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Journal articles on the topic '4. PKA'

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Published: 4 June 2021

Last updated: 11 February 2022

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1

Wodzinski, Stefan, and John W. Bunting. "The acidities of 4-arylsulfonylmethylpyridines and N-methyl and N-benzyl 4-arylsulfonylmethylpyridinium cations in aqueous solution." Canadian Journal of Chemistry 70, no. 10 (1992): 2635–44. http://dx.doi.org/10.1139/v92-332.

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The pKa values for the deprotonation of a series of 4-(X-phenylsulfonylmethyl)pyridines (6) (pKa = 19.89 (X = H); ρ = 3.0) were determined in aqueous dimethyl sulfoxide solutions at 25 °C using the H0q acidity function. The pKa values were also measured for the corresponding series of N-mefhyl 4-(X-phenylsulfonylmethyl)pyridinium cations (2) (pKa = 11.27 (X = H); ρ = 1.45) and also for a series of N-(X-benzyl) 4-phenylsulfonylmethylpyridinium cations (7) (pKa = 10.70 (X = H); ρ = 0.65) in aqueous solution (ionic strength 0.1 at 25 °C). Comparison of the substituent effects upon the pKa values

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2

Verbic, Tatjana, Branko Drakulic, Mire Zloh, Jovana Pecelj, Gordana Popovic, and Ivan Juranic. "An LFER study of the protolytic equilibria of 4-aryl-2,4-dioxobutanoic acids in aqueous solutions." Journal of the Serbian Chemical Society 72, no. 12 (2007): 1201–16. http://dx.doi.org/10.2298/jsc0712201v.

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The protolytic equilibria of 13 4-aryl-2,4-dioxobutanoic acids (ADKs) were spectrophotometrically studied in aqueous solutions in the pH range 1-9 at 25?1 ?C and an ionic strength of 0.1 mol l-1 (NaCl), with the exception of the 4-OH-derivative which was also potentiometrically studied in the pH range 7-10 at 25?1 ?C and an ionic strength of 0.1 mol l-1 (NaCl). In solution, the compounds simultaneously exist in one diketo and two enolic forms; therefore, the determined acidity constants (pKa1 1.87-2.29, pKa2 6.63-8.13 and pKa3(4-OH-) 9.52) represent system macro constants. The 1H-NMR spectrum

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3

Kiliç, Hasan, and Er Birol. "Potentiometric investigation of acid-base equilibria of two new pyrimidine derivatives in various methanol-water media." Journal of the Serbian Chemical Society 71, no. 1 (2006): 43–54. http://dx.doi.org/10.2298/jsc0601043k.

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The acid-base properties of 1-amino-5-benzoyl-4-phenyl-1H-pyrimidine-2-one (L1) and 1-amino-5-benzoyl-4-phenyl-1H-pyrimidine-2-thione (L2) were investigated potentiometrically at an ionic strength of 0.10M(LiCl) in 19.8, 33.6 and 55.9 % (v/v) methanol-water mixtures at 25.0 ? 0.1 ?C. The apparent dissociation constants (psKa) were calculated for the di-protonated form (L1H2+2 and L2H2+2) of pyrimidine bases, using a software package TITFIT, which were then extrapolated to pure water to derive the dissociation constants in aqueous solution (pKa). The aqueous pKa constants were found to be: L1,

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4

Gurumurthy, Sushma, Anindya Goswami, Krishna Murthi Vasudevan, and Vivek M. Rangnekar. "Phosphorylation of Par-4 by Protein Kinase A Is Critical for Apoptosis." Molecular and Cellular Biology 25, no. 3 (2005): 1146–61. http://dx.doi.org/10.1128/mcb.25.3.1146-1161.2005.

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ABSTRACT Despite distinct dissimilarities, diverse cancers express several common protumorigenic traits. We present here evidence that the proapoptotic protein Par-4 utilizes one such common tumorigenic trait to become selectively activated and induce apoptosis in cancer cells. Elevated protein kinase A (PKA) activity noted in cancer cells activated the apoptotic function of ectopic Par-4 or its SAC (selective for apoptosis induction in cancer cells) domain, which induces apoptosis selectively in cancer cells and not in normal or immortalized cells. PKA preferentially phosphorylated Par-4 at t

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5

Farrell, JR, and P. Mctigue. "The Basicity of 2,6-Dimethyl-4-pyrone." Australian Journal of Chemistry 38, no. 6 (1985): 985. http://dx.doi.org/10.1071/ch9850985.

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Conductimetric and spectrophotometric measurements of the Ka of protonated 2,6-dimethyl-4-pyrone have been made. The conductimetrically determined value of pKa = 0.17�0.03 was 0.2 pK units higher than the value of pKa = -0.02�0.05 found spectrophotometrically . The spectrophotometric studies in concentrated sulfuric and hydrochloric acids revealed that, at low acid concentrations, the pyrone had an excess acidity slope parameter (m‡) of -0.29. However, over a large acid concentration range, m‡ was observed to vary in a way that caused moderate systematic errors in the excess acidity extrapolat

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6

Nirula, Ajay, Mary Ho, Hyewon Phee, Jeroen Roose, and Arthur Weiss. "Phosphoinositide-dependent kinase 1 targets protein kinase A in a pathway that regulates interleukin 4." Journal of Experimental Medicine 203, no. 7 (2006): 1733–44. http://dx.doi.org/10.1084/jem.20051715.

