• Title/Summary/Keyword: 1,2-DAG

Search Result 84, Processing Time 0.022 seconds

G Protein-Coupled Receptor Signaling in Gastrointestinal Smooth Muscle

  • Sohn, Uy-Dong;Kim, Dong-Seok;Murthy, Karnam S.
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.5 no.4
    • /
    • pp.287-297
    • /
    • 2001
  • Contraction of smooth muscle is initiated by an increase in cytosolic $Ca^{2+}$ leading to activation of $Ca^{2+}$/ calmodulin-dependnet myosin light chain (MLC) kinase and phosphorylation of MLC. The types of contraction and signaling mechanisms mediating contraction differ depending on the region. The involvement of these different mechanisms varies depending on the source of $Ca^{2+}$ and the kinetic of $Ca^{2+}$ mobilization. $Ca^{2+}$ mobilizing agonists stimulate different phospholipases $(PLC-{\beta},\;PLD\;and\;PLA_2)$ to generate one or more $Ca^{2+}$ mobilizing messengers $(IP_3\;and\;AA),$ and diacylglycerol (DAG), an activator of protein kinase C (PKC). The relative contributions of $PLC-{\beta},\;PLA_2$ and PLD to generate second messengers vary greatly between cells and types of contraction. In smooth muscle cell derived form the circular muscle layer of the intestine, preferential hydrolysis of $PIP_2$ and generation of $IP_3$ and $IP_3-dependent\;Ca^{2+}$ release initiate the contraction. In smooth muscle cells derived from longitudinal muscle layer of the intestine, preferential hydrolysis of PC by PLA2, generation of AA and AA-mediated $Ca^{2+}$ influx, cADP ribose formation and $Ca^{2+}-induced\;Ca^{2+}$ release initiate the contraction. Sustained contraction, however, in both cell types is mediated by $Ca^{2+}-independent$ mechanism involving activation of $PKC-{\varepsilon}$ by DAG derived form PLD. A functional linkage between $G_{13},$ RhoA, ROCK, $PKC-{\varepsilon},$ CPI-17 and MLC phosphorylation in sustained contraction has been implicated. Contraction of normal esophageal circular muscle (ESO) in response to acetylcholine (ACh) is linked to $M_2$ muscarinic receptors activating at least three intracellular phospholipases, i.e. phosphatidylcholine-specific phospholipase C (PC-PLC), phospholipase D (PLD) and the high molecular weight (85 kDa) cytosolic phospholipase $A_2\;(cPLA_2)$ to induce phosphatidylcholine (PC) metabolism, production of diacylglycerol (DAG) and arachidonic acid (AA), resulting in activation of a protein kinase C (PKC)-dependent pathway. In contrast, lower esophageal sphincter (LES) contraction induced by maximally effective doses of ACh is mediated by muscarinic $M_3$ receptors, linked to pertussis toxin-insensitive GTP-binding proteins of the $G_{q/11}$ type. They activate phospholipase C, which hydrolyzes phosphatidylinositol bisphosphate $(PIP_2),$ producing inositol 1, 4, 5-trisphosphate $(IP_3)$ and DAG. $IP_3$ causes release of intracellular $Ca^{2+}$ and formation of a $Ca^{2+}$-calmodulin complex, resulting in activation of myosin light chain kinase and contraction through a calmodulin-dependent pathway.

  • PDF

Development of CPLD Technology Mapping Algorithm for Sequential Circuit Improved Run-Time Under Time Constraint (시간제약 조건하에서 순차 회로를 위한 수행시간을 개선한 CPLD 기술 매핑 알고리즘 개발)

  • Yun, Chung-Mo;Kim, Hui-Seok
    • Journal of the Institute of Electronics Engineers of Korea SD
    • /
    • v.37 no.4
    • /
    • pp.80-89
    • /
    • 2000
  • In this paper, we propose a new CPLD technology mapping algorithm for sequential circuit under time constraints. The algorithm detects feedbacks of sequential circuit, separate each feedback variables into immediate input variable, and represent combinational part into DAG. Also, among the nodes of the DAG, the nodes that the number of outdegree is more than or equal to 2 is not separated, but replicated from the DAG, and reconstructed to fanout-free-tree. To use this construction method is for reason that area is less consumed than the TEMPLA algorithm to implement circuits, and process time is improved rather than TMCPLD within given time constraint. Using time constraint and delay of device the number of partitionable multi-level is defined, the number of OR terms that the initial costs of each nodes is set to and total costs that the$^1$costs is set to after merging nodes is calculated, and the nodes that the number of OR terms of CLBs that construct CPLD is excessed is partitioned and is reconstructed as subgraphs. The nodes in the partitioned subgraphs is merged through collapsing, and the collapsed equations is performed by bin packing so that it fit to the number of OR terms in the CLBs of a given device. In the results of experiments to MCNC circuits for logic synthesis benchmark, we can shows that proposed technology mapping algorithm reduces the number of CLBs by 15.58% rather than the TEMPLA, and reduces process time rather than the TMCPLD.

