2-dependent pathway. ..
  4. Gaffield M, Betz W. Synaptic vesicle mobility in mouse motor nerve terminals with and without synapsin. J Neurosci. 2007;27:13691-700 pubmed
    ..Thus, in TKO mice, and perhaps WT mice, a phospho-protein different from synapsin but otherwise of unknown identity is the primary regulator of synaptic vesicle mobility. ..
  5. Wang H, Kohr M, Traynham C, Wheeler D, Janssen P, Ziolo M. Neuronal nitric oxide synthase signaling within cardiac myocytes targets phospholamban. Am J Physiol Cell Physiol. 2008;294:C1566-75 pubmed publisher
    ..In summary, NOS1 inhibition or knockout leads to decreased contraction and slowed [Ca2+]i decline, and this effect is absent in PLB-/- myocytes. Thus NOS1 signaling modulates PLB serine16 phosphorylation, in part, via peroxynitrite. ..
  6. Hadden M, Hill S, Davenport J, Matts R, Blagg B. Synthesis and evaluation of Hsp90 inhibitors that contain the 1,4-naphthoquinone scaffold. Bioorg Med Chem. 2009;17:634-40 pubmed publisher
    ..The identification of these naphthoquinones as Hsp90 inhibitors provides a new scaffold upon which improved Hsp90 inhibitors can be developed. ..
  7. Parker S, Barkley R, Rino J, Vasil M. Mycobacterium tuberculosis Rv3802c encodes a phospholipase/thioesterase and is inhibited by the antimycobacterial agent tetrahydrolipstatin. PLoS ONE. 2009;4:e4281 pubmed publisher
    ..tuberculosis pathogenesis, identification of a novel cell wall enzyme and its inhibition has therapeutic and diagnostic implications. ..
  8. Zmarowski A, Wu H, Brooks J, Potter M, Pellicciari R, Schwarcz R, et al. Astrocyte-derived kynurenic acid modulates basal and evoked cortical acetylcholine release. Eur J Neurosci. 2009;29:529-38 pubmed publisher
  9. Qiao L, Zhang J. Inhibition of lysosomal functions reduces proteasomal activity. Neurosci Lett. 2009;456:15-9 pubmed publisher
    ..Inhibition of lysosomal or proteasomal activities led to higher levels of chaperone heat shock cognate protein Hsc70, suggesting an attempt to compensate protein degradation deficiency by enhancing chaperone-mediated autophagy. ..
  10. Dailey M, Hait C, Holt P, Maguire J, Meier J, Miller M, et al. Structure-based drug design: from nucleic acid to membrane protein targets. Exp Mol Pathol. 2009;86:141-50 pubmed publisher
    ..We also review examples of molecular modeling to understand receptors and using virtual screening against G-protein coupled receptor membrane proteins. ..
  11. Cody V, Pace J. Structural analysis of Pneumocystis carinii and human DHFR complexes with NADPH and a series of five potent 6-[5'-(ω-carboxyalkoxy)benzyl]pyrido[2,3-d]pyrimidine derivatives. Acta Crystallogr D Biol Crystallogr. 2011;67:1-7 pubmed publisher
  12. Giannone P, Alcamo A, Schanbacher B, Nankervis C, Besner G, Bauer J. Poly(ADP-ribose) polymerase-1: a novel therapeutic target in necrotizing enterocolitis. Pediatr Res. 2011;70:67-71 pubmed publisher
    ..We speculate that PARP-1 overactivation in NEC may drive mucosal cell death in this disease and that PARP-1 may be a novel therapeutic target in NEC. ..
  13. ZIMMERMAN B, Sargeant A, Landes K, Fernandez S, Chen C, Lairmore M. Efficacy of novel histone deacetylase inhibitor, AR42, in a mouse model of, human T-lymphotropic virus type 1 adult T cell lymphoma. Leuk Res. 2011;35:1491-7 pubmed publisher
    ..Our data provide new directions for the treatment of ATL and support the further development of AR-42 against HTLV-1-associated lymphoid malignancies. ..
  14. Secor J, Kotha S, Gurney T, Patel R, Kefauver N, Gupta N, et al. Novel lipid-soluble thiol-redox antioxidant and heavy metal chelator, N,N'-bis(2-mercaptoethyl)isophthalamide (NBMI) and phospholipase D-specific inhibitor, 5-fluoro-2-indolyl des-chlorohalopemide (FIPI) attenuate mercury-induced lipid signaling lead. Int J Toxicol. 2011;30:619-38 pubmed publisher
    ..For the first time, this study demonstrated that redox-dependent and PLD-mediated bioactive lipid signaling was involved in mercury-induced vascular EC cytotoxicity which was protected by NBMI and FIPI. ..