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CD28 plays a critical role in T cell immune responses. Although the kinase Akt has been shown to act downstream of CD28 in T helper (Th)1 cytokine induction, it does not induce Th2 cytokines such as interleukin 4 (IL-4). We recently reported that phosphoinositide-dependent kinase 1 (PDK1) partially corrects the defect in IL-4 production present in CD28-deficient T cells, suggesting that PDK1 regulates IL-4 independently of Akt. We now describe a signaling pathway in which PDK1 targets IL-4 in the murine Th2 cell line D10. PDK1-mediated activation of this pathway is dependent on protein kinase

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7

Pfendt, L., G. Popovic, M. Kostic, Lj Stevovic, B. Drakulic, and I. Juranic. "Determination and structural correlation of the pKa values of p-substituted trans-2,3-epoxy-4-oxo-4-phenylbutanoic acids." Journal of the Serbian Chemical Society 65, no. 11 (2000): 781–88. http://dx.doi.org/10.2298/jsc0011781p.

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The pKa values for a series of eight p-substituted trans-2,3-epoxy-4-phenyl butanoic acids (p-substituted trans-b-aroylepoxyacrylic acids) have been determined potentiometrically in aqueous media at 25?C at an ionic strength of 0.1 mol/dm3 (NaCl). The transmission of polar effects from the substituents on the phenyl nucleus to the carboxylic group through the side chain involving a carbonyl group and an epoxide ring was investigated. The pKa values were correlated with structure using the Hammett, Taft and Yukawa-Tsuno approaches. The Hammett r constant (0.34) was compared with analogue values

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8

Carraro-Lacroix, Luciene R., Gerhard Malnic, and Adriana C. C. Girardi. "Regulation of Na+/H+ exchanger NHE3 by glucagon-like peptide 1 receptor agonist exendin-4 in renal proximal tubule cells." American Journal of Physiology-Renal Physiology 297, no. 6 (2009): F1647—F1655. http://dx.doi.org/10.1152/ajprenal.00082.2009.

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The gut incretin hormone glucagon-like peptide 1 (GLP-1) is released in response to ingested nutrients and enhances insulin secretion. In addition to its insulinotropic properties, GLP-1 has been shown to have natriuretic actions paralleled by a diminished proton secretion. We therefore studied the role of the GLP-1 receptor agonist exendin-4 in modulating the activity of Na+/H+ exchanger NHE3 in LLC-PK1 cells. We found that NHE3-mediated Na+-dependent intracellular pH (pHi) recovery decreased ∼50% after 30-min treatment with 1 nM exendin-4. Pharmacological inhibitors and cAMP analogs that sel

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9

Mikeš, František, Jiří Labský, Drahomír Výprachtický, and Jiří Chalabala. "Microenvironment of polymer chains in solution: pKa of indicators bound to the polymer chain." Collection of Czechoslovak Chemical Communications 55, no. 9 (1990): 2226–32. http://dx.doi.org/10.1135/cccc19902226.

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Polymers bearing at the end of side chains acidobasic indicator moieties exhibiting a solvatochromic absorption band were prepared by a polymeranalogous reaction of copolymers N-(2-hydroxy propyl) methacrylamide-N-methacryloylated 4-nitrophenyl ester ω-aminoacids with 1-(2-aminoethyl)-4-(4-hydroxystyryl)pyridinium bromide. It was found that pKa of reporters bound at a medium long side chain (six methylene groups) is close to pKa of a low-molecular model compound, while pKa of a reporter bound close to the polymer backbone is approximately by one pKa unit higher. Changes in the pKa value of the

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10

Katsura, T., C. E. Gustafson, D. A. Ausiello, and D. Brown. "Protein kinase A phosphorylation is involved in regulated exocytosis of aquaporin-2 in transfected LLC-PK1 cells." American Journal of Physiology-Renal Physiology 272, no. 6 (1997): F816—F822. http://dx.doi.org/10.1152/ajprenal.1997.272.6.f816.

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Vasopressin-dependent translocation of aquaporin-2 (AQP2) between intracellular vesicles and the plasma membrane has been demonstrated in vivo and in vitro. Furthermore, the vasopressin-induced increase in apical membrane water permeability of renal principal cells is dependent on a rise in intracellular adenosine 3',5'-cyclic monophosphate and activation of protein kinase A (PKA). To determine whether trafficking of AQP2 is dependent on PKA phosphorylation, we first examined the effect of the PKA-inhibitor N-(2[[3-(4-bromophenyl)-2-propenyl]-amino]-ethyl)-5-isoquinolinesulfonam ide (H-89) on

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11

Cheng, Chen, Yulin Chen, Yue Cao, Yongmin Ma, and Robert C. Hider. "Synthesis and characterization of methyl substituted 3-hydroxypyridin-4-ones and their complexes with iron(III)." Canadian Journal of Chemistry 96, no. 3 (2018): 293–98. http://dx.doi.org/10.1139/cjc-2017-0545.

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Methyl substituted 3-hydroxypyridin-4(1H)-ones have been synthesized. The pKa values and Fe3+ affinity constants of these ligands were studied. The introduction of an electron-donating methyl group at a different position of pyridinone ring markedly influences the pKa values of 3-hydroxy and 4-oxo groups. The pFe3+ values were also affected and are in the range of 17.6–20.7. The findings can be used to guide a design of 3-hydroxypyridin-4-ones with desirable pKa and pFe3+ values.

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12

Konçe, İlkay, Ebru Çubuk Demiralay, and Hülya Yılmaz Ortak. "Chromatographic Determination of Thermodynamic Acid Dissociation Constants of Tetracycline Antibiotics and Their Epimers." Journal of Chromatographic Science 57, no. 8 (2019): 745–50. http://dx.doi.org/10.1093/chromsci/bmz051.

