PDPK1

Summary

Gene Symbol: PDPK1
Description: 3-phosphoinositide dependent protein kinase 1
Alias: PDK1, PDPK2, PDPK2P, PRO0461, 3-phosphoinositide-dependent protein kinase 1, 3-phosphoinositide-dependent protein kinase 2 pseudogene, PkB kinase like gene 1
Species: human
Products:     PDPK1

Top Publications

  1. Currie R, Walker K, Gray A, Deak M, Casamayor A, Downes C, et al. Role of phosphatidylinositol 3,4,5-trisphosphate in regulating the activity and localization of 3-phosphoinositide-dependent protein kinase-1. Biochem J. 1999;337 ( Pt 3):575-83 pubmed
    3-Phosphoinositide-dependent protein kinase-1 (PDK1) interacts stereoselectively with the d-enantiomer of PtdIns(3,4,5)P3 (KD 1.6 nM) and PtdIns(3,4)P2 (KD 5.2 nM), but binds with lower affinity to PtdIns3P or PtdIns(4,5)P2...
  2. Egawa K, Maegawa H, Shi K, Nakamura T, Obata T, Yoshizaki T, et al. Membrane localization of 3-phosphoinositide-dependent protein kinase-1 stimulates activities of Akt and atypical protein kinase C but does not stimulate glucose transport and glycogen synthesis in 3T3-L1 adipocytes. J Biol Chem. 2002;277:38863-9 pubmed
    ..On the other hand, only atypical PKC and Akt activation was insufficient for stimulation of glucose transport, and constitutive activation of Akt-GSK-3 pathway may inhibit glycogen synthesis and MAPK cascade in 3T3-L1 adipocytes. ..
  3. Mora A, Komander D, van Aalten D, Alessi D. PDK1, the master regulator of AGC kinase signal transduction. Semin Cell Dev Biol. 2004;15:161-70 pubmed
    ..we review recent biochemical, genetic and structural studies on the 3-phosphoinositide-dependent protein kinase-1 (PDK1), which phosphorylates and activates the AGC kinase members regulated by PI 3-kinase...
  4. Scheid M, Marignani P, Woodgett J. Multiple phosphoinositide 3-kinase-dependent steps in activation of protein kinase B. Mol Cell Biol. 2002;22:6247-60 pubmed
    ..b>PDK1 phosphorylation of threonine 308 was primarily dependent upon prior serine 473 phosphorylation and, to a lesser ..
  5. Maurer M, Su T, Saal L, Koujak S, Hopkins B, Barkley C, et al. 3-Phosphoinositide-dependent kinase 1 potentiates upstream lesions on the phosphatidylinositol 3-kinase pathway in breast carcinoma. Cancer Res. 2009;69:6299-306 pubmed publisher
    ..in a majority of human breast cancers and that 21% of tumors had five or more copies of the gene encoding PDK1, PDPK1. We found that increased PDPK1 copy number was associated with upstream pathway lesions (ERBB2 amplification, PTEN ..
  6. Alessi D, Kozlowski M, Weng Q, Morrice N, Avruch J. 3-Phosphoinositide-dependent protein kinase 1 (PDK1) phosphorylates and activates the p70 S6 kinase in vivo and in vitro. Curr Biol. 1998;8:69-81 pubmed
    ..Co-expression of p70 with 3-phosphoinositide-dependent protein kinase 1 (PDK1), a protein kinase that has previously been shown to phosphorylate and activate protein kinase B (PKB, also known ..
  7. Tian X, Rusanescu G, Hou W, Schaffhausen B, Feig L. PDK1 mediates growth factor-induced Ral-GEF activation by a kinase-independent mechanism. EMBO J. 2002;21:1327-38 pubmed
    ..Here we show that Ral-GEF stimulation by EGF involves an additional mechanism, PI3-K-dependent kinase 1 (PDK1)-induced enhancement of Ral-GEF catalytic activity...