  15. Sciarretta S, Zhai P, Volpe M, Sadoshima J. Pharmacological modulation of autophagy during cardiac stress. J Cardiovasc Pharmacol. 2012;60:235-41 pubmed publisher
    ..We will discuss the potential usefulness of different pharmacological activators and inhibitors of autophagy in the treatment of cardiac diseases. ..
  16. Argyros R, Nelson S, Kull A, Chen M, Stadheim T, Jiang B. A phenylalanine to serine substitution within an O-protein mannosyltransferase led to strong resistance to PMT-inhibitors in Pichia pastoris. PLoS ONE. 2013;8:e62229 pubmed publisher
    ..Our data also indicate that the main target of these PMT-inhibitors in P. pastoris is Pmt2p, and that the F664 residue most likely interacts directly with the PMTi-compounds...
  17. Tsuji H, Wang W, Sunil J, Shimizu N, Yoshimura K, Uemura H, et al. Involvement of renin-angiotensin-aldosterone system in calcium oxalate crystal induced activation of NADPH oxidase and renal cell injury. World J Urol. 2016;34:89-95 pubmed publisher
    ..Results indicate that hyperoxaluria-induced production of ROS, injury and inflammation are in part associated with the activation of Nox through renin-angiotensin-aldosterone pathway. ..
  18. Woodford M, Truman A, Dunn D, Jensen S, Cotran R, Bullard R, et al. Mps1 Mediated Phosphorylation of Hsp90 Confers Renal Cell Carcinoma Sensitivity and Selectivity to Hsp90 Inhibitors. Cell Rep. 2016;14:872-884 pubmed publisher
    ..Mps1 expression level can potentially serve as a predictive indicator of tumor response to Hsp90 inhibitors. ..
  19. Ostrerova N, Petrucelli L, Farrer M, Mehta N, Choi P, Hardy J, et al. alpha-Synuclein shares physical and functional homology with 14-3-3 proteins. J Neurosci. 1999;19:5782-91 pubmed
    ..The activity and binding profile of alpha-synuclein suggests that it might act as a protein chaperone and that accumulation of alpha-synuclein could contribute to cell death in neurodegenerative diseases. ..
  20. Roselli C, Resko J, Stormshak F. Estrogen synthesis in fetal sheep brain: effect of maternal treatment with an aromatase inhibitor. Biol Reprod. 2003;68:370-4 pubmed
    ..They also demonstrate that AA can be inhibited in the fetal lamb brain by treating the mother with ATD, without harming fetal development. ..
  21. Sylte M, Leite F, Kuckleburg C, Inzana T, Czuprynski C. Caspase activation during Haemophilus somnus lipooligosaccharide-mediated apoptosis of bovine endothelial cells. Microb Pathog. 2003;35:285-91 pubmed
    ..These data suggest that LOS-mediated activation of caspase-3 and apoptosis of endothelial cells is caspase-8 dependent...
  22. Diaz Meyer N, Day C, Khatod K, Maher E, Cooper W, Reik W, et al. Silencing of CDKN1C (p57KIP2) is associated with hypomethylation at KvDMR1 in Beckwith-Wiedemann syndrome. J Med Genet. 2003;40:797-801 pubmed
    ..An epimutation at KvDMR1, the absence of maternal methylation, causes the aberrant silencing of CDKN1C, some 180 kb away on the maternal chromosome. Similar to mutations at this locus, this silencing may give rise to BWS. ..
  23. Stanley W, Morgan E, Huang H, McElfresh T, Sterk J, Okere I, et al. Malonyl-CoA decarboxylase inhibition suppresses fatty acid oxidation and reduces lactate production during demand-induced ischemia. Am J Physiol Heart Circ Physiol. 2005;289:H2304-9 pubmed
    ..Thus modulation of MCD activity is an effective means of regulating myocardial fatty acid oxidation under normal and ischemic conditions and reducing lactate production during demand-induced ischemia. ..
  24. Kessl J, Meshnick S, Trumpower B. Modeling the molecular basis of atovaquone resistance in parasites and pathogenic fungi. Trends Parasitol. 2007;23:494-501 pubmed
    ..To better understand the molecular basis of drug resistance, we have developed the yeast and bovine bc1 complexes as surrogates to model the molecular interaction of atovaquone with human and resistant pathogen enzymes. ..
