(4-[6-(4-isopropoxyphenyl) pyrazolo [1,5-a]pyrimidin- 3-yl] quinoline) is a novel inhibitor of autophagy

British Journal of Pharmacology

Volumn 171, Issue 21, 2014, Pages 4970-4980

  Sheng, Yue ^a   Sun, Bo ^a   Guo, Wen Ting ^a   Liu, Xiao ^a   Wang, Yu Chun ^a   Xie, Xin ^a   Xiao, Xiao Lin ^a   Li, Na ^a   Dong, De Li ^a  

^a HARBIN MEDICAL UNIVERSITY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

4 [6 (4 ISOPROPOXYPHENYL)PYRAZOLO [1,5 A]PYRIMIDIN 3 YL]QUINOLINE; 5 AMINO 4 IMIDAZOLECARBOXAMIDE RIBOSIDE; BONE MORPHOGENETIC PROTEIN 4; GLYCOGEN SYNTHASE KINASE 3; MAMMALIAN TARGET OF RAPAMYCIN; P70S6 KINASE; PROTEIN KINASE B; PROTEIN KINASE B INHIBITOR; PROTEIN SERINE THREONINE KINASE; QUINOLINE DERIVATIVE; RAPAMYCIN; SMALL INTERFERING RNA; UNCLASSIFIED DRUG; DMH1 COMPOUND; PYRAZOLE DERIVATIVE;

ANIMAL CELL; ARTICLE; AUTOPHAGY; AUTOPHAGY INHIBITION; CELL CULTURE; CELL STIMULATION; CONTROLLED STUDY; DRUG MECHANISM; ENZYME ACTIVATION; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; FLUORESCENCE MICROSCOPY; HEART MUSCLE CELL; HELA CELL LINE; HUMAN; HUMAN CELL; MCF 7 CELL LINE; NEWBORN; NONHUMAN; RAT; SIGNAL TRANSDUCTION; STARVATION; TRANSMISSION ELECTRON MICROSCOPY; WESTERN BLOTTING; ANIMAL; DRUG EFFECTS; HT 29 CELL LINE; METABOLISM; PHYSIOLOGY; WISTAR RAT;

ANIMALS; AUTOPHAGY; CELLS, CULTURED; HELA CELLS; HT29 CELLS; HUMANS; MCF-7 CELLS; MYOCYTES, CARDIAC; PROTO-ONCOGENE PROTEINS C-AKT; PYRAZOLES; QUINOLINES; RATS, WISTAR;

EID: 84919338724     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.12821     Document Type: Article

References (22)

1. Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, McGrath JC et al. (2013a). The concise guide to PHARMACOLOGY 2013/14: overview. Br J Pharmacol 170: 1449-1458.
2. Alexander SPH , Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M et al. (2013b). The concise guide to PHARMACOLOGY 2013/14: G protein-coupled receptors. Br J Pharmacol 170: 1459-1581.
3. Arico S, Pet iot A, Bauvy C, Dubbelhuis PF, Meijer AJ, Codogno P et al. (2001). The tumor suppressor PTEN positively regulates macroautophagy by inhibiting the phosphatidylinositol 3-kinase/protein kinase B pathway. J Biol Chem 2 76: 35243-35246.
4. Blommaart EFC, Luiken JJFP, Blommaart PJE, van Woerkom GM, Meijer AJ (1995). Phosphorylation of ribosomal protein S6 is inhibitory for autophagy in isolated rat hepatocytes. J Biol Chem 270: 2320-2326.
5. Cao DJ, Wang ZV, Battiprolu PK, Jiang N, Morales CR, Kong Y et al. (2011). Histone deacetylase (HDAC) inhibitors attenuate cardiac hypertrophy by suppressing autophagy. Proc Natl Acad Sci U S A 108: 4123-4128.
6. Dong DL, Chen C, Huo R, Wang N, Li Z, Tu YJ et al. (2010). Reciprocal repression between microRNA-133 and calcineurin regulates cardiac hypertrophy: a novel mechanism f or progressive cardiac hypertrophy. Hypertension 55: 946-952.
7. Gwinn DM, Shackelford DB, Egan DF, Mihaylova MM, Mery A, Vasquez DS et al. (2008). AMPK phosphorylation of raptor mediates a met abolic checkpoint. Mol Cell 30: 214-226.
8. Hao J, Ho JN, Lewis JA, Karim KA, Daniels RN, Gentry PR et al. (2010). In vivo structure-Activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem Biol 5: 245-253.
9. Jung CH, Ro S-H, Cao J, Otto NM, Kim D-H (2010). mTOR regulation of autophagy. FEBS Lett 584: 1287-1295.
10. Kim J, Kundu M, Viollet B, Guan K-L (2011). AMPK and mTOR regulate autophagy through direct phosphorylation of Ulk1. Nat Cell Biol 13: 132-141.
11. King TD, Song L, Jope RS (2006). AMP-Activated prote in kinase (AMPK) activating agents cause dephosphorylation of Akt and glycogen synthase kinase-3. Biochem Pharmacol 71: 1637-1647.
12. Li J, Qin Z, Liang Z (2009). The prosurvival role of autophagy in resveratrol-induced cytotoxicity in human U251 glioma cells. BMC Cancer 9: 215.
13. Pawson AJ,Sharman JL,Benson HE,Faccenda E,Alexander SP,Buneman OP,Davenport AP,McGrath JC,Peters JA,Southan C,Spedding M,Yu W,Harmar AJ NC-IUPHAR. 2014). The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledge base of drug targets and their ligands. Nucl. Acids Res. 42 (Database Issue): D1098-1106.
14. Sheng Y, Sun B, Guo WT, Zhang YH, Liu X, Xing Y et al. (2013). 3-Methyladenine induces cell death and its interaction with chemotherapeutic drugs is independent of autophagy. Biochem Biophys Res Commun 432: 5-9.
15. Shigemitsu K, Tsujishita Y, Hara K, Nanahoshi M, Avruch J, Yonezawa K (1999). Regulation of translational effectors by amino acid and mammalian target of rapamycin signaling pathways. Possible involve ment of autophagy in cultured hepatoma cells. J Biol Chem 274: 1058-1065.
16. Sun B, Huo R, Sheng Y, Li Y, Xie X, Chen C et al. (2013). Bone Morphogenetic protein-4 mediates cardiac hypertrophy, apo ptosis, and fibrosis in experimentally pathological cardiac hypertrophy novelty and significance. Hypertension 61: 352-360.
17. Vucicevic L, Misirkic M, Kristina J, Vilimanovich U, Sudar E, Isenovic E et al. (2011). Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy 7: 40-50.
18. Wang J, Whiteman MW, Lian H, Wang G, Singh A, Huang D et al. (2009). A non-canonical MEK/ERK signaling pathway regulates autophagy via regulating Beclin 1. J Biol Chem 284: 21412-21424.
19. Wong AS, Lee RH, Cheung AY, Yeung PK, Chung SK, Cheung ZH et al. (2011). Cdk5-mediated phosphorylation of endophilin B1 is required for induced autophagy in models of Parkinson's disease. Nat Cell Biol 13: 568-579.
20. Yang YP, Hu LF, Zheng HF, Mao CJ, Hu WD, Xiong KP et al. (2013). Application and interpretation of current autophagy inhibitors and activators. Acta Pharmacol Sin 34: 625-635.
21. Yang Z, Klionsky DJ (2010). Mammalian autophagy: core molecular machinery and signaling regulation. Curr Opin Cell Biol 22: 124-131.
22. Zhu H, Tannous P, Johnstone JL, Kong Y, Shelton JM, Richardson JA et al. (2007). Cardiac autophagy is a maladapt ive response to hemodynamic stress. J Clin Invest 117: 1782-1793.