  8. Lin H, Hsieh F, Song H, Lin J. Elevated phosphorylation and activation of PDK-1/AKT pathway in human breast cancer. Br J Cancer. 2005;93:1372-81 pubmed
  9. Balendran A, Biondi R, Cheung P, Casamayor A, Deak M, Alessi D. A 3-phosphoinositide-dependent protein kinase-1 (PDK1) docking site is required for the phosphorylation of protein kinase Czeta (PKCzeta ) and PKC-related kinase 2 by PDK1. J Biol Chem. 2000;275:20806-13 pubmed
    ..The 3-phosphoinositide-dependent protein kinase (PDK1) activates many members of the AGC subfamily of kinases in vitro, including PKCzeta and PRK2 by phosphorylating the ..

More Information

Publications79

  1. Sarbassov D, Guertin D, Ali S, Sabatini D. Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex. Science. 2005;307:1098-101 pubmed
    ..requires the phosphorylation of Thr308 in the activation loop by the phosphoinositide-dependent kinase 1 (PDK1) and Ser473 within the carboxyl-terminal hydrophobic motif by an unknown kinase...
  2. Kobayashi T, Deak M, Morrice N, Cohen P. Characterization of the structure and regulation of two novel isoforms of serum- and glucocorticoid-induced protein kinase. Biochem J. 1999;344 Pt 1:189-97 pubmed
    ..with protein kinase B (PKB) and, like PKB, is activated in vitro by 3-phosphoinositide-dependent protein kinase-1 (PDK1) and in vivo in response to signals that activate phosphatidylinositol (PI) 3-kinase...
  3. Collins B, Deak M, Arthur J, Armit L, Alessi D. In vivo role of the PIF-binding docking site of PDK1 defined by knock-in mutation. EMBO J. 2003;22:4202-11 pubmed
    ..and growth factors and are activated following phosphorylation by 3-phosphoinositide-dependent protein kinase-1 (PDK1)...
  4. Tan J, Lee P, Li Z, Jiang X, Lim Y, Hooi S, et al. B55?-associated PP2A complex controls PDK1-directed myc signaling and modulates rapamycin sensitivity in colorectal cancer. Cancer Cell. 2010;18:459-71 pubmed publisher
    ..B55?-associated PP2A interacts with PDK1 and modulates its activity toward Myc phosphorylation...
  5. Raimondi C, Chikh A, Wheeler A, Maffucci T, Falasca M. A novel regulatory mechanism links PLC?1 to PDK1. J Cell Sci. 2012;125:3153-63 pubmed publisher
    3-Phosphoinositide-dependent protein kinase-1 (PDK1) and phospholipase C (PLC)?1 are two key enzymes in signal transduction that control several intracellular processes...
  6. Park J, Leong M, Buse P, Maiyar A, Firestone G, Hemmings B. Serum and glucocorticoid-inducible kinase (SGK) is a target of the PI 3-kinase-stimulated signaling pathway. EMBO J. 1999;18:3024-33 pubmed
    ..Cotransfection of PDK1 with SGK caused a 6-fold activation of SGK activity, whereas kinase-dead PDK1 caused no activation...
  7. Stephens L, Anderson K, Stokoe D, Erdjument Bromage H, Painter G, Holmes A, et al. Protein kinase B kinases that mediate phosphatidylinositol 3,4,5-trisphosphate-dependent activation of protein kinase B. Science. 1998;279:710-4 pubmed
  8. Ericson K, Gan C, Cheong I, Rago C, Samuels Y, Velculescu V, et al. Genetic inactivation of AKT1, AKT2, and PDPK1 in human colorectal cancer cells clarifies their roles in tumor growth regulation. Proc Natl Acad Sci U S A. 2010;107:2598-603 pubmed publisher
    ..To gain insight into the roles of members of this pathway in growth regulation, we inactivated AKT1, AKT2, or PDPK1 genes by targeted homologous recombination in human colon cancer cell lines...
  9. King C, Newton A. The adaptor protein Grb14 regulates the localization of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2004;279:37518-27 pubmed
    ..Thus, Grb14 serves as an adaptor protein to recruit PDK-1 to activated insulin receptor, thus promoting Akt phosphorylation and transduction of the insulin signal. ..