  25. Yan G, Chen S, You B, Sun J. Activation of sphingosine kinase-1 mediates induction of endothelial cell proliferation and angiogenesis by epoxyeicosatrienoic acids. Cardiovasc Res. 2008;78:308-14 pubmed publisher
    ..Thus, SK1 may represent a novel therapeutic modality for the treatment of angiogenesis-related diseases such as cancer and ischaemia. ..
  26. Suryanarayana S, Göttle M, Hübner M, Gille A, Mou T, Sprang S, et al. Differential inhibition of various adenylyl cyclase isoforms and soluble guanylyl cyclase by 2',3'-O-(2,4,6-trinitrophenyl)-substituted nucleoside 5'-triphosphates. J Pharmacol Exp Ther. 2009;330:687-95 pubmed publisher
    ..TNP-ATP is the most potent sGC inhibitor known so far. ..
  27. Rowe J, Greenblatt R, Liu D, Moffat J. Compounds that target host cell proteins prevent varicella-zoster virus replication in culture, ex vivo, and in SCID-Hu mice. Antiviral Res. 2010;86:276-85 pubmed publisher
    ..In SCID mice with skin xenografts, roscovitine (0.7 mg/kg/day) was as effective as PAA (36 mg/kg/day). The screening systems described here are useful models for evaluating novel antiviral drugs for VZV. ..
  28. Kauser K, da Cunha V, Fitch R, Mallari C, Rubanyi G. Role of endogenous nitric oxide in progression of atherosclerosis in apolipoprotein E-deficient mice. Am J Physiol Heart Circ Physiol. 2000;278:H1679-85 pubmed
    ..The acceleration in lesion size concomitant to the severely impaired NO-mediated responses indicates that lack of endogenous NO is an important progression factor of atherosclerosis in the apoE-KO mouse...
  29. Zhou Y, Guo X, Yi T, Yoshimoto T, Pei D. Two continuous spectrophotometric assays for methionine aminopeptidase. Anal Biochem. 2000;280:159-65 pubmed
    ..These results demonstrate that the current assays are convenient, rapid, and sensitive methods for kinetic studies of MetAPs and effective tools for screening MetAP inhibitors. ..
  30. Rubin L, Johnson L, Dodam J, Dhalla A, Magliola L, Laughlin M, et al. Selective transport of adenosine into porcine coronary smooth muscle. Am J Physiol Heart Circ Physiol. 2000;279:H1397-410 pubmed
    ..These data indicate CSM possess a high-affinity nucleoside transporter and that the activity of this transporter is sufficient to modulate ADO sensitivity of large and small coronary arteries...
  31. Geiger L, Kortuem K, Alexejun C, Levin L. Reduced redox state allows prolonged survival of axotomized neonatal retinal ganglion cells. Neuroscience. 2002;109:635-42 pubmed
    ..Understanding the mechanisms by which ROS signal neuronal death could result in strategies for increasing their long-term survival after axonal injury. ..
  32. Roberts A, Bowman M, Kramer D. Certain metal ions are inhibitors of cytochrome b6f complex 'Rieske' iron-sulfur protein domain movements. Biochemistry. 2002;41:4070-9 pubmed
    ..These results support the role of ISP domain movements in Q(o) site catalysis. ..
  33. Ward E, Wolfsen H. Pharmacological management of Cronkhite-Canada syndrome. Expert Opin Pharmacother. 2003;4:385-9 pubmed
    ..Most recently, a combination regimen using histamine-receptor antagonists, cromolyn sodium, prednisone and suppressive antibiotics has been described. The reported treatment options and rates of success are reviewed. ..
  34. Puri S, Magenheimer B, Maser R, Ryan E, Zien C, Walker D, et al. Polycystin-1 activates the calcineurin/NFAT (nuclear factor of activated T-cells) signaling pathway. J Biol Chem. 2004;279:55455-64 pubmed
  35. Chaisson M, Branstetter D, Derry J, Armstrong A, Tometsko M, Takeda K, et al. Osteoclast differentiation is impaired in the absence of inhibitor of kappa B kinase alpha. J Biol Chem. 2004;279:54841-8 pubmed
  36. Protasevich I, Brouillette C, Snow M, Dunham S, Rubin J, Gogliotti R, et al. Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance. Biochemistry. 2004;43:13380-9 pubmed
    ..This finding, coupled with a binding site conformation that is likely to be more rigid in the mutant, appears to result in the drug resistance of (F203L)FabI. ..
