Identification of a small molecule activator of novel PKCs for promoting glucose-dependent insulin secretion

Cell Research

Volumn 21, Issue 4, 2011, Pages 588-599

  Han, Shuai ^a   Pan, Heling ^b   Zhang, Jianhua ^a   Tan, Li ^b   Ma, Dawei ^b   Yuan, Junying ^c   Wu, Jia Rui ^a,d  

^a Shanghai Jiao Tong University Affiliated Sixth People s Hospital   (China)

^b SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY   (China)

^c HARVARD MEDICAL SCHOOL   (United States)

^d UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA   (China)

Author keywords

glucose dependency; Golgi; insulin secretion; PKC

Indexed keywords

RATTUS;

EID: 85027920383     PISSN: 10010602     EISSN: 17487838     Source Type: Journal    
DOI: 10.1038/cr.2010.137     Document Type: Article

References (38)

1. Straub SG, Sharp GW. Glucose-stimulated signaling pathways in biphasic insulin secretion. Diabetes Metab Res Rev 2002; 18:451-463. (Pubitemid 36041600)
2. Henquin JC. Triggering and amplifying pathways of regulation of insulin secretion by glucose. Diabetes 2000; 49:1751-1760.
3. Henquin JC. Pathways in β-cell stimulus-secretion coupling as targets for therapeutic insulin secretagogues. Diabetes 2004; 53 Suppl 3:S48-S58.
4. Gembal M, Detimary P, Gilon P, Gao ZY, Henquin JC. Mechanisms by which glucose can control insulin release independently from its action on adenosine triphosphate-sensitive K+ channels in mouse B cells. J Clin Invest 1993; 91:871-880. (Pubitemid 23095261)
5. Knutson KL, Hoenig M. Identification and subcellular characterization of protein kinase-C isoforms in insulinoma β-cells and whole islets. Endocrinology 1994; 135:881-886. (Pubitemid 24271175)
6. Zawalich WS, Zawalich KC. Effects of protein kinase C inhibitors on insulin secretory responses from rodent pancreatic islets. Mol Cell Endocrinol 2001; 177:95-105. (Pubitemid 32506810)
7. Uchida T, Iwashita N, Ohara-Imaizumi M, et al. Protein kinase Cδ plays a non-redundant role in insulin secretion in pancreatic β cells. J Biol Chem 2007; 282:2707-2716. (Pubitemid 47076769)
8. Mendez CF, Leibiger IB, Leibiger B, et al. Rapid association of protein kinase C-ε with insulin granules is essential for insulin exocytosis. J Biol Chem 2003; 278:44753-44757. (Pubitemid 37377233)
9. Warwar N, Efendic S, Ostenson CG, Haber EP, Cerasi E, Nesher R. Dynamics of glucose-induced localization of PKC isoenzymes in pancreatic β-cells: diabetes-related changes in the GK rat. Diabetes 2006; 55:590-599. (Pubitemid 43343214)
10. Yedovitzky M, Mochly-Rosen D, Johnson JA, et al. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic β-cells. J Biol Chem 1997; 272:1417-1420. (Pubitemid 27043212)
11. Pan H, Yu J, Zhang L, et al. A novel small molecule regulator of guanine nucleotide exchange activity of the ADP-ribosylation factor and golgi membrane trafficking. J Biol Chem 2008; 283:31087-31096.
12. Hauri HP, Kappeler F, Andersson H, Appenzeller C. ERGIC-53 and traffic in the secretory pathway. J Cell Sci 2000; 113:587-596. (Pubitemid 30133037)
13. Ma D, Zhang T, Wang G, Kozikowski AP, Lewin NE, Blumberg PM. Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C. Bioorg Med Chem Lett 2001; 11:99-101. (Pubitemid 32099618)
14. Ma D, Tang G, Kozikowski AP. Synthesis of 7-substituted benzolactam-V8s and their selectivity for protein kinase C isozymes. Org Lett 2002; 4:2377-2380.
15. Nakamura N, Rabouille C, Watson R, et al. Characterization of a cis-Golgi matrix protein, GM130. J Cell Biol 1995; 131:1715-1726. (Pubitemid 26007969)
16. Sullivan BM, Harrison-Lavoie KJ, Marshansky V, et al. RGS4 and RGS2 bind coatomer and inhibit COPI association with Golgi membranes and intracellular transport. Mol Biol Cell 2000; 11:3155-3168. (Pubitemid 32107090)
17. Warner CL, Stewart A, Luzio JP, et al. Loss of myosin VI reduces secretion and the size of the Golgi in fibroblasts from Snell's waltzer mice. EMBO J 2003; 22:569-579. (Pubitemid 36193601)
