Genomes and Genes
Experts and Doctors on enzyme inhibitors in United States
Locale: United States
Topic: enzyme inhibitors
Publications269 found, 100 shown here
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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...
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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...
- 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...
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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). ..
- 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. ..
- 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
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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
- 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
- Shukla S, MacLennan G, Hartman D, Fu P, Resnick M, Gupta S. Activation of PI3K-Akt signaling pathway promotes prostate cancer cell invasion. Int J Cancer. 2007;121:1424-32 pubmed..Taken together, these results suggest that aberrant activation of PI3K-Akt pathway may contribute to increased cell invasiveness and facilitate prostate cancer progression. ..
- Jordan D, Braker J. Inhibition of the two-subsite beta-d-xylosidase from Selenomonas ruminantium by sugars: competitive, noncompetitive, double binding, and slow binding modes. Arch Biochem Biophys. 2007;465:231-46 pubmed
- Reid P, Lin S, Vanier M, Ohno Iwashita Y, Harwood H, Hickey W, et al. Partial blockage of sterol biosynthesis with a squalene synthase inhibitor in early postnatal Niemann-Pick type C npcnih null mice brains reduces neuronal cholesterol accumulation, abrogates astrogliosis, but may inhibit myelin maturation. J Neurosci Methods. 2008;168:15-25 pubmed..The methods described in the current work have general applicability for lipid metabolism studies in mice brains in various pathophysiological conditions. ..
- Zhang T, Hamza A, Cao X, Wang B, Yu S, Zhan C, et al. A novel Hsp90 inhibitor to disrupt Hsp90/Cdc37 complex against pancreatic cancer cells. Mol Cancer Ther. 2008;7:162-70 pubmed publisher..The data suggest that celastrol is a novel Hsp90 inhibitor to disrupt Hsp90-Cdc37 interaction against pancreatic cancer cells. ..
- Xie X, Mhaskar Y, Arbogast L, Trammell R, Hughes L, Toth L. Adenosine receptor antagonists and behavioral activation in NF-kappaB p50 subunit knockout mice. Life Sci. 2009;85:226-34 pubmed publisher..These findings support the conclusions that 1) A2AAR has a major impact on behavioral activation of p50 KO mice, and 2) D2R mediated neurotransmission is important to this effect. ..
- Ngoh G, Hamid T, Prabhu S, Jones S. O-GlcNAc signaling attenuates ER stress-induced cardiomyocyte death. Am J Physiol Heart Circ Physiol. 2009;297:H1711-9 pubmed publisher..These results provide new insights into a possible interaction between O-GlcNAc signaling and ER stress and may partially explain a mechanism of O-GlcNAc-mediated cardioprotection. ..
- Mulabagal V, Calderón A. Development of an ultrafiltration-liquid chromatography/mass spectrometry (UF-LC/MS) based ligand-binding assay and an LC/MS based functional assay for Mycobacterium tuberculosis shikimate kinase. Anal Chem. 2010;82:3616-21 pubmed publisher..95 microg/mL (9.75 ng on-column). This is the first application of UF-LC/MS and LC/MS in the development of ligand-binding and functional assays, respectively as a useful approach to screen MtSK inhibitors. ..
- Goel M, Schilling W. Role of TRPC3 channels in ATP-induced Ca2+ signaling in principal cells of the inner medullary collecting duct. Am J Physiol Renal Physiol. 2010;299:F225-33 pubmed publisher..Only activation of TRPC3 leads to net transepithelial apical-to-basolateral Ca(2+) flux. Furthermore, these results demonstrate that native TRPC3 is not a store-operated channel in IMCD-3 cells. ..
- Niederlechner S, Baird C, Petrie B, Wischmeyer E, Wischmeyer P. Epidermal growth factor receptor expression and signaling are essential in glutamine's cytoprotective mechanism in heat-stressed intestinal epithelial-6 cells. Am J Physiol Gastrointest Liver Physiol. 2013;304:G543-52 pubmed publisher..GLN-mediated EGFR signaling activated ERK1/2 and decreased p38MAPK signaling. However, GLN-mediated Akt phosphorylation after HS seems to be independent of EGFR signaling. ..
- Guo L, Kozlosky C, Ericsson L, Daniel T, Cerretti D, Johnson R. Studies of ligand-induced site-specific phosphorylation of epidermal growth factor receptor. J Am Soc Mass Spectrom. 2003;14:1022-31 pubmed..Pretreatment of A431 cells with a small molecule EGFR inhibitor nearly eliminated the ligand-induced phosphorylation on all of the sites except for Y992 and Y1068. ..
- Holden W, Wilkins J, Harris M, Milczuk H, Giraud G. Temperature conditioning of nasal air: effects of vasoactive agents and involvement of nitric oxide. J Appl Physiol (1985). 1999;87:1260-5 pubmed..7 +/- 14.2 to 44.2 +/- 23.7 nl. min(-1). m(-2); P < 0.01). The results suggest that vascular tone and/or flow modulates temperature conditioning and that NO may participate in that function...