  37. McMullen C, Hayess K, Andrade F. Fatigue resistance of rat extraocular muscles does not depend on creatine kinase activity. BMC Physiol. 2005;5:12 pubmed
    ..Total AK activity was similar in EDL and extraocular muscles. These data indicate that the characteristic fatigue resistance of the extraocular muscles does not depend on CK activity. ..
  38. Do T, Kerr B, Kuzhikandathil E. Brain-derived neurotrophic factor regulates the expression of D1 dopamine receptors. J Neurochem. 2007;100:416-28 pubmed
    ..Promoter deletion analysis identified a D(1) promoter region necessary for mediating the effect of BDNF. These results provide novel evidence that D(1) dopamine receptor expression is regulated by BDNF and its signaling pathway. ..
  39. Muja N, Nelson J, DeVries G. Schwann cells express IP prostanoid receptors coupled to an elevation in intracellular cyclic AMP. J Neurosci Res. 2007;85:1159-69 pubmed
    ..These findings suggest that signaling via the IP prostanoid receptor may by relevant to Schwann cell biology in vivo. ..
  40. Tian N, Moore R, Phillips W, Lin L, Braddy S, Pryor J, et al. NADPH oxidase contributes to renal damage and dysfunction in Dahl salt-sensitive hypertension. Am J Physiol Regul Integr Comp Physiol. 2008;295:R1858-65 pubmed publisher
    ..These data suggest that NADPH oxidase plays an important role in causing renal cortical oxidative stress and inflammation, which lead to decreases in renal hemodynamics, renal cortical damage, and increases in arterial pressure. ..
  41. Tang K, Mansoorabadi S, Reed G, Frey P. Radical triplets and suicide inhibition in reactions of 4-thia-D- and 4-thia-L-lysine with lysine 5,6-aminomutase. Biochemistry. 2009;48:8151-60 pubmed publisher
    ..The observation of the transient radical supports the hypothetical isomerization mechanism. ..
  42. Lee D, Lin X, Paskaleva E, Liu Y, Puttamadappa S, Thornber C, et al. Palmitic Acid Is a Novel CD4 Fusion Inhibitor That Blocks HIV Entry and Infection. AIDS Res Hum Retroviruses. 2009;25:1231-41 pubmed publisher
    ..Understanding the structure-affinity relationship (SAR) between PA and CD4 should lead to the development of PA analogs with greater potency against HIV-1 entry...
  43. Doshi U, Li A. Luciferin IPA-based higher throughput human hepatocyte screening assays for CYP3A4 inhibition and induction. J Biomol Screen. 2011;16:903-9 pubmed publisher
  44. Stephens E, Walsh A, Scott E. Evaluation of inhibition selectivity for human cytochrome P450 2A enzymes. Drug Metab Dispos. 2012;40:1797-802 pubmed publisher
  45. Wysham N, Sullivan D, Allada G. An opportunistic infection associated with ruxolitinib, a novel janus kinase 1,2 inhibitor. Chest. 2013;143:1478-1479 pubmed publisher
    ..Clinicians should be aware of the potential for intracellular or opportunistic infections associated with this novel drug class. ..
  46. Wilson A, Erdman R, Castellano F, Maltese W. Prenylation of Rab8 GTPase by type I and type II geranylgeranyl transferases. Biochem J. 1998;333 ( Pt 3):497-504 pubmed
    ..Prenylation of the Y78D mutant was reduced by 60-70% in intact cells, consistent with the conclusion that the majority of Rab8 is prenylated by the REP/GGTaseII system in vivo. ..
  47. Pathak M, Yi T. Sodium stibogluconate is a potent inhibitor of protein tyrosine phosphatases and augments cytokine responses in hemopoietic cell lines. J Immunol. 2001;167:3391-7 pubmed
    ..Our results provide novel insights into the pharmacological effects of the drug and suggest potential new therapeutic applications. ..
  48. Ackerman W, Rovin B, Kniss D. Epidermal growth factor and interleukin-1beta utilize divergent signaling pathways to synergistically upregulate cyclooxygenase-2 gene expression in human amnion-derived WISH cells. Biol Reprod. 2004;71:2079-86 pubmed
    ..The synergism observed between IL-1beta and EGF does not rely on augmented NFkappaB function, but rather, occurs through differential use of independent response elements within the COX-2 promoter. ..