  10. Scheid M, Parsons M, Woodgett J. Phosphoinositide-dependent phosphorylation of PDK1 regulates nuclear translocation. Mol Cell Biol. 2005;25:2347-63 pubmed
    3-phosphoinositide-dependent kinase 1 (PDK1) phosphorylates the activation loop of a number of protein serine/threonine kinases of the AGC kinase superfamily, including protein kinase B (PKB; also called Akt), serum and glucocorticoid-..
  11. Lee K, D Acquisto F, Hayden M, Shim J, Ghosh S. PDK1 nucleates T cell receptor-induced signaling complex for NF-kappaB activation. Science. 2005;308:114-8 pubmed
    ..We demonstrate that 3-phosphoinositide-dependent kinase 1 (PDK1) has an essential role in this pathway by regulating the activation of PKC and through signal-dependent recruiting ..
  12. Primo L, di Blasio L, Roca C, Droetto S, Piva R, Schaffhausen B, et al. Essential role of PDK1 in regulating endothelial cell migration. J Cell Biol. 2007;176:1035-47 pubmed
    The serine/threonine protein kinase phosphoinositide-dependent kinase 1 (PDK1) plays a central role in cellular signaling by phosphorylating members of the AGC family of kinases, including PKB/Akt...
  13. Lu Z, Cox Hipkin M, Windsor W, Boyapati A. 3-phosphoinositide-dependent protein kinase-1 regulates proliferation and survival of cancer cells with an activated mitogen-activated protein kinase pathway. Mol Cancer Res. 2010;8:421-32 pubmed publisher
    ..This second messenger leads to the recruitment of 3-phosphoinositide-dependent protein kinase-1 (PDK1) to the proximal side of the plasma membrane, which results in the activation of AKT kinase...
  14. Raimondi C, Falasca M. Targeting PDK1 in cancer. Curr Med Chem. 2011;18:2763-9 pubmed
    ..Among the downstream effectors of PI3Ks, 3- phosphoinositide-dependent protein kinase 1 (PDK1) and protein kinase B (PKB)/Akt have a key role in several cancer types...
  15. Vanhaesebroeck B, Alessi D. The PI3K-PDK1 connection: more than just a road to PKB. Biochem J. 2000;346 Pt 3:561-76 pubmed
    ..to cellular membranes by PI3K lipid products and phosphorylation by 3'-phosphoinositide-dependent kinase-1 (PDK1). Here we review the mechanism by which PKB is activated and the downstream actions of this multifunctional kinase...
  16. Gagliardi P, di Blasio L, Orso F, Seano G, Sessa R, Taverna D, et al. 3-phosphoinositide-dependent kinase 1 controls breast tumor growth in a kinase-dependent but Akt-independent manner. Neoplasia. 2012;14:719-31 pubmed
    3-phosphoinositide-dependent protein kinase 1 (PDK1) is the pivotal element of the phosphatidylinositol 3 kinase (PI3K) signaling pathway because it phosphorylates Akt/PKB through interactions with phosphatidylinositol 3,4,5 phosphate...
  17. Kobayashi T, Cohen P. Activation of serum- and glucocorticoid-regulated protein kinase by agonists that activate phosphatidylinositide 3-kinase is mediated by 3-phosphoinositide-dependent protein kinase-1 (PDK1) and PDK2. Biochem J. 1999;339 ( Pt 2):319-28 pubmed
    ..activation of protein kinase B (PKB) by 3-phosphoinositide-dependent protein kinases-1 and -2 (PDK1 and PDK2 respectively) is a key event in mediating the effects of signals that activate PtdIns 3-kinase...
  18. Le Good J, Ziegler W, Parekh D, Alessi D, Cohen P, Parker P. Protein kinase C isotypes controlled by phosphoinositide 3-kinase through the protein kinase PDK1. Science. 1998;281:2042-5 pubmed
    ..Thus, the PKB kinase PDK1 may be responsible for the phosphorylation of PKC isotypes...
  19. Weber D, Taniyama Y, Rocic P, Seshiah P, Dechert M, Gerthoffer W, et al. Phosphoinositide-dependent kinase 1 and p21-activated protein kinase mediate reactive oxygen species-dependent regulation of platelet-derived growth factor-induced smooth muscle cell migration. Circ Res. 2004;94:1219-26 pubmed
    ..the Src- and Rac-effector p21-activated protein kinase (PAK) 1 on Thr423 (the phosphoinositide-dependent kinase-1 [PDK1] site) was attenuated by ROS inhibition, and infection of VSMCs with dominant-negative PAK1 adenovirus attenuated ..