- Horvath R, DeLeo J. Morphine enhances microglial migration through modulation of P2X4 receptor signaling. J Neurosci. 2009;29:998-1005 pubmed publisher..These data provide the first necessary step in supporting microglial migration as an attractive target for the prevention or attenuation of morphine-induced side effects including tolerance and hyperalgesia. ..
- Deng X, Ewton D, Pawlikowski B, Maimone M, Friedman E. Mirk/dyrk1B is a Rho-induced kinase active in skeletal muscle differentiation. J Biol Chem. 2003;278:41347-54 pubmed..Other members of the dyrk/minibrain/HIPK family of kinases in lower organisms have been shown to regulate the transition from growth to differentiation, and Mirk is now shown to participate in skeletal muscle development. ..
- Li H, Mittal A, Makonchuk D, Bhatnagar S, Kumar A. Matrix metalloproteinase-9 inhibition ameliorates pathogenesis and improves skeletal muscle regeneration in muscular dystrophy. Hum Mol Genet. 2009;18:2584-98 pubmed publisher..Collectively, our study suggests that the increased production of MMP-9 exacerbates dystrophinopathy and MMP-9 represents as one of the most promising therapeutic targets for the prevention of disease progression in DMD...
- Gille A, Seifert R. 2'(3')-O-(N-methylanthraniloyl)-substituted GTP analogs: a novel class of potent competitive adenylyl cyclase inhibitors. J Biol Chem. 2003;278:12672-9 pubmed..Instead, MANT-GTP gamma S/MANT-GppNHp constitute a novel class of potent competitive AC inhibitors. ..
- Hu H, Horton J, Gryk M, Prasad R, Naron J, Sun D, et al. Identification of small molecule synthetic inhibitors of DNA polymerase beta by NMR chemical shift mapping. J Biol Chem. 2004;279:39736-44 pubmed..Our results illustrate that NMR-based mapping techniques can be used in the design of small molecule enzyme inhibitors including those with potential use in a clinical setting. ..
- Lin D, Takemoto D. Oxidative activation of protein kinase Cgamma through the C1 domain. Effects on gap junctions. J Biol Chem. 2005;280:13682-93 pubmed..Results suggested that H2O2 caused oxidation of the C1 domain, activation of the PKCgamma, and inhibition of gap junctions. This inhibition of gap junctions could provide a protection to cells against oxidative stress. ..
- Bayard M, Farrow J, Tudiver F. Acute methemoglobinemia after endoscopy. J Am Board Fam Pract. 2004;17:227-9 pubmed
- Richards N, Kilberg M. Asparagine synthetase chemotherapy. Annu Rev Biochem. 2006;75:629-54 pubmed..In addition, the first successful, mechanism-based efforts to prepare and characterize nanomolar ASNS inhibitors are discussed, together with the implications of these studies for future efforts to develop useful drugs. ..
- Fleseriu M, Pivonello R, Young J, Hamrahian A, Molitch M, Shimizu C, et al. Osilodrostat, a potent oral 11Î²-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease. Pituitary. 2016;19:138-48 pubmed publisher..Osilodrostat treatment reduced UFC in all patients; 78.9% (n/N = 15/19) had normal UFC at week 22. Treatment with osilodrostat was generally well tolerated. ..
- Westphal R, Tavalin S, Lin J, Alto N, Fraser I, Langeberg L, et al. Regulation of NMDA receptors by an associated phosphatase-kinase signaling complex. Science. 1999;285:93-6 pubmed..Hence, yotiao is a scaffold protein that physically attaches PP1 and PKA to NMDA receptors to regulate channel activity. ..
- Choi Y, Nash K, Byrne B, Muzyczka N, Song S. The effect of DNA-dependent protein kinase on adeno-associated virus replication. PLoS ONE. 2010;5:e15073 pubmed publisher..Finally, we showed that AAV-ITRs directly interacted with Ku proteins. Collectively, our results showed that that DNA-PK enhances rAAV replication through the interaction of Ku proteins and AAV-ITRs. ..
- Lou D, Griffith N, Noonan D. The tuberous sclerosis 2 gene product can localize to nuclei in a phosphorylation-dependent manner. Mol Cell Biol Res Commun. 2001;4:374-80 pubmed..Here we provide evidence for TSC2 translocation to the nucleus and a possible role for phosphorylation in both TSC2 translocation and TSC2 modulation of steroid receptor-mediated transcription. ..
- Grunewald G, Seim M, Regier R, Criscione K. Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors. Bioorg Med Chem. 2007;15:1298-310 pubmed..22mM), which has a lipophilic 7-substituent that cannot hydrogen bond to the enzyme, is twice as potent at PNMT than 11. This once again illustrates the limitations of docking studies for lead optimization. ..
- Sargeant A, Klein R, Rengel R, Clinton S, Kulp S, Kashida Y, et al. Chemopreventive and bioenergetic signaling effects of PDK1/Akt pathway inhibition in a transgenic mouse model of prostate cancer. Toxicol Pathol. 2007;35:549-61 pubmed..We conclude that targeting of the PDK1/Akt pathway has chemopreventive relevance in prostate cancer and causes other in vivo effects mediated in part by an alteration of bioenergetic signaling. ..