  49. Wang X, Yu S. Novel regulation of Na, K-ATPase by Src tyrosine kinases in cortical neurons. J Neurochem. 2005;93:1515-23 pubmed
    ..These data suggest that the Na+, K+-ATPase activity in central neurons is regulated by specific Src tyrosine kinases via a protein-protein mechanism and may play a role in apoptosis. ..
  50. Tada Y, Brena R, Hackanson B, Morrison C, Otterson G, Plass C. Epigenetic modulation of tumor suppressor CCAAT/enhancer binding protein alpha activity in lung cancer. J Natl Cancer Inst. 2006;98:396-406 pubmed
    ..DNA hypermethylation of the upstream C/EBPalpha promoter region, not the core promoter region as previously reported, is critical in the regulation of C/EBPalpha expression in human lung cancer. ..
  51. Zhang H, Cui D, Wang B, Han Y, Balimane P, Yang Z, et al. Pharmacokinetic drug interactions involving 17alpha-ethinylestradiol: a new look at an old drug. Clin Pharmacokinet. 2007;46:133-57 pubmed
    ..An effort is made to relate this information to known clinical drug-drug interactions. The inhibition and induction of drug-metabolising enzymes by EE is also reviewed. ..
  52. Jin B, Tao Q, Peng J, Soo H, Wu W, Ying J, et al. DNA methyltransferase 3B (DNMT3B) mutations in ICF syndrome lead to altered epigenetic modifications and aberrant expression of genes regulating development, neurogenesis and immune function. Hum Mol Genet. 2008;17:690-709 pubmed
    ..Therefore, this study provides important new insights into the role of DNMT3B in modulating gene expression and chromatin structure and reveals new connections between DNMT3B and polycomb-mediated repression. ..
  53. Carmen J, Southard R, Sinai A. The complexity of signaling in host-pathogen interactions revealed by the Toxoplasma gondii-dependent modulation of JNK phosphorylation. Exp Cell Res. 2008;314:3724-36 pubmed publisher
    ..It further highlights the complexity of these systems and the danger of extrapolating results both within and across pathogen-host cell systems based on limited studies. ..
  54. Sobota J, Bäck N, Eipper B, Mains R. Inhibitors of the V0 subunit of the vacuolar H+-ATPase prevent segregation of lysosomal- and secretory-pathway proteins. J Cell Sci. 2009;122:3542-53 pubmed publisher
    ..shRNA-mediated knockdown of the proteolipid subunit of V(0) also caused vesiculation of immature granules. Thus, V-ATPase has a role in protein sorting in immature granules that is distinct from its role in acidification. ..
  55. Schaeffer V, Arbabi S, García I, Knoll M, Cuschieri J, Bulger E, et al. Role of the mTOR pathway in LPS-activated monocytes: influence of hypertonic saline. J Surg Res. 2011;171:769-76 pubmed publisher
    ..Meanwhile, pretreatment of PBMCs with a HTS solution suppresses mTOR activity as well as LPS-induced IL-6, suggesting a more central role for mTOR as a regulator of the immuno-inflammatory response. ..
  56. Hua Y, Zhang Y, Dolence J, Shi G, Ren J, Nair S. Cathepsin K knockout mitigates high-fat diet-induced cardiac hypertrophy and contractile dysfunction. Diabetes. 2013;62:498-509 pubmed publisher
    ..Collectively, our data indicate that cathepsin K contributes to the development of obesity-associated cardiac hypertrophy and may represent a potential target for the treatment to obesity-associated cardiac anomalies. ..
  57. Tillotson J, Kedzior M, Guimarães L, Ross A, Peters T, Ambrose A, et al. ATP-competitive, marine derived natural products that target the DEAD box helicase, eIF4A. Bioorg Med Chem Lett. 2017;27:4082-4085 pubmed publisher
    ..However, only compound 2 showed potent inhibition of helicase activity congruent with its ATPase inhibitory activity. ..
  58. Chung T, Crilly K, Anderson W, Mukherjee J, Kiss Z. ATP-dependent choline phosphate-induced mitogenesis in fibroblasts involves activation of pp70 S6 kinase and phosphatidylinositol 3'-kinase through an extracellular site. Synergistic mitogenic effects of choline phosphate and sphingosine 1-phosphate. J Biol Chem. 1997;272:3064-72 pubmed
    ..The results indicate that in the presence of extracellular ATP and/or S1P, ChoP induces mitogenesis through an extracellular site by mechanisms involving the activation of pp70 S6 kinase and, to a lesser extent, PI 3'-kinase. ..