  20. Alessi D, Deak M, Casamayor A, Caudwell F, Morrice N, Norman D, et al. 3-Phosphoinositide-dependent protein kinase-1 (PDK1): structural and functional homology with the Drosophila DSTPK61 kinase. Curr Biol. 1997;7:776-89 pubmed
    ..We recently identified a protein kinase, termed PDK1, that phosphorylates PKB at Thr308 only in the presence of lipid vesicles containing phosphatidylinositol 3,4,5-..
  21. Eser S, Reiff N, Messer M, Seidler B, Gottschalk K, Dobler M, et al. Selective requirement of PI3K/PDK1 signaling for Kras oncogene-driven pancreatic cell plasticity and cancer. Cancer Cell. 2013;23:406-20 pubmed publisher
    ..We show that cell-autonomous phosphoinositide 3-kinase (PI3K) and 3-phosphoinositide-dependent protein kinase 1 (PDK1), but not Craf, are key effectors of oncogenic Kras in the pancreas, mediating cell plasticity, acinar-to-ductal ..
  22. Anderson K, Coadwell J, Stephens L, Hawkins P. Translocation of PDK-1 to the plasma membrane is important in allowing PDK-1 to activate protein kinase B. Curr Biol. 1998;8:684-91 pubmed
    ..In response to PDGF, binding of Ptdlns (3,4,5)P3 and/or Ptdlns(3,4)P2 to the PH domain of PDK-1 causes its translocation to the plasma membrane where it co-localises with PKB, significantly contributing to the scale of PKB activation. ..
  23. Xie Z, Yuan H, Yin Y, Zeng X, Bai R, Glazer R. 3-phosphoinositide-dependent protein kinase-1 (PDK1) promotes invasion and activation of matrix metalloproteinases. BMC Cancer. 2006;6:77 pubmed
    ..b>PDK1 is a key molecule that couples PI3K to cell proliferation and survival signals in response to growth factor ..
  24. Pearn L, Fisher J, Burnett A, Darley R. The role of PKC and PDK1 in monocyte lineage specification by Ras. Blood. 2007;109:4461-9 pubmed
    ..We further show that Ras promoted the expression of the AGC kinase master regulator, PDK1, which maintains the stability and activity of PKC isoforms...
  25. Pullen N, Dennis P, Andjelkovic M, Dufner A, Kozma S, Hemmings B, et al. Phosphorylation and activation of p70s6k by PDK1. Science. 1998;279:707-10 pubmed
    ..kinase B (PKB), Thr308, has been shown to be phosphorylated by the phosphoinositide-dependent protein kinase PDK1. A regulatory link between p70s6k and PKB was demonstrated, as PDK1 was found to selectively phosphorylate p70s6k ..
  26. Freeley M, Park J, Yang K, Wange R, Volkov Y, Kelleher D, et al. Loss of PTEN expression does not contribute to PDK-1 activity and PKC activation-loop phosphorylation in Jurkat leukaemic T cells. Cell Signal. 2007;19:2444-57 pubmed
    ..We conclude therefore that loss of PTEN expression in Jurkat T cells does not impact on the PDK-1/PKC pathway and that only a subset of kinases, such as PKB/Akt, are perturbed as a consequence PTEN loss. ..
  27. Kurata A, Katayama R, Watanabe T, Tsuruo T, Fujita N. TUSC4/NPRL2, a novel PDK1-interacting protein, inhibits PDK1 tyrosine phosphorylation and its downstream signaling. Cancer Sci. 2008;99:1827-34 pubmed publisher
    3-Phosphoinositide-dependent protein kinase-1 (PDK1) is a key regulator of cell proliferation and survival signal transduction...