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Abstract The presented study describes the development of reversed-phase liquid chromatography method using a core-shell particle column with a pentafluorophenyl stationary phase for the dissociation constant (pKa) determination of the tetracycline group antibiotics (tetracycline, oxytetracycline, chlortetracycline) and their epimers (4-epitetracycline, 4-epioxytetracycline, 4-epichlortetracycline). The pH values were measured in the acetonitrile (ACN)–water binary mixtures, used as mobile phases, instead of in water and take into account the effect of the activity coefficients. Thermodynamic

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13

Polášek, Miroslav, Karel Waisser та Tomáš Bouček. "Determination of the substituent constant σp- for the thioamide group -CSNH2 from the ionization of anilines and phenols". Collection of Czechoslovak Chemical Communications 56, № 12 (1991): 2964–68. http://dx.doi.org/10.1135/cccc19912964.

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Thermodynamic ionization constants pKa 2.62 ± 0.01 for the primary aromatic amino group of 4-aminothiobenzamide and pKa 8.28 ± 0.01 for the phenolic hydroxy group of 4-hydroxythiobenzamide have been determined by ultra-violet spectrophotometry at 25°C. By using these pKa values and the Hammett equations (log Ka vs σ) for the ionization of fourteen 3- or 4-substituted phenols and thirteen 3- or 4-substituted anilines the substituent constant σp- = 0.68 (from the ionization of anilines) or σp- = 0.73 (from the ionization of phenols) of the thioamide group -CSNH2 was calculated.

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14

Muthu Vijayan Enoch, Israel V., та Meenakshisundaram Swaminathan. "Spectral and Photoprototropic Characteristics of 4-Aminobiphenyl in β-Cyclodextrin". Collection of Czechoslovak Chemical Communications 69, № 4 (2004): 748–58. http://dx.doi.org/10.1135/cccc20040748.

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The photophysical and photoprototropic behaviour of 4-aminobiphenyl (4ABP) in aqueous β-cyclodextrin (β-CDx) solution has been investigated using steady-state and time-resolved fluorescence spectroscopy. Fluorescence of the neutral form of 4ABP is enhanced due to the formation of a 1:1 complex with β-CDx. The formation of this complex has been confirmed by time-resolved spectroscopy. In the presence of β-CDx, no change was observed in the ground state pKa value but the excited state pKa value changed. Based on its photophysical and photoprototropic characteristics in β-CDx, the structure of th

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15

Viollet, B., A. Kahn, and M. Raymondjean. "Protein kinase A-dependent phosphorylation modulates DNA-binding activity of hepatocyte nuclear factor 4." Molecular and Cellular Biology 17, no. 8 (1997): 4208–19. http://dx.doi.org/10.1128/mcb.17.8.4208.

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Hepatocyte nuclear factor 4 (HNF4), a liver-enriched transcription factor of the nuclear receptor superfamily, is critical for development and liver-specific gene expression. Here, we demonstrate that its DNA-binding activity is modulated posttranslationally by phosphorylation in vivo, ex vivo, and in vitro. In vivo, HNF4 DNA-binding activity is reduced by fasting and by inducers of intracellular cyclic AMP (cAMP) accumulation. A consensus protein kinase A (PKA) phosphorylation site located within the A box of its DNA-binding domain has been identified, and its role in phosphorylation-dependen

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16

Liu, Xiangdong, Quynh-Thu Wall, Lynn Taylor та Norman P. Curthoys. "C/EBPβ contributes to cAMP-activated transcription of phosphoenolpyruvate carboxykinase in LLC-PK1-F+ cells". American Journal of Physiology-Renal Physiology 281, № 4 (2001): F649—F657. http://dx.doi.org/10.1152/ajprenal.2001.281.4.f649.

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Phospho enolpyruvate carboxykinase (PEPCK) is a key regulatory enzyme in renal gluconeogenesis. Activation of various PEPCK−2300Luc reporter constructs in LLC-PK1-F+ cells, a gluconeogenic line of porcine renal proximal tubule-like cells, by protein kinase A (PKA) is mediated, in part, through the cAMP-response element (CRE)-1 of the PEPCK promoter. Incubation of a CRE-1 containing oligonucleotide with nuclear extracts from LLC-PK1-F+ cells produced multiple bands, all of which were blocked by antibodies that are specific for C/EBPβ but not for C/EBPα or C/EBPδ. Treatment of cells with cAMP di

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17

London, Edra, Maria Nesterova, and Constantine A. Stratakis. "Acute vs chronic exposure to high fat diet leads to distinct regulation of PKA." Journal of Molecular Endocrinology 59, no. 1 (2017): 1–12. http://dx.doi.org/10.1530/jme-16-0188.

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The cAMP-dependent protein kinase (PKA) is an essential regulator of lipid and glucose metabolism that plays a critical role in energy homeostasis. The impact of diet on PKA signaling has not been defined, although perturbations in individual PKA subunits are associated with changes in adiposity, physical activity and energy intake in mice and humans. We hypothesized that a high fat diet (HFD) would elicit peripheral and central alterations in the PKA system that would differ depending on length of exposure to HFD; these differences could protect against or promote diet-induced obesity (DIO).

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18

Schubert, R., V. N. Serebryakov, H. Engel, and H. H. Hopp. "Iloprost activates KCa channels of vascular smooth muscle cells: role of cAMP-dependent protein kinase." American Journal of Physiology-Cell Physiology 271, no. 4 (1996): C1203—C1211. http://dx.doi.org/10.1152/ajpcell.1996.271.4.c1203.