  59. Verma R, Feldman R, Deshaies R. SIC1 is ubiquitinated in vitro by a pathway that requires CDC4, CDC34, and cyclin/CDK activities. Mol Biol Cell. 1997;8:1427-37 pubmed
    ..The complementary C-terminal segment of SIC1 binds to the S-phase cyclin CLB5, indicating a modular structure for SIC1. ..
  60. Maser R, Monsen K, Nelms B, Petrini J. hMre11 and hRad50 nuclear foci are induced during the normal cellular response to DNA double-strand breaks. Mol Cell Biol. 1997;17:6087-96 pubmed
    ..Further, these data indicate that hMre11-hRad50 foci form in response to DNA DSBs and are dependent upon a DNA damage-induced signaling pathway. ..
  61. Halliwill J, Minson C, Joyner M. Effect of systemic nitric oxide synthase inhibition on postexercise hypotension in humans. J Appl Physiol (1985). 2000;89:1830-6 pubmed
    ..g., mean arterial pressure after L-NMMA was 108.0+/-2.4 mmHg postsham vs. 102.1+/-3.3 mmHg postexercise; P<0.05). Thus it does not appear that postexercise hypotension is dependent on increased production of nitric oxide in humans...
  62. Willett K, Wassenberg D, Lienesch L, Reichert W, Di Giulio R. In vivo and in vitro inhibition of CYP1A-dependent activity in Fundulus heteroclitus by the polynuclear aromatic hydrocarbon fluoranthene. Toxicol Appl Pharmacol. 2001;177:264-71 pubmed
    ..Because FL and perhaps other inhibitory PAHs, co-occur in the environment with CYP1A inducers, CYP1A-dependent bioassays may cause an underestimation of PAH exposures. ..
  63. Ding J, Wang K, Brems J, Gamelli R. Protection against concanavalin A-induced hepatocyte apoptosis by molsidomine is time-dependent. J Am Coll Surg. 2004;198:67-77 pubmed
    ..Administration of a NO donor early after Con A injection protects the liver from injury. This is the first study demonstrating a time-dependent inhibition of liver injury induced by Con A administration. ..
  64. Borra M, Langer M, Slama J, Denu J. Substrate specificity and kinetic mechanism of the Sir2 family of NAD+-dependent histone/protein deacetylases. Biochemistry. 2004;43:9877-87 pubmed
    ..Product and dead-end inhibition analyses revealed that nicotinamide is the first product released followed by random release of OAADPr and the deacetylated product. ..
  65. Staker B, Feese M, Cushman M, Pommier Y, Zembower D, Stewart L, et al. Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex. J Med Chem. 2005;48:2336-45 pubmed
    ..These new X-ray structures explain how very different molecules can stabilize top1-DNA covalent complexes and will aid the rational design of completely novel structural classes of anticancer drugs. ..
  66. Hamza A, Abdulhameed M, Zhan C. Understanding microscopic binding of human microsomal prostaglandin E synthase-1 with substrates and inhibitors by molecular modeling and dynamics simulation. J Phys Chem B. 2008;112:7320-9 pubmed publisher
    ..The new structural insights obtained from this study should be valuable for rational design of next-generation anti-inflammatory drugs. ..
  67. Ishikawa M, Mu P, Moyer J, Wolf J, Quock R, Davies N, et al. Homeostatic synapse-driven membrane plasticity in nucleus accumbens neurons. J Neurosci. 2009;29:5820-31 pubmed publisher
    ..These results suggest that hSMP is a novel form of synapse-to-membrane homeostatic plasticity and dysregulation of hSMP may contribute to cocaine-induced cellular alterations in the NAc. ..
  68. Ou X, Lu D, Johnson C, Chen K, Youdim M, Rajkowska G, et al. Glyceraldehyde-3-phosphate dehydrogenase-monoamine oxidase B-mediated cell death-induced by ethanol is prevented by rasagiline and 1-R-aminoindan. Neurotox Res. 2009;16:148-59 pubmed publisher
  69. Borlee B, Geske G, Blackwell H, Handelsman J. Identification of synthetic inducers and inhibitors of the quorum-sensing regulator LasR in Pseudomonas aeruginosa by high-throughput screening. Appl Environ Microbiol. 2010;76:8255-8 pubmed publisher
    ..Nine compounds that inhibit and 14 compounds that induce LasR activity were identified in our high-throughput screen. ..