  28. Ding Z, Liang J, Li J, Lu Y, Ariyaratna V, Lu Z, et al. Physical association of PDK1 with AKT1 is sufficient for pathway activation independent of membrane localization and phosphatidylinositol 3 kinase. PLoS ONE. 2010;5:e9910 pubmed publisher
    ..phosphate-mediated recruitment of AKT and its upstream kinases, including 3-Phosphoinositide-dependent kinase 1 (PDK1), to the inner surface of the cell membrane...
  29. Alessi D, James S, Downes C, Holmes A, Gaffney P, Reese C, et al. Characterization of a 3-phosphoinositide-dependent protein kinase which phosphorylates and activates protein kinase Balpha. Curr Biol. 1997;7:261-9 pubmed
    ..were effective in potently activating the kinase, which has been named PtdIns(3,4,5)P3-dependent protein kinase-1 (PDK1)...
  30. Shen X, Xi G, Radhakrishnan Y, Clemmons D. PDK1 recruitment to the SHPS-1 signaling complex enhances insulin-like growth factor-i-stimulated AKT activation and vascular smooth muscle cell survival. J Biol Chem. 2010;285:29416-24 pubmed publisher
    ..Therefore, we investigated the mechanism of PDK1 recruitment to the SHPS-1 signaling complex and the consequences of disrupting PDK1 recruitment for downstream ..
  31. Gao X, Harris T. Steady-state kinetic mechanism of PDK1. J Biol Chem. 2006;281:21670-81 pubmed
    b>PDK1 catalyzes phosphorylation of Thr in the conserved activation loop region of a number of its downstream AGC kinase family members...
  32. Persad S, Attwell S, Gray V, Mawji N, Deng J, Leung D, et al. Regulation of protein kinase B/Akt-serine 473 phosphorylation by integrin-linked kinase: critical roles for kinase activity and amino acids arginine 211 and serine 343. J Biol Chem. 2001;276:27462-9 pubmed
    ..These data demonstrate that ILK is an important upstream kinase for the regulation of PKB/Akt. ..
  33. Pinner S, Sahai E. PDK1 regulates cancer cell motility by antagonising inhibition of ROCK1 by RhoE. Nat Cell Biol. 2008;10:127-37 pubmed publisher
    ..In this study, we show that PDK1 is required for phosphorylation of myosin light chain and cell motility, both on deformable gels and in vivo...
  34. Jensen C, Buch M, Krag T, Hemmings B, Gammeltoft S, Frodin M. 90-kDa ribosomal S6 kinase is phosphorylated and activated by 3-phosphoinositide-dependent protein kinase-1. J Biol Chem. 1999;274:27168-76 pubmed
    ..Here, we show that the isolated N-terminal kinase of RSK2 (amino acids 1-360) is phosphorylated at Ser(227) by PDK1, a constitutively active kinase, leading to 100-fold stimulation of kinase activity...
  35. Casamayor A, Morrice N, Alessi D. Phosphorylation of Ser-241 is essential for the activity of 3-phosphoinositide-dependent protein kinase-1: identification of five sites of phosphorylation in vivo. Biochem J. 1999;342 ( Pt 2):287-92 pubmed
    3-phosphoinositide-dependent protein kinase-1 (PDK1) expressed in unstimulated 293 cells was phosphorylated at Ser-25, Ser-241, Ser-393, Ser-396 and Ser-410 and the level of phosphorylation of each site was unaffected by stimulation with ..
  36. del Peso L, Gonzalez Garcia M, Page C, Herrera R, Nunez G. Interleukin-3-induced phosphorylation of BAD through the protein kinase Akt. Science. 1997;278:687-9 pubmed
    ..Thus, the proapoptotic function of BAD is regulated by the PI 3-kinase-Akt pathway. ..