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The patch-clamp technique was used to investigate the effect of iloprost on activity of calcium-activated potassium (KCa) channels of freshly isolated rat tail artery smooth muscle cells. In the whole cell configuration, outward current, determined largely by KCa channels, was enhanced 1.73 +/- 0.11-fold by 5 x 10(-7) M iloprost, 1.80 +/- 0.12-fold by 10(-4) M 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole-3', 5'-cyclic monophosphothioate (Sp-5,6-DCl-cBIMPS), a specific activator of adenosine 3',5'-cyclic monophosphate (cAMP)-dependent protein kinase (PKA), and 2.78 +/- 0.95-fold by 10 U/ml

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19

Singh, Saranjit, Nishi Sharda, and Lalit Mahajan. "Spectrophotometric determination of pKa of nimesulide." International Journal of Pharmaceutics 176, no. 2 (1999): 261–64. http://dx.doi.org/10.1016/s0378-5173(98)00304-4.

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20

McKinney, Leslie C., Sumitra Chakraverty, and Paul De Weer. "Purification, solubility, and pKa of veratridine." Analytical Biochemistry 153, no. 1 (1986): 33–38. http://dx.doi.org/10.1016/0003-2697(86)90056-4.

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21

Hallé, Jean-Claude, Pascale Soulié, Marie-José Pouet, and Malika Mokhtari. "Évaluation de l'effet électroattracteur du motif 4-nitrobenzofurazanyle : ionisation de 7-anilino 4-nitrobenzofurazanes." Canadian Journal of Chemistry 75, no. 9 (1997): 1240–47. http://dx.doi.org/10.1139/v97-150.

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The ionization of a series of 7-(4′-X anilino) 4-nitrobenzofurazans (4H) (X = NO2, CN, CO2Me, F, H, Me, OMe) to give the conjugate amide anions 4− has been studied by 1H and 13C NMR in Me2SO-d6. Concomitantly, their acidity (pKa) has been measured spectrophotometrically in a H2O–Me2SO mixture with a molar fraction [Formula: see text] Although the measured pKa values for the whole series of compounds 4H lie in a relatively narrow range (6.40, X = NO2/7.98, X = OMe), they reveal that each derivative is about 3 times more acidic than the similarly X-substituted 2,4,6-trinitrodiphenylamines. These

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22

Bunting, John W., and P. Philippe Aubin. "Thermodynamic and kinetic acidities of N-(substituted benzyl) 4-phenylacetylpyridinium cations in aqueous solution." Canadian Journal of Chemistry 69, no. 6 (1991): 945–48. http://dx.doi.org/10.1139/v91-140.

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The pKa values for the deprotonation of a series of eight 1-(X-benzyl)-4-phenylacetylpyridinium cations (6) have been measured in aqueous solutions of ionic strength 0.1 at 25 °C: pKa = −0.18σ + 8.91. The pseudo-first-order rate constants for deprotonation of these carbon acids have been measured over the range pH = 11–13, and have been found to display kinetic saturation effects that are consistent with the addition of hydroxide ion to the carbonyl group (pKz) as the product of kinetic control upon basification of neutral aqueous solutions of these pyridinium cations, with the subsequent tran

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23

Chen, Yu-Lin, Dave J. Barlow, Xiao-Le Kong, Yong-Min Ma, and Robert C. Hider. "Prediction of 3-hydroxypyridin-4-one (HPO) hydroxyl pKa values." Dalton Transactions 41, no. 21 (2012): 6549. http://dx.doi.org/10.1039/c2dt12396g.

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24

Lewendon, A., and W. V. Shaw. "The pKa of the catalytic histidine residue of chloramphenicol acetyltransferase." Biochemical Journal 290, no. 1 (1993): 15–19. http://dx.doi.org/10.1042/bj2900015.

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A catalytically essential histidine residue (His-195) of chloramphenicol acetyltransferase (CAT) acts as a general base in catalysis, abstracting a proton from the primary hydroxy group of chloramphenicol. The pKa of His-195 has been determined from the pH-dependence of chemical modification. Both methyl 4-nitrobenzenesulphonate and iodoacetamide inactivate CAT by irreversible modification of His-195. The kinetics of inactivation by methyl 4-nitrobenzenesulphonate are pseudo-first-order, and the pH-dependence of inactivation yields a pKa value of 6.60. Iodoacetamide inactivation proceeds with

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25

Houslay, M. D., and G. S. Baillie. "Phosphodiesterase-4 gates the ability of protein kinase A to phosphorylate G-protein receptor kinase-2 and influence its translocation." Biochemical Society Transactions 34, no. 4 (2006): 474–75. http://dx.doi.org/10.1042/bst0340474.

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Challenge of the β2Ar (β2-adrenergic receptor) with isoprenaline in HEK-293β2 cells (human embryonic kidney cells stably overexpressing a FLAG- and green fluorescent protein-tagged β2Ar) results in the PKA (cAMP-dependent protein kinase) phosphorylation of GRK2 (G-protein receptor kinase-2). This response was enhanced when PDE4 (phosphodiesterase-4) activity was attenuated using either rolipram, a PDE4-selective inhibitor, or with siRNA (small interfering RNA) knockdown of both PDE4B and PDE4D. Rolipram also facilitated GRK2 recruitment to the membrane and phosphorylation of the β2Ar by GRK2 i

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26

Du, Min, Robert L. S. Perry, Nathaniel B. Nowacki, et al. "Protein Kinase A Represses Skeletal Myogenesis by Targeting Myocyte Enhancer Factor 2D." Molecular and Cellular Biology 28, no. 9 (2008): 2952–70. http://dx.doi.org/10.1128/mcb.00248-08.