  70. Faralli J, Newman J, Sheibani N, Dedhar S, Peters D. Integrin-linked kinase regulates integrin signaling in human trabecular meshwork cells. Invest Ophthalmol Vis Sci. 2011;52:1684-92 pubmed publisher
    ..This study suggests that cooperative ?5?1/?4?1 integrin signaling may be regulated by ILK trans-dominantly and that alterations in ILK activity may affect actin cytoskeleton organization and contractility in the TM. ..
  71. Beane W, Morokuma J, Adams D, Levin M. A chemical genetics approach reveals H,K-ATPase-mediated membrane voltage is required for planarian head regeneration. Chem Biol. 2011;18:77-89 pubmed publisher
    ..Our data suggest well-characterized drugs (already approved for human use) might be exploited to control adult stem cell-driven pattern formation during the regeneration of complex structures...
  72. Nichols D, Leão R, Basu A, Chudayeu M, de Moraes P, Talele T, et al. Evaluation of coumarin and neoflavone derivatives as HCV NS5B polymerase inhibitors. Chem Biol Drug Des. 2013;81:607-14 pubmed publisher
    ..NS5B-TP-1-8a interaction map provided insight into 8a binding and offered clues for future SAR optimization...
  73. Zaidman N, O Grady K, Patil N, Milavetz F, Maniak P, Kita H, et al. Airway epithelial anion secretion and barrier function following exposure to fungal aeroallergens: role of oxidative stress. Am J Physiol Cell Physiol. 2017;313:C68-C79 pubmed publisher
  74. Chen H, Rojas Soto M, Oguni A, Kennedy M. A synaptic Ras-GTPase activating protein (p135 SynGAP) inhibited by CaM kinase II. Neuron. 1998;20:895-904 pubmed
    ..Inhibition of p135 SynGAP by CaMKII will stop inactivation of GTP-bound Ras and thus could result in activation of the mitogen-activated protein (MAP) kinase pathway in hippocampal neurons upon activation of NMDA receptors. ..
  75. Murphy M, Egelhoff T. Biochemical characterization of a Dictyostelium myosin II heavy-chain phosphatase that promotes filament assembly. Eur J Biochem. 1999;264:582-90 pubmed
    ..This system should provide a valuable model for studying the regulation and localization of protein phosphatase 2A in the context of cytoskeletal reorganization. ..
  76. Downs S, Ruan B, Schroepfer G. Meiosis-activating sterol and the maturation of isolated mouse oocytes. Biol Reprod. 2001;64:80-9 pubmed
    ..These results confirm the stimulatory action of FF-MAS on hypoxanthine-arrested DO but do not support a universal meiosis-inducing function for this sterol. ..
  77. Lee D, Duan H, Chang C. Androgen receptor interacts with the positive elongation factor P-TEFb and enhances the efficiency of transcriptional elongation. J Biol Chem. 2001;276:9978-84 pubmed
    ..Taken together, our reports suggest that AR interacts with TFIIH and P-TEFb and enhances the elongation stage of transcription. ..
  78. Petroski M, Deshaies R. Context of multiubiquitin chain attachment influences the rate of Sic1 degradation. Mol Cell. 2003;11:1435-44 pubmed
    ..Our results reveal that a single multiubiquitin chain can sustain a physiological turnover rate, but that chain position plays an unexpectedly significant role in the rate of proteasomal proteolysis. ..
  79. Ferrani Kile K, Randall P, Leslie S. Acute ethanol affects phosphorylation state of the NMDA receptor complex: implication of tyrosine phosphatases and protein kinase A. Brain Res Mol Brain Res. 2003;115:78-86 pubmed
    ..We conclude that ethanol has the ability to modulate phosphorylation of both NR2 and NR1 subunits and these effects appear to implicate tyrosine phosphatases and PKA, respectively. ..
  80. Hu X, Nguyen K, Verlinde C, Hol W, Pei D. Structure-based design of a macrocyclic inhibitor for peptide deformylase. J Med Chem. 2003;46:3771-4 pubmed
    ..The cyclic inhibitor showed potent inhibitory activity toward Escherichia coli deformylase (K(I) = 0.67 nM) and antibacterial activity against both Gram-positive and Gram-negative bacteria (MIC = 0.7-12 microg/mL). ..