  37. Rigatti M, Le A, Gerber C, Moraru I, Dodge Kafka K. Phosphorylation state-dependent interaction between AKAP7δ/γ and phospholamban increases phospholamban phosphorylation. Cell Signal. 2015;27:1807-15 pubmed publisher
  38. Jacob J, Sakakibara K, Mischel R, Henderson G, Dewey W, Akbarali H. Ethanol Reversal of Oxycodone Tolerance in Dorsal Root Ganglia Neurons. Mol Pharmacol. 2018;93:417-426 pubmed publisher
  39. Cherla R, Zhang Y, Ledbetter L, Zhang G. Coxiella burnetii Inhibits Neutrophil Apoptosis by Exploiting Survival Pathways and Antiapoptotic Protein Mcl-1. Infect Immun. 2018;86: pubmed publisher
  40. Velagapudi S, Luo Y, Tran T, Haniff H, Nakai Y, Fallahi M, et al. Defining RNA-Small Molecule Affinity Landscapes Enables Design of a Small Molecule Inhibitor of an Oncogenic Noncoding RNA. ACS Cent Sci. 2017;3:205-216 pubmed publisher
  41. Nandipati K, Subramanian S, Agrawal D. Protein kinases: mechanisms and downstream targets in inflammation-mediated obesity and insulin resistance. Mol Cell Biochem. 2017;426:27-45 pubmed publisher
    ..This review is focused on the protein kinases involved in the inflammatory cascade and molecular mechanisms and their downstream targets with special reference to obesity-induced T2-DM. ..
  42. Fan X, Tian C, Wang H, Xu Y, Ren K, Zhang B, et al. Activation of the AMPK-ULK1 pathway plays an important role in autophagy during prion infection. Sci Rep. 2015;5:14728 pubmed publisher
    ..These results showed that, in addition to the abolishment of the mTOR regulatory pathway, activation of the AMPK-ULK1 pathway during prion infection contributes to autophagy activation in prion-infected brain tissues. ..
  43. Chen C, Zhang S, Liu Z, Tian Y, Sun Q. Cadmium toxicity induces ER stress and apoptosis via impairing energy homoeostasis in cardiomyocytes. Biosci Rep. 2015;35: pubmed publisher
    ..Our work will help to reveal a novel mechanism to clarify the role of cadmium toxicity to cardiomyocytes and provide new possibilities for the treatment of cardiovascular diseases related to cadmium toxicity. ..
  44. Kim S, Kim J, Won J, Song Y. Characterization of the rapamycin-inducible EBV LMP1 activation system. J Microbiol. 2015;53:732-8 pubmed publisher
    ..In the current study, a ligand-dependent activation system for LMP1 using rapamycin-inducible dimerization was generated to delineate the LMP1 signaling pathway. ..
  45. Pastor Flores D, Ferrer Dalmau J, Bahí A, Boleda M, Biondi R, Casamayor A. Depletion of yeast PDK1 orthologs triggers a stress-like transcriptional response. BMC Genomics. 2015;16:719 pubmed publisher
    Pkh proteins are the PDK1 orthologs in S. cerevisiae. They have redundant and essential activity and are responsible for the phosphorylation of several members of the AGC family of protein kinases...
  46. Bhalla N, Di Lorenzo M, Estrela P, Pula G. Semiconductor technology in protein kinase research and drug discovery: sensing a revolution. Drug Discov Today. 2017;22:204-209 pubmed publisher
    ..Here, we describe current techniques and novel applications of semiconductor technologies in protein kinase inhibitor drug discovery. ..
  47. Shen T, Alvarez Garcia O, Li Y, Olmer M, Lotz M. Suppression of Sestrins in aging and osteoarthritic cartilage: dysfunction of an important stress defense mechanism. Osteoarthritis Cartilage. 2017;25:287-296 pubmed publisher
    ..Sesn support chondrocyte survival under stress conditions and promote autophagy activation through modulating mTOR activity. Suppression of Sesn in OA cartilage contributes to deficiency in an important cellular homeostasis mechanism. ..
  48. Chen S, Fang X, Zhang J, Ma Y, Tang X, Zhou Z, et al. Lycorine protects cartilage through suppressing the expression of matrix metalloprotenases in rat chondrocytes and in a mouse osteoarthritis model. Mol Med Rep. 2016;14:3389-96 pubmed publisher
  49. Zhang Y, Mei H, Shan W, Shi L, Chang X, Zhu Y, et al. Lentinan protects pancreatic ? cells from STZ-induced damage. J Cell Mol Med. 2016;20:1803-12 pubmed publisher
  50. Ren C, Li X, Xie Y, Fu H, Yan Z, Zhu Y. RNAi of Grp78 may disturb the fusion of ICR mouse palate cultured in vitro. Hum Exp Toxicol. 2017;:960327117692132 pubmed publisher
    ..By the system of RNAi strategies with mouse palate culture, we found the siRNA of Grp78 disturbed the fusion of mouse palate cultured in vitro...