- Godeny M, Sayeski P. ERK1/2 regulates ANG II-dependent cell proliferation via cytoplasmic activation of RSK2 and nuclear activation of elk1. Am J Physiol Cell Physiol. 2006;291:C1308-17 pubmed
- Nelin L, Chicoine L, Reber K, English B, Young T, Liu Y. Cytokine-induced endothelial arginase expression is dependent on epidermal growth factor receptor. Am J Respir Cell Mol Biol. 2005;33:394-401 pubmed..We speculate that EGFR inhibitors may attenuate vascular remodeling without affecting NO release, and thus may represent novel therapeutic modalities for pulmonary hypertensive disorders. ..
- Gao N, Hu H, Liu S, Gao C, Xia Y, Wood J. Stimulation of adenosine A1 and A2A receptors by AMP in the submucosal plexus of guinea pig small intestine. Am J Physiol Gastrointest Liver Physiol. 2007;292:G492-500 pubmed
- Noel J, Fernandez de Castro J, DeMarco P, Franco L, Wang W, Vukmanic E, et al. Iodoacetic acid, but not sodium iodate, creates an inducible swine model of photoreceptor damage. Exp Eye Res. 2012;97:137-47 pubmed publisher..Because of these attributes this large animal model of controlled photoreceptor damage should be useful in the investigation of treatments to replace damaged photoreceptors...
- Tian G, Paschetto K, Gharahdaghi F, Gordon E, Wilkins D, Luo X, et al. Mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles: long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency. Biochemistry. 2011;50:6867-78 pubmed publisher..The long residence time displayed by 1 does not appear to derive exclusively from great thermodynamic potency and is consistent with an increased kinetic energy barrier that prevents dissociation from happening quickly. ..
- King M, Coker M, Goldberg A, McElmurray J, Gunasinghe H, Mukherjee R, et al. Selective matrix metalloproteinase inhibition with developing heart failure: effects on left ventricular function and structure. Circ Res. 2003;92:177-85 pubmed..These results suggest that targeting a selective portfolio of myocardial MMP species for inhibition may provide a more rational therapeutic strategy in the setting of congestive heart failure. ..
- Antonov A, Antonova G, Munn D, MIVECHI N, Lucas R, Catravas J, et al. ?V?3 integrin regulates macrophage inflammatory responses via PI3 kinase/Akt-dependent NF-?B activation. J Cell Physiol. 2011;226:469-76 pubmed publisher..We hypothesize that ?V?3 activation can maintain chronic inflammatory processes in pathological conditions and that the loss of ?V?3 ligation will allow macrophages to escape from the inflammatory state. ..
- Hasan N, Longacre M, Stoker S, Kendrick M, Druckenbrod N, Laychock S, et al. Sphingosine kinase 1 knockdown reduces insulin synthesis and secretion in a rat insulinoma cell line. Arch Biochem Biophys. 2012;518:23-30 pubmed publisher..The results indicate that SphK1 activity is important for insulin synthesis and secretion. ..
- Zhu D, Xiong W, Mei L. Lipid rafts serve as a signaling platform for nicotinic acetylcholine receptor clustering. J Neurosci. 2006;26:4841-51 pubmed..These results provide insight into mechanisms of AChR cluster formation. ..
- Waterborg J, Kapros T. Kinetic analysis of histone acetylation turnover and Trichostatin A induced hyper- and hypoacetylation in alfalfa. Biochem Cell Biol. 2002;80:279-93 pubmed..Thus, application of TSA to change gene expression in vivo in plants may have unexpected consequences. ..
- Lin H, Liu C, Cao D, Chen P, Chen M, Lin S, et al. Endogenous methyl palmitate modulates nicotinic receptor-mediated transmission in the superior cervical ganglion. Proc Natl Acad Sci U S A. 2008;105:19526-31 pubmed publisher..Endogenous PAME appears to play a role in modulation of the autonomic ganglionic transmission and to complement the vasodilator effect of NO. ..
- Dai M, Yang Y, Shi X. Lactate dilates cochlear capillaries via type V fibrocyte-vessel coupling signaled by nNOS. Am J Physiol Heart Circ Physiol. 2011;301:H1248-54 pubmed publisher..The data suggest that type V fibrocytes are the source of the lactate-induced NO. Cochlear microvessel tone, regulated by lactate, is mediated by an NO-signaled coupling of fibrocytes and capillaries. ..
- Han Q, Pabba P, Barbosa J, Mabon R, Healy J, Gardyan M, et al. 4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase. Bioorg Med Chem Lett. 2016;26:1184-7 pubmed publisher..We developed SAR on three series based on carbon, oxygen and sulfur replacement of the 5-position. In each series, highly potent Notum Pectinacetylesterase inhibitors were identified. ..
- 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. ..
- 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. ..
- 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. ..
- 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. ..
- 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...
- 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...
- 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. ..
- 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. ..
- 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...
- 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. ..
- 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. ..
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