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ABSTRACT Activation of protein kinase A (PKA) by elevation of the intracellular cyclic AMP (cAMP) level inhibits skeletal myogenesis. Previously, an indirect modulation of the myogenic regulatory factors (MRFs) was implicated as the mechanism. Because myocyte enhancer factor 2 (MEF2) proteins are key regulators of myogenesis and obligatory partners for the MRFs, here we assessed whether these proteins could be involved in PKA-mediated myogenic repression. Initially, in silico analysis revealed several consensus PKA phosphoacceptor sites on MEF2, and subsequent analysis by in vitro kinase assay

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27

Peng, Hsien-Yu, Chao-Hsiang Chang, Shin-Jei Tsai та ін. "Protein Kinase A–dependent Spinal α-Amino-3-hydroxy-5-methyl-4-isoxazoleproprionate–receptor Trafficking Mediates Capsaicin-induced Colon-Urethra Cross-organ Reflex Sensitization". Anesthesiology 114, № 1 (2011): 70–83. http://dx.doi.org/10.1097/aln.0b013e3181fe4204.

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Background Intracellular redistribution of α-amino-3-hydroxy-5-methyl-4-isoxazoleproprionate receptors (AMPARs) is known to be induced by natural painful stimulation. We tested the hypothesis that that protein kinase A (PKA)-dependent AMPAR trafficking underlies the development of N-methyl-d-aspartate receptor-mediated cross-organ sensitization in vivo. Methods We recorded urethra reflex activity and analyzed immunoblotting of lumbosacral (L6-S2) dorsal horn (DH) tissue obtained from animal preparations after intrathecal 8-bromo-cyclic adenosine monophosphate injection or intracolonic instilla

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28

Chen, Y., J. R. Cardinaux, R. H. Goodman, and S. M. Smolik. "Mutants of cubitus interruptus that are independent of PKA regulation are independent of hedgehog signaling." Development 126, no. 16 (1999): 3607–16. http://dx.doi.org/10.1242/dev.126.16.3607.

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Hedgehog (HH) is an important morphogen involved in pattern formation during Drosophila embryogenesis and disc development. cubitus interruptus (ci) encodes a transcription factor responsible for transducing the hh signal in the nucleus and activating hh target gene expression. Previous studies have shown that CI exists in two forms: a 75 kDa proteolytic repressor form and a 155 kDa activator form. The ratio of these forms, which is regulated positively by hh signaling and negatively by PKA activity, determines the on/off status of hh target gene expression. In this paper, we demonstrate that

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29

Wyatt, T. A., J. H. Sisson, M. A. Forgèt, R. G. Bennett, F. G. Hamel, and J. R. Spurzem. "Relaxin Stimulates Bronchial Epithelial Cell PKA Activation, Migration, and Ciliary Beating1." Experimental Biology and Medicine 227, no. 11 (2002): 1047–53. http://dx.doi.org/10.1177/153537020222701114.

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Relaxin is an insulin-like serum protein secreted during pregnancy and found in many tissues, including the lung. Relaxin is reported to stimulate epithelial cell proliferation, but the effects of relaxin on airway epithelium are unknown. We tested the hypothesis that relaxin would stimulate the increased migration of bronchial epithelial cells (BEC) in response to wounding. Using monolayers of BEC in a wound-healing model, relaxin augmented wound closure with maximal closure occurring at 12.hr (1 μM). Unlike cytokines, relaxin did not stimulate increased BEC interleukin-8 (IL-8) release. Rela

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30

Horáčková, Jaroslava, and Vojeslav Štěrba. "Kinetics of Substitution of 4-Methoxyphenylazo Groups of 2,6-Dioxo-5(3)-(4-methoxyphenylazo)-3(5)-(4-methoxyphenylhydrazono)-1,2,3,6-tetrahydropyridine-4-carboxylic Acid by Reaction with 4-Nitrobenzenediazonium Cation." Collection of Czechoslovak Chemical Communications 59, no. 7 (1994): 1665–72. http://dx.doi.org/10.1135/cccc19941665.

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Kinetics have been studied of gradual replacement of 4-methoxyphenylazo groups in 2,6-dioxo-5(3)-(4-methoxyphenylazo)-3(5)-(4-methoxyphenylhydrazono)-1,2,3,6-tetrahydropyridine-4-carboxylic acid (IIIa) by 4-nitrophenylazo groups using the reaction with 4-nitrobenzenediazonium cation (IIc) in acetate and phosphate buffers. The rate constant of replacement of the second methoxyphenylazo group is lower by a factor of ca 60. From the experimentally found pKa values of the corresponding azohydrazone compounds with methoxy, chloro, or nitro substituent at 4-position (IIIa - IIIf) it has been conclud

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31

Song, Bin, Gerda Oswald, Matthias Bastian, Helmut Sigel, and Bernhard Lippert. "Extent of the Acidification by N7-Coordinated cis-Diammine-Platinum(II) on the Acidic Sites of Guanine Derivatives." Metal-Based Drugs 3, no. 3 (1996): 131–41. http://dx.doi.org/10.1155/mbd.1996.131.