  51. Menon B, Gulappa T, Menon K. miR-122 Regulates LH Receptor Expression by Activating Sterol Response Element Binding Protein in Rat Ovaries. Endocrinology. 2015;156:3370-80 pubmed publisher
    ..These results conclusively show that miR-122 plays a regulatory role in LH/hCG-induced LHR mRNA down-regulation by increasing LRBP expression through the activation of SREBP pathway. ..
  52. Shim H, Jang S, Jang D, Jin Y, Chang W, Park J, et al. mGlu1 receptor mediates homeostatic control of intrinsic excitability through Ih in cerebellar Purkinje cells. J Neurophysiol. 2016;115:2446-55 pubmed publisher
  53. Yang Y, Xiong D, Yao L, Zhao C. An SNP in Exon 11 of Chicken 5'-AMP-Activated Protein Kinase Gamma 3 Subunit Gene was Associated with Meat Water Holding Capacity. Anim Biotechnol. 2016;27:13-6 pubmed publisher
    ..And locus V315 M was associated with water holding capacity significantly (P < 0.05). The studied polymorphic locus has the potential to be used as a genetic marker for poultry breeding work. ..
  54. Tang F, Pacheco M, Chen P, Liang D, Li W. Secretogranin III promotes angiogenesis through MEK/ERK signaling pathway. Biochem Biophys Res Commun. 2018;495:781-786 pubmed publisher
    ..Furthermore, ERK inhibitor SCH772984 also suppressed Scg3-induced proliferation and migration of HUVECs. Taken together, these findings suggest that MEK-ERK pathway plays an important role in Scg3-induced angiogenesis. ..
  55. Xu S, Niu P, Chen K, Xia Y, Yu Q, Liu N, et al. The liver protection of propylene glycol alginate sodium sulfate preconditioning against ischemia reperfusion injury: focusing MAPK pathway activity. Sci Rep. 2017;7:15175 pubmed publisher
    ..PSS protected the liver from IR injury by suppressing the MAPK signaling and down-regulating inflammation, apoptosis, and autophagy. ..
  56. Li B, Wang F, Liu N, Shen W, Huang T. Astragaloside IV inhibits progression of glioma via blocking MAPK/ERK signaling pathway. Biochem Biophys Res Commun. 2017;491:98-103 pubmed publisher
    ..Taken together our study has identified a novel function of AS-IV and provided a molecular basis for AS-IV potential applications in the treatment of glioma and other cancers. ..
  57. Han F, Xue M, Chang Y, Li X, Yang Y, Sun B, et al. Triptolide Suppresses Glomerular Mesangial Cell Proliferation in Diabetic Nephropathy Is Associated with Inhibition of PDK1/Akt/mTOR Pathway. Int J Biol Sci. 2017;13:1266-1275 pubmed publisher
    ..However, the specific mechanisms and therapies remain unclear. PDK1 is a critical regulator of cell proliferation, but the specific role of PDK1 in diabetic nephropathy has not been ..
  58. van Vliet A, Agostinis P. PERK and filamin A in actin cytoskeleton remodeling at ER-plasma membrane contact sites. Mol Cell Oncol. 2017;4:e1340105 pubmed publisher
    ..We uncovered that PERK, by interacting with Filamin A, elicits F-actin remodeling required for ER-plasma membrane contact site formation after ER-Ca2+ depletion, through a UPR-independent mechanism...
  59. Bansal A, Molina Cruz A, Brzostowski J, Mu J, Miller L. Plasmodium falciparum Calcium-Dependent Protein Kinase 2 Is Critical for Male Gametocyte Exflagellation but Not Essential for Asexual Proliferation. MBio. 2017;8: pubmed publisher
    ..Moreover, molecular understanding of the signaling pathway of PfCDPK2 may provide additional targets for malaria control. ..