18. Blackshear PJ. The MARCKS family of cellular protein kinase C substrates. J Biol Chem 1993; 268:1501-1504. (Pubitemid 23033530)
19. Steinberg SF. Structural basis of protein kinase C isoform function. Physiol Rev 2008; 88:1341-1378.
20. Gould CM, Newton AC. The life and death of protein kinase C. Curr Drug Targets 2008; 9:614-625.
21. Newton AC. Protein kinase C: structure, function, and regulation. J Biol Chem 1995; 270:28495-28498.
22. + channels in mouse B cells. J Clin Invest 1992; 89:1288-1295.
23. Zawalich WS, Zawalich KC. Species differences in the induction of time-dependent potentiation of insulin secretion. Endocrinology 1996; 137:1664-1669. (Pubitemid 26133939)
24. Carpenter L, Mitchell CJ, Xu ZZ, Poronnik P, Both GW, Biden TJ. PKCα is activated but not required during glucose-induced insulin secretion from rat pancreatic islets. Diabetes 2004; 53:53-60. (Pubitemid 38044697)
25. Schmitz-Peiffer C, Laybutt DR, Burchfield JG, et al. Inhibition of PKCε improves glucose-stimulated insulin secretion and reduces insulin clearance. Cell Metab 2007; 6:320-328. (Pubitemid 47450184)
26. Cantley J, Burchfield JG, Pearson GL, Schmitz-Peiffer C, Leitges M, Biden TJ. Deletion of PKCε selectively enhances the amplifying pathways of glucose-stimulated insulin secretion via increased lipolysis in mouse β-cells. Diabetes 2009; 58:1826-1834.
27. 2+-secretion coupling is impaired in diabetic Goto Kakizaki rats. J Gen Physiol 2007; 129:493-508.
28. Bisbis S, Bailbe D, Tormo MA, et al. Insulin resistance in the GK rat: decreased receptor number but normal kinase activity in liver. Am J Physiol 1993; 265:E807-813.
29. Griffin ME, Marcucci MJ, Cline GW, et al. Free fatty acid-induced insulin resistance is associated with activation of protein kinase C theta and alterations in the insulin signaling cascade. Diabetes 1999; 48:1270-1274. (Pubitemid 29241025)
30. Schmitz-Peiffer C, Browne CL, Oakes ND, et al. Alterations in the expression and cellular localization of protein kinase C isozymes epsilon and theta are associated with insulin resistance in skeletal muscle of the high-fat-fed rat. Diabetes 1997; 46:169-178. (Pubitemid 27272248)
31. Itani SI, Ruderman NB, Schmieder F, Boden G. Lipid-induced insulin resistance in human muscle is associated with changes in diacylglycerol, protein kinase C, and IkappaB-alpha. Diabetes 2002; 51:2005-2011. (Pubitemid 34729001)
32. Yu C, Chen Y, Cline GW, et al. Mechanism by which fatty acids inhibit insulin activation of insulin receptor substrate-1 (IRS-1)-associated phosphatidylinositol 3-kinase activity in muscle. J Biol Chem 2002; 277:50230-50236. (Pubitemid 36042170)
33. Dey D, Basu D, Roy SS, Bandyopadhyay A, Bhattacharya S. Involvement of novel PKC isoforms in FFA induced defects in insulin signaling. Mol Cell Endocrinol 2006; 246:60-64. (Pubitemid 43238397)
34. Mack E, Ziv E, Reuveni H, et al. Prevention of insulin resistance and beta-cell loss by abrogating PKCε-induced serine phosphorylation of muscle IRS-1 in Psammomys obesus. Diabetes Metab Res Rev 2008; 24:577-584.
35. Merglen A, Theander S, Rubi B, Chaffard G, Wollheim CB, Maechler P. Glucose sensitivity and metabolism-secretion coupling studied during two-year continuous culture in INS-1E insulinoma cells. Endocrinology 2004; 145:667-678. (Pubitemid 38183809)
36. Zhang L, Yu J, Pan H, et al. Small molecule regulators of autophagy identified by an image-based high-throughput screen. Proc Natl Acad Sci USA 2007; 104:19023-19028.
37. Lacy PE, Kostianovsky M. Method for the isolation of intact islets of Langerhans from the rat pancreas. Diabetes 1967; 16:35-39.
38. Lacy PE, Walker MM, Fink CJ. Perifusion of isolated rat islets in vitro. Participation of the microtubular system in the biphasic release of insulin. Diabetes 1972; 21:987-998.