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Coordination of two monoprotonated 2'-deoxyguanosine 5'-monophosphate species, H(dGMP)−, via N7 to cis-(NH3)2Pt2+ gives the complex cis-(NH3)2Pt(H·dGMP)2 which is a four-protonic acid. The corresponding acidity constants were measured by potentiometric pH titrations (25℃; I = 0.1 M, NaNO3). The first two protons are released from the two -P(O)2(OH)− groups (PKa/1 = 5.57; PKa/2 = 6.29) and the next two protons are from the H(N1) sites of the guanine residues (PKa/3 = 8.73; PKa/4 = 9.48). The micro acidity constants of the various sites are also evaluated. Comparison of these data with those det

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32

Naro, Fabio, Claudio Sette, Elena Vicini, et al. "Involvement of Type 4 cAMP-Phosphodiesterase in the Myogenic Differentiation of L6 Cells." Molecular Biology of the Cell 10, no. 12 (1999): 4355–67. http://dx.doi.org/10.1091/mbc.10.12.4355.

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Myogenic cell differentiation is induced by Arg8-vasopressin, whereas high cAMP levels and protein kinase A (PKA) activity inhibit myogenesis. We investigated the role of type 4 phosphodiesterase (PDE4) during L6-C5 myoblast differentiation. Selective PDE4 inhibition resulted in suppression of differentiation induced by vasopressin. PDE4 inhibition prevented vasopressin-induced nuclear translocation of the muscle-specific transcription factor myogenin without affecting its overall expression level. The effects of PDE4 inhibition could be attributed to an increase of cAMP levels and PKA activit

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Ohno, Kazuki, Yoshio Inoue, and Minoru Sakurai. "Application of 4-layer ONIOM method to pKa calculations for proteins." Seibutsu Butsuri 41, supplement (2001): S103. http://dx.doi.org/10.2142/biophys.41.s103_4.

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Chen, Yu-Lin, Nikos L. Doltsinis, Robert C. Hider, and Dave J. Barlow. "Prediction of Absolute Hydroxyl pKa Values for 3-Hydroxypyridin-4-ones." Journal of Physical Chemistry Letters 3, no. 20 (2012): 2980–85. http://dx.doi.org/10.1021/jz301061m.

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Taurin, Sebastien, Nathan Sandbo, Douglas M. Yau, Nan Sethakorn та Nickolai O. Dulin. "Phosphorylation of β-catenin by PKA promotes ATP-induced proliferation of vascular smooth muscle cells". American Journal of Physiology-Cell Physiology 294, № 5 (2008): C1169—C1174. http://dx.doi.org/10.1152/ajpcell.00096.2008.

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Extracellular ATP stimulates proliferation of vascular smooth muscle cells (VSMC) through activation of G protein-coupled P2Y purinergic receptors. We have previously shown that ATP stimulates a transient activation of protein kinase A (PKA), which, together with the established mitogenic signaling of purinergic receptors, promotes proliferation of VSMC (Hogarth DK, Sandbo N, Taurin S, Kolenko V, Miano JM, Dulin NO. Am J Physiol Cell Physiol 287: C449–C456, 2004). We also have shown that PKA can phosphorylate β-catenin at two novel sites (Ser552 and Ser675) in vitro and in overexpression cell

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Chin, E. C., and D. R. E. Abayasekara. "Progesterone secretion by luteinizing human granulosa cells: a possible cAMP-dependent but PKA-independent mechanism involved in its regulation." Journal of Endocrinology 183, no. 1 (2004): 51–60. http://dx.doi.org/10.1677/joe.1.05550.

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The corpus luteum formed after luteinization of follicular cells secretes progesterone under the control of luteinizing hormone (LH). Binding of LH to its G-protein-coupled receptor leads to the activation of the adenylate cyclase/ cyclic AMP (cAMP)/cAMP-dependent protein kinase (PKA) signalling pathway. The identification of a new class of cAMP-binding proteins termed ‘guanine nucleotide exchange factors’ (cAMP-GEFs) provides a means by which changes in cAMP could yield actions that are independent of PKA. Hence, in this study, we have explored the hypothesis that steroidogenesis in luteinizi

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Miller, Megan, Rashaun Wilson, TuKiet Lam, Angus Nairn, and Marina Picciotto. "Evaluation of the Phosphoproteome of Mouse Alpha 4/Beta 2-Containing Nicotinic Acetylcholine Receptors In Vitro and In Vivo." Proteomes 6, no. 4 (2018): 42. http://dx.doi.org/10.3390/proteomes6040042.

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Activation of nicotinic acetylcholine receptors containing α4 and β2 subunits (α4/β2* nAChRs) in the mammalian brain is necessary for nicotine reinforcement and addiction. We previously identified interactions between α4/β2* nAChRs and calcium/calmodulin-dependent protein kinase II (CaMKII) in mouse and human brain tissue. Following co-expression of α4/β2 nAChR subunits with CaMKII in HEK cells, mass spectrometry identified 8 phosphorylation sites in the α4 subunit. One of these sites and an additional site were identified when isolated α4/β2* nAChRs were dephosphorylated and subsequently incu

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Ichikawa, T., K. Horie-Inoue, K. Ikeda, B. Blumberg, and S. Inoue. "Vitamin K2 induces phosphorylation of protein kinase A and expression of novel target genes in osteoblastic cells." Journal of Molecular Endocrinology 39, no. 4 (2007): 239–47. http://dx.doi.org/10.1677/jme-07-0048.