  81. Yun B, Huang W, Leach N, Hartson S, Matts R. Novobiocin induces a distinct conformation of Hsp90 and alters Hsp90-cochaperone-client interactions. Biochemistry. 2004;43:8217-29 pubmed
    ..The unique structure and properties of novobocin-bound Hsp90 suggest that it may represent the "client-release" conformation of the Hsp90 machine. ..
  82. Domina A, Vrana J, Gregory M, Hann S, Craig R. MCL1 is phosphorylated in the PEST region and stabilized upon ERK activation in viable cells, and at additional sites with cytotoxic okadaic acid or taxol. Oncogene. 2004;23:5301-15 pubmed
  83. West D, Porter D, Saxl R, Maley F. A trojan horse approach for silencing thymidylate synthase. Biochemistry. 2004;43:9177-84 pubmed
    ..This technique, either alone or combined with other modalities, suggest a new approach to targeting cells for chemotherapy. ..
  84. Richards G, Hammer C, Garfield M, Parveen S. Characterization of a lysyl aminopeptidase activity associated with phosphoglucose isomerase of Vibrio vulnificus. Biochim Biophys Acta. 2004;1700:219-29 pubmed
    ..The finding of LysAP activity associated with heterodimeric PGI should foster a broad search for putative substrates in an effort to elucidate the role of PGI-LysAP in bacteria and its roles in the pathophysiology of diseases. ..
  85. Liu Y, Zhang S. Phosphorylation of 1-aminocyclopropane-1-carboxylic acid synthase by MPK6, a stress-responsive mitogen-activated protein kinase, induces ethylene biosynthesis in Arabidopsis. Plant Cell. 2004;16:3386-99 pubmed
    ..Equally important, this study uncovers a signaling pathway that modulates the biosynthesis of ethylene, an important plant hormone, in plants under stress. ..
  86. Reid E, Kristo G, Yoshimura Y, Ballard Croft C, Keith B, Mentzer R, et al. In vivo adenosine receptor preconditioning reduces myocardial infarct size via subcellular ERK signaling. Am J Physiol Heart Circ Physiol. 2005;288:H2253-9 pubmed
    ..These results indicate that the unique adenosine receptor agonist AMP-579 exerts its beneficial effects in vivo via both A1 and A2a receptor modulation of subcellular ERK isoform signaling. ..
  87. Won J, Im Y, Khan M, Singh A, Singh I. Involvement of phospholipase A2 and lipoxygenase in lipopolysaccharide-induced inducible nitric oxide synthase expression in glial cells. Glia. 2005;51:13-21 pubmed
    ..These results indicate a role for cPLA2 and iPLA2 in LPS-mediated iNOS gene induction in glial cells and the involvement of LO in these reactions. ..
  88. Ding B, Abe J, Wei H, Huang Q, Walsh R, Molina C, et al. Functional role of phosphodiesterase 3 in cardiomyocyte apoptosis: implication in heart failure. Circulation. 2005;111:2469-2476 pubmed publisher
    ..Drugs that maintain PDE3A function may represent an attractive therapeutic approach to treat heart failure. ..
  89. Ochsner U, Young C, Stone K, Dean F, Janjic N, Critchley I. Mode of action and biochemical characterization of REP8839, a novel inhibitor of methionyl-tRNA synthetase. Antimicrob Agents Chemother. 2005;49:4253-62 pubmed
    ..In conclusion, we demonstrate by biochemical, physiologic, and genetic mode-of-action studies that REP8839 exerts its antibacterial activity through specific inhibition of MetS, a novel target. ..
  90. Lee D, Gelein R, Opanashuk L. Heme-oxygenase-1 promotes polychlorinated biphenyl mixture aroclor 1254-induced oxidative stress and dopaminergic cell injury. Toxicol Sci. 2006;90:159-67 pubmed
    ..These observations suggest that enhanced HO-1 catalytic activity and subsequent liberation of Fe participate in neurotoxic DAergic cell injury caused by A1254 exposure in vitro. ..
  91. Ricart K, J Pearson R, Viera L, Cassina P, Kamaid A, Carroll S, et al. Interactions between beta-neuregulin and neurotrophins in motor neuron apoptosis. J Neurochem. 2006;97:222-33 pubmed
  92. Wang Q, Lu R, Zhao J, Limbird L. Arrestin serves as a molecular switch, linking endogenous alpha2-adrenergic receptor to SRC-dependent, but not SRC-independent, ERK activation. J Biol Chem. 2006;281:25948-55 pubmed