  60. Liang Z, Li T, Jiang S, Xu J, Di W, Yang Z, et al. AMPK: a novel target for treating hepatic fibrosis. Oncotarget. 2017;8:62780-62792 pubmed publisher
    ..Finally, we summarize and briefly explain the current objections to targeting AMPK. This review may aid clinical and basic research on AMPK, which may be a novel drug candidate for hepatic fibrosis...
  61. Ha T, Ko W, Lee S, Kim Y, Son J, Sohn J, et al. Anti-Inflammatory Effects of Curvularin-Type Metabolites from a Marine-Derived Fungal Strain Penicillium sp. SF-5859 in Lipopolysaccharide-Induced RAW264.7 Macrophages. Mar Drugs. 2017;15: pubmed publisher
  62. Lee S, Kim D, Kang J, Kim E, Kim W, Youn H, et al. Surfactant Protein B Suppresses Lung Cancer Progression by Inhibiting Secretory Phospholipase A2 Activity and Arachidonic Acid Production. Cell Physiol Biochem. 2017;42:1684-1700 pubmed publisher
    ..Our results revealed that down-regulation of SP-B was involved in the radiation-induced metastatic conversion of NSCLC and provided evidence that SP-B acted as a suppressor of NSCLC progression. ..
  63. Sigala I, Ganidis G, Thysiadis S, Zografos A, Giannakouros T, Sarli V, et al. Lynamicin D an antimicrobial natural product affects splicing by inducing the expression of SR protein kinase 1. Bioorg Med Chem. 2017;25:1622-1629 pubmed publisher
    ..We provide evidence that this effect is mainly due to the ability of lynamicin D to alter the levels of SRPK1, the key kinase involved in both constitutive and alternative splicing. ..
  64. Zhao F, Zhang J, Zhang L, Hao Y, Shi C, Xia G, et al. Discovery and optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase. Bioorg Med Chem. 2016;24:4281-4290 pubmed publisher
    ..45nM) and cellular (IC50=24.7nM in H1993 cell line) assays, as well as exquisite selectivity and satisfactory metabolic stability in human and rat liver microsomes. ..
  65. Chen Y, Tsai C, Shen C, Day C, Yeh Y, Chen R, et al. Palmitic acid interferes with energy metabolism balance by adversely switching the SIRT1-CD36-fatty acid pathway to the PKC zeta-GLUT4-glucose pathway in cardiomyoblasts. J Nutr Biochem. 2016;31:137-49 pubmed publisher
    ..In conclusion, PA and high-fat diets cause lipotoxicity in vivo and in vitro and adversely switch the energy source from the CD36 pathway to the GLUT4 pathway. ..
  66. Li X, Liu R, Luo L, Yu L, Chen X, Sun L, et al. Role of AMP-activated protein kinase ?1 in 17?-ethinylestradiol-induced cholestasis in rats. Arch Toxicol. 2017;91:481-494 pubmed publisher
    ..AMPK?1 may represent an important therapeutic target for estrogen-induced cholestasis. ..
  67. Butler R, Ehling S, Barbar M, Thomas J, Hughes M, Smith C, et al. Distinct neuronal populations in the basolateral and central amygdala are activated with acute pain, conditioned fear, and fear-conditioned analgesia. Neurosci Lett. 2017;661:11-17 pubmed publisher
    ..This information will be important in developing novel therapies for treating pain and emotive disorders in humans. ..
  68. Deng J, Zeng L, Lai X, Li J, Liu L, Lin Q, et al. Metformin protects against intestinal barrier dysfunction via AMPK?1-dependent inhibition of JNK signalling activation. J Cell Mol Med. 2018;22:546-557 pubmed publisher
    ..These findings highlight metformin protects against intestinal barrier dysfunction. The potential mechanism may involve in the inhibition of JNK activation via an AMPK?1-dependent signalling pathway. ..
  69. Che Y, Wang Q, Xiao R, Zhang J, Zhang Y, Gu W, et al. Kudinoside-D, a triterpenoid saponin derived from Ilex kudingcha suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes. Fitoterapia. 2018;125:208-216 pubmed publisher
    ..And the current findings demonstrated that KD-D was a potential therapeutic candidate for alleviating obesity and hyperlipidemia. ..
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