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AbstractVitamin K is known as a critical nutrient required for bone homeostasis and blood coagulation, and it is clinically used as a therapeutic agent for osteoporosis in Japan. Besides its enzymatic action as a cofactor of vitamin K-dependent γ-glutamyl carboxylase (GGCX), we have previously shown that vitamin K2 is a transcriptional regulator of bone marker genes and extracellular matrix-related genes, by activating the steroid and xenobiotic receptor (SXR). To explore a novel action of vitamin K in osteoblastic cells, we identified genes up-regulated by a vitamin K2 isoform menaquinone-4 (

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Hartshorn, R. T., and G. R. Moore. "A denaturation-induced proton-uptake study of horse ferricytochrome c." Biochemical Journal 258, no. 2 (1989): 595–98. http://dx.doi.org/10.1042/bj2580595.

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The observation that 6 M-urea denatures horse ferricytochrome c in the pH range 4-6, but not horse ferrocytochrome c, has been exploited to determine the denaturation-induced proton uptake of ferricytochrome c. This is related to the pKa values of ionizable groups buried within the native protein. The data indicate that one of the haem propionic acid substituents of ferricytochrome c has a pKa of less than 4.5, whereas the other has a pKa of greater than 9.

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McClelland, Robert A., Daniel Ren, Raechelle D'Sa, and Abid R. Ahmed. "Acidity constants and reactivities of the benzidine and N,N-dimethylbenzidine dications, the two electron oxidation intermediates of benzidine carcinogens." Canadian Journal of Chemistry 78, no. 9 (2000): 1178–85. http://dx.doi.org/10.1139/v00-123.

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This paper describes the behavior in aqueous solutions of the two electron oxidation products of the carcinogens benzidine and N,N-dimethylbenzidine. In biological systems there is evidence that these diamines are oxidized by peroxidases, and that a product of this oxidation may be partly responsible for carcinogenicity. Entry into the oxidation products in the present study was provided through the bis-perchlorate salts of dications obtained upon chemical oxidation and through the irradiation of 4'-amino and 4'-N,N-dimethylamino-4-azidobiphenyls. The benzidine oxidation product exists in thre

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Izumi, Yuichiro, Yushi Nakayama, Tomohiko Mori, et al. "Downregulation of vasopressin V2 receptor promoter activity via V1a receptor pathway." American Journal of Physiology-Renal Physiology 292, no. 5 (2007): F1418—F1426. http://dx.doi.org/10.1152/ajprenal.00358.2006.

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Vasopressin V1a and V2 receptors (V1aR and V2R, respectively) distribute in the collecting duct of the kidney. Although the function of V2R mediating the antidiuretic effect of AVP has been investigated in detail, the role of V1aR in the collecting ducts has not been elucidated. In the present study, we have investigated the role of the V1aR pathway in V2R promoter activity. We cloned the 5′-flanking region of rat V2R (rV2R) and investigated rV2R promoter activity in the LLC-PK1 cell line transfected to express rat V1aR (rV1aR) dominantly (LLC-PK1/rV1aR). AVP induced a transient increase, foll

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Li, Xiang, Elaine Huston, Martin J. Lynch, Miles D. Houslay та George S. Baillie. "Phosphodiesterase-4 influences the PKA phosphorylation status and membrane translocation of G-protein receptor kinase 2 (GRK2) in HEK-293β2 cells and cardiac myocytes". Biochemical Journal 394, № 2 (2006): 427–35. http://dx.doi.org/10.1042/bj20051560.

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Membrane-recruitment of GRK2 (G-protein receptor kinase 2) provides a fundamental step in the desensitization process controlling GPCRs (G-protein-coupled receptors), such as the β2AR (β2-adrenergic receptor). In the present paper, we show that challenge of HEK-293β2 [human embryonic kidney cells stably overexpressing the FLAG-tagged β2AR–GFP (green fluorescent protein)] cells with the β-adrenoceptor agonist, isoprenaline, causes GRK2 to become phosphorylated by PKA (cAMP-dependent protein kinase). This action is facilitated when cAMP-specific PDE4 (phosphodiesterase-4) activity is selectively

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HOFFMANN, Ralf, Ian R. WILKINSON, J. Fraser McCALLUM, Peter ENGELS, and Miles D. HOUSLAY. "cAMP-specific phosphodiesterase HSPDE4D3 mutants which mimic activation and changes in rolipram inhibition triggered by protein kinase A phosphorylation of Ser-54: generation of a molecular model." Biochemical Journal 333, no. 1 (1998): 139–49. http://dx.doi.org/10.1042/bj3330139.

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Ser-13 and Ser-54 were shown to provide the sole sites for the protein kinase A (PKA)-mediated phosphorylation of the human cAMP-specific phosphodiesterase isoform HSPDE4D3. The ability of PKA to phosphorylate and activate HSPDE4D3 was mimicked by replacing Ser-54 with either of the negatively charged amino acids, aspartate or glutamate, within the consensus motif of RRES54. The PDE4 selective inhibitor rolipram {4-[3-(cyclopentoxy)-4-methoxyphenyl]-2-pyrrolidone} inhibited both PKA-phosphorylated HSPDE4D3 and the Ser-54 → Asp mutant, with an IC50 value that was ∼ 8-fold lower than that seen f

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Cullen, Kimberly A., John McCool, M. Sawkat Anwer, and Cynthia R. L. Webster. "Activation of cAMP-guanine exchange factor confers PKA-independent protection from hepatocyte apoptosis." American Journal of Physiology-Gastrointestinal and Liver Physiology 287, no. 2 (2004): G334—G343. http://dx.doi.org/10.1152/ajpgi.00517.2003.