  • PDF

Development of CPLD technology mapping algorithm for Sequential Circuit under Time Constraint (시간제약 조건하에서 순차 회로를 위한 CPLD 기술 매핑 알고리즘 개발)

  • Youn, Chung-Mo;Kim, Hi-Seok
    • The Transactions of the Korea Information Processing Society
    • /
    • v.7 no.1
    • /
    • pp.224-234
    • /
    • 2000
  • In this paper, we propose a new CPLD technology mapping algorithm for sequential circuit under time constraints. The algorithm detects feedbacks of sequential circuit, separate each feedback variables into immediate input variable, and represent combinational part into DAG. Also, among the nodes of the DAG, the nodes that the number of outdegree is more than or equal to 2 is not separated, but replicated from the DAG, and reconstructed to fanout-free-tree. To use this construction method is for reason that area is less consumed than the TEMPLA algorithm to implement circuits, and process time is improved rather than TMCPLD within given time constraint. Using time constraint and delay of device the number of partitionable multi-level is defined, the number of OR terms that the initial costs of each nodes is set to and total costs that the costs is set to after merging nodes is calculated, and the nodes that the number of OR terms of CLBs that construct CPLD is excessed is partitioned and is reconstructed as subgraphs. The nodes in the partitioned subgraphs is merged through collapsing, and the collapsed equations is performed by bin packing so that if fit to the number of OR terms in the CLBs of a given device. In the results of experiments to MCNC circuits for logic synthesis benchmark, we can shows that proposed technology mapping algorithm reduces the number of CLBs bu 15.58% rather than the TEMPLA, and reduces process time rather than the TMCPLD.

  • PDF

Palladium-Catalyzed Cross-Coupling Reaction of (E)-1-Alkenyl-1,3,2-benzo-dioxaboroles with Allylic Phenoxides. A Simple Route 1,4-Alkadienes from Alkynes via Hydroboration$^\dag$

  • Sasaya Fumihito;Norio Miyaura;Akira Suzuki
    • Bulletin of the Korean Chemical Society
    • /
    • v.8 no.4
    • /
    • pp.329-332
    • /
    • 1987
  • The reaction of (E)-1-alkenyl-1,3,2-benzodioxaboroles with a variety of allylic phenoxides in the presence of a catalytic amount of Pd$(PPh_3)_4$ is described. The reaction affords a general and simple procedure for the preparation of 1,4-alkadienes from alkynes via hydroboration.

Biological Significance of Essential Fatty Acids/Prostanoids/Lipoxygenase-Derived Monohydroxy Fatty Acids in the Skin

  • Ziboh, Vincent-A.;Cho, Yunhi;Mani, Indu;Xi, Side
    • Archives of Pharmacal Research
    • /
    • v.25 no.6
    • /
    • pp.747-758
    • /
    • 2002
  • The skin displays a highly active metabolism of polyunsaturated fatty acids (PUFA). Dietary deficiency of linoleic acid (LA), an 18-carbon (n-6) PUFA, results in characteristic scaly skin disorder and excessive epidermal water loss. Although arachidonic acid (AA), a 20-carbon (n6) PUFA, is metabolized via cyclooxygenase pathway into predominantly prostaglandin $E_2(PGE_2)$ and $PGF_{2{\alpha}}$, the metabolism of AA via the 15-lipoxygenase (15-LOX) pathway, which is very active in skin epidermis and catalyzes the transformation of M into predominantly 15S-hydroxyeicosatetraenoic acid (15S-HETE). Additionally, the 15-LOX also metabolizes the 18-carbon LA into 13S-hydroxyoctadecadienoic acid (13S-HODE), respectively. Interestingly, 15-LOX catalyzes the transformation of $dihomo-{\gamma}-linolenic$ acid (DGLA), derived from dietary gamma-linolenic acid, to 15S-hydroxyeicosatrienoic acid (15S-HETrE). These monohydroxy fatty acids are incorporated into the membrane inositol phospholipids which undergo hydrolytic cleavage to yield substituted-diacylglycerols such as 13S-HODE-DAG from 13S-HODE and 15S-HETrE-DAG from 15S-HETrE. These substituted-monohydroxy fatty acids seemingly exert anti-inflammatory/antiproliferative effects via the modulation of selective protein kinase C as well as on the upstream/down-stream nuclear MAP-kinase/AP-1/apoptotic signaling events.

The Inhibitory Mechanism of Aloe Glycoprotein (NY945) on the Mediator Release in the Guinea Pig Lung Mast Cell Activated with Antigen-Antibody Complexes

  • Ro, Jai-Youl;Lee, Byung-Chul;Chung, Myung-Hee;Lee, Seung-Ki;Sung, Chung-Ki;Kim, Kyung-Hwan;Park, Young-In
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.2 no.1
    • /
    • pp.119-131
    • /
    • 1998
  • It has been reported that the glycoprotein extracted from Aloe has strong anti-inflammatory response. However, there has been no research report yet about the effect of Aloe on allergic hypersensitivity reactivity. By using guinea pig lung mast cells, this study aimed to examine the effects of Aloe glycoprotein (NY945) on the mediator releases caused by mast cell activation, and also aimed to assess the effects of NY945 on the mechanism of mediator releases in the mast cell activation. We partially purified mast cell from guinea pig lung tissues by using the enzyme digestion, the rough and the discontinuous density percoll gradient method. Mast cells were sensitized with IgG1 (anti-OA) and challenged with ovalbumin. Histamine was assayed by fluorometric analyzer, leukotrienes by radioimmunoassay. The phospholipase D activity was assessed by the production of labeled phosphatidylalcohol. The amount of mass 1, 2-diacylglycerol (DAG) was measured by the $[^3H]DAG$ produced when prelabeled with $[^3H]myristic$ acid. The phospholipid methylation was assessed by measuring the incorporation of the $[^3H]methyl$ moiety into phospholipids of cellular membranes. Pretreatment of NY945 (10 ${\mu}g$) significantly decreased histamine and leukotrienes releases during mast cell activation. The decrease of histamine release was stronger than that of leukotriene during mast cell activation. The phospholipase D activity increased by the mast cell activation was decreased by the dose-dependent manner in the pretreatment of NY945. The amount of DAG produced by PLC activity was decreased by NY945 pretreatment. The amount of mass 1, 2-diacylglycerol produced by activation of mast cells was decreased in the pretreatment of NY945. NY945 pretreatment strongly inhibited the incorporation of the $[^3H]methyl$ moiety into phospholipids. The data suggest that NY945 purified from Aloe inhibits in part an increase of 1, 2-diacylglycerol which is produced by activating mast cells with antigen-antibody reactions, which is mediated via phosphatidylcholine-phospholipase D and phosphatidylinositol-phospholipase C systems, and then followed by the inhibition of histamine release. Furthermore, NY945 reduces the production of phosphatidylcholine by inhibiting the methyltransferase I and II, which decreases the conversion of phosphatidylcholine into arachidonic acid and inhibits the production of leukotrienes.

  • PDF

Cationic Cyclization to Tricyclene Structures$^\dag$

  • Kang, Ja-Hyo;Lee, Won-Koo;Shin, Hyun-Tai
    • Bulletin of the Korean Chemical Society
    • /
    • v.8 no.4
    • /
    • pp.264-269
    • /
    • 1987
  • Various carbocation-mediated cyclizations to tricyclene structure (basically, tricyclo $[2,2,1,0^{2,6}]$ heptane skeleton) were carried out, starting from protonated species of either 3-methyl-2,5-norbornadiene-2-carboxylic acid (10) or 3-methylene-5-norbornene-2-carboxylic acids (18 and 19). The resulting products were individually converted to ${\pi}$-iodotricyclene (35), a pivotal intermediate in almost all syntheses of tricyclene terpenes.

An Efficient CPLD Technology Mapping considering Area under Time Constraint (시간 제약 조건하에서 면적을 고려한 효율적인 CPLD 기술 매핑)

  • Kim, Jae-Jin;Kim, Hui-Seok
    • Journal of the Institute of Electronics Engineers of Korea SD
    • /
    • v.38 no.1
    • /
    • pp.79-85
    • /
    • 2001
  • In this paper, we propose a new technology mapping algorithm for CPLD consider area under time constraint(TMFCPLD). This technology mapping algorithm detect feedbacks from boolean networks, then variables that have feedback are replaced to temporary variables. Creating the temporary variables transform sequential circuit to combinational circuit. The transformed circuits are represented to DAG. After traversing all nodes in DAG, the nodes that have output edges more than two are replicated and reconstructed to fanout free tree. This method is for reason to reduce area and improve total run time of circuits by TEMPLA proposed previously. Using time constraints and delay time of device, the number of graph partitionable multi-level is decided. Initial cost of each node are the number of OR-terms that it have. Among mappable clusters, clusters of which the number of multi-level is least is selected, and the graph is partitioned. Several nodes in partitioned clusters are merged by collapsing, and are fitted to the number of OR-terms in a given CLB by bin packing. Proposed algorithm have been applied to MCNC logic synthesis benchmark circuits, and have reduced the number of CLBs by 62.2% than those of DDMAP. And reduced the number of CLBs by 17.6% than those of TEMPLA, and reduced the number of CLBs by 4.7% than those of TMCPLD. This results will give much efficiency to technology mapping for CPLDs.

  • PDF

Class function table matrix of finite groups

  • Park, Won-Sun
    • Journal of the Korean Mathematical Society
    • /
    • v.32 no.4
    • /
    • pp.689-695
    • /
    • 1995
  • Let G be a finite group with k distinct conjugacy classes $C_1, C_2, \cdots, C_k$ and F an algebraically closed field such that char$(F){\dag}\left$\mid$ G \right$\mid$$. We denoted by $Irr_F$(G) the set of all irreducible F-characters of G and $Cf_F$(G) the set of all class functions of G into F. Then $Cf_F$(G) is a commutative F-algebra with an F-basis $Irr_F(G) = {\chi_1, \chi_2, \cdots, \chi_k}$.

  • PDF