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cAMP has previously been shown to promote cell survival in a variety of cell types, but the downstream signaling pathway(s) of this antiapoptotic effect is unclear. Thus the role of cAMP signaling through PKA and cAMP-regulated guanine nucleotide exchange factors (cAMP-GEFs) in cAMP's antiapoptotic action was investigated in the present study. cAMP's protective effect against bile acid-, Fas ligand-, and TNF-α-induced apoptosis in rat hepatocytes was largely unaffected by the selective PKA inhibitor, Rp-8-(4-chlorophenylthio)-cAMP (Rp-cAMP). In contrast, a novel cAMP analog, 8-(4-chlorophenylt

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Schubert, Rudolf, Gernot Lehmann, Vladimir N. Serebryakov, Hartmut Mewes, and Hans-Heinrich Hopp. "cAMP-dependent protein kinase is in an active state in rat small arteries possessing a myogenic tone." American Journal of Physiology-Heart and Circulatory Physiology 277, no. 3 (1999): H1145—H1155. http://dx.doi.org/10.1152/ajpheart.1999.277.3.h1145.

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The hypothesis that cAMP-dependent protein kinase (protein kinase A; PKA) is in an active state in small arteries possessing a myogenic tone was investigated in pressurized rat tail small arteries. At a pressure of 80 mmHg, these vessels constricted to 71.6 ± 1.0% ( n = 32) of the diameter of the fully relaxed state. The PKA inhibitors Rp-8-(4-chlorophenylthio)-adenosine 3′,5′-cyclic monophosphothioate (Rp-CPT-cAMPS) and N-(2-{[3-(4-bromophenyl)-2-propenyl]amino}-ethyl)-5-isoquinolinesulfonamide HCl (H-89) constricted these vessels dose dependently. For example, 300 μM Rp-CPT-cAMPS and 9 μM H-

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Persaud, Leah, Jason Mighty, Xuelin Zhong, et al. "IL-24 Promotes Apoptosis through cAMP-Dependent PKA Pathways in Human Breast Cancer Cells." International Journal of Molecular Sciences 19, no. 11 (2018): 3561. http://dx.doi.org/10.3390/ijms19113561.

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Interleukin 24 (IL-24) is a tumor-suppressing protein, which inhibits angiogenesis and induces cancer cell-specific apoptosis. We have shown that IL-24 regulates apoptosis through phosphorylated eukaryotic initiation factor 2 alpha (eIF2α) during endoplasmic reticulum (ER) stress in cancer. Although multiple stresses converge on eIF2α phosphorylation, the cellular outcome is not always the same. In particular, ER stress-induced apoptosis is primarily regulated through the extent of eIF2α phosphorylation and activating transcription factor 4 (ATF4) action. Our studies show for the first time th

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Qi, Zhonghua, Chuan-Ming Hao, Kelli Salter, Reyadh Redha, and Matthew D. Breyer. "Type II cAMP-dependent protein kinase regulates electrogenic ion transport in rabbit collecting duct." American Journal of Physiology-Renal Physiology 276, no. 4 (1999): F622—F628. http://dx.doi.org/10.1152/ajprenal.1999.276.4.f622.

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cAMP mediates many of the effects of vasopressin, prostaglandin E2, and β-adrenergic agents upon salt and water transport in the renal collecting duct. The present studies examined the role of cAMP-dependent protein kinase (PKA) in mediating these effects. PKA is a heterotetramer comprised of two regulatory (R) subunits and two catalytic (C) subunits. The four PKA isoforms may be distinguished by their R subunits that have been designated RIα, RIβ, RIIα, and RIIβ. Three regulatory subunits, RIα, RIIα, and RIIβ, were detected by immunoblot and ribonuclease protection in both primary cultures an

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Schreiber, Rudy, Romain Hollands, and Arjan Blokland. "A Mechanistic Rationale for PDE-4 Inhibitors to Treat Residual Cognitive Deficits in Acquired Brain Injury." Current Neuropharmacology 18, no. 3 (2020): 188–201. http://dx.doi.org/10.2174/1570159x17666191010103044.

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Patients with acquired brain injury (ABI) suffer from cognitive deficits that interfere significantly with their daily lives. These deficits are long-lasting and no treatment options are available. A better understanding of the mechanistic basis for these cognitive deficits is needed to develop novel treatments. Intracellular cyclic adenosine monophosphate (cAMP) levels are decreased in ABI. Herein, we focus on augmentation of cAMP by PDE4 inhibitors and the potentially synergistic mechanisms in traumatic brain injury. A major acute pathophysiological event in ABI is the breakdown of the blood

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MacInnis, Judith A., Greg D. Boucher, R. Palepu, and D. Gerrard Marangoni. "The properties of a family of two-headed surfactant systems: the 4-alkyl-3-sulfosuccinates 2. Surface properties of alkyl sulfosuccinate micelles." Canadian Journal of Chemistry 77, no. 3 (1999): 340–47. http://dx.doi.org/10.1139/v99-008.

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The micellar properties of a family of two-headed surfactants, the alkyl sulfosuccinates, were investigated employing fluorescence, ultra-violet spectroscopy, and acid-base titrations, as a function of the chain length of the surfactant. Polarity of the micellar interior was investigated using pyrene and the ionic probe 8-anilino-1-naphthalensulfonic acid ammonium salt (ANS). Pyrene I1/I3 ratios were used to probe the microenvironment of the probe in the palisade layer of the micelle. The pKa values of both of the anionic head groups were determined using acid-base titrations. Surface potentia

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Sandberg, Lars, and Olle Edholm. "pKa calculations along a bacteriorhodopsin molecular dynamics trajectory." Biophysical Chemistry 65, no. 2-3 (1997): 189–204. http://dx.doi.org/10.1016/s0301-4622(96)02262-4.

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