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溴酚化合物ptp1b抑制活性与松节藻提取物在糖尿病大鼠体内降血糖活性.pdf

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1、 2008 年 第 53 卷 第 10 期 : 1196 1199 1196 uS Sv SCIENCE IN CHINA PRESS pPTP1B (4 | Uhv 8 = Nv, , , , Sk, b ,* S SZ , 266071; vD D, 266003 *“ , E-mail: 2007-11-08 l, 2008-04-23 s SE/ ?Z9( |: 2007AA09Z410 2007AA091604)S S M7( |: KZCX2-YW-209) “ K1 1B (PTP1B) O |V1 ey0, PTP1B 2 Uhr. Z( ( Rhodomela conf

2、ervoides 4p , 2,2 ,3,3- -4,4,5,5- =&J( 1), 3- -4,5-(2,3-= -4,5-=)- #&=p (2), -(2,3-= -4,5-=)- ( 3) 2,2,3- -3,4,4,5- -6 -YJ=&J (4), VC 500) aa T“ l, / % Yi. Z( ( 4 p 8 k, TV , VC PTP1B (IC50sY 2.4, 1.7, 1.5 0.84 mol/L). Ja Q ) 1199 2 Uhv (Y?4 | 8= L, TA U , Uh FM1, Z(?4 |a4 FVCA r . N , $4 LV , (?4 |

3、 . V , (?4 |8 = zr V ?sYVp PTP1B o T, T2DM 0 7? 1il. ID 1 ORahilly S, Barroso I, Wareham N J. Genetic factors in type 2 diabetes: The end of the beginning? Science, 2005, 307: 370373 doi 2 Lowell B B, Shulman G L. Mitochondrial dysfunction and type 2 diabetes. Science, 2005, 307: 384387 doi 3 Dadke

4、S, Kusari J, Chernoff J. Down-regulation of insulin signalling by protein-tyrosine phosphatase 1B is mediated by an N-terminal binding region. J Biol Chem, 2000, 275: 2364223647 doi 4 Walchli S, Walchli S, Curchod M L, et al. Identification of tyrosine phosphatases that dephosphorylate the insulin r

5、eceptor: A brute-force approach based on substrate trapping mutants. J Biol Chem, 2000, 275: 97929796 doi 5 Goldstein B J, Bittner-Kowalczyk A, White M F, et al. Tyrosine dephosphorylation and deactivation of insulin receptor substrate-1 by protein-tyrosine phosphatase 1B. Possible facilitation by t

6、he formation of a ternary complex with the Grb2 adaptor protein. J Biol Chem, 2000, 275: 42834289 doi 6 Calera M R, Vallega G, Pilch P F. Dynamics of protein-tyrosine phosphatases in rat adipocytes. J Biol Chem, 2000, 275: 63086312doi 7 Elchebly M, Payette P, Michaliszyn E, et al. Increased insulin

7、sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase-1B gene. Science, 1999, 283: 15441548 doi 8 Fan X, Xu N J, Shi J G. Bromophenols from the red agla Rhodomela confervoides. J Nat Prod, 2003, 66: 455458 doi 9 Fan X, Xu N J, Shi J G. Two new bromophenols from red alga

8、 Rhodomela confervoids. Chin Chem Lett, 2003, 14(9): 939941 10 Fan X, Xu N J, Shi J G. A new brominated phenylpropylaldehyde and its dimethyl acetal from red alga Rhodomela confervoides. Chin Chem Lett, 2003, 14(10): 10451047 11 Xu N J, Fan X, Yan X J, et al. Antibacterial bromophenols from the mari

9、ne red alga Rhodomela confervoids. Phytochemistry, 2003, 62: 12211224doi 12 Zhao J L, Fan X, Wang S J, et al. Bromophenol derivatives from the red alga Rhodomela confervoids. J Nat Prod, 2004, 67: 10321035doi 13 Zhao J L, Ma M, Wang S J, et al. Bromophenols coupled with derivatives of amino acids an

10、d nucleosides from the red alga Rhodome-la confervoids. J Nat Prod, 2005, 68: 691694 doi 14 Ma M, Zhao J L, Wang S J, et al. Bromophenols coupled with methyl -ureidobutyrate and9 bromophenol sulfates from the red alga Rhodomela confervoides. J Nat Prod, 2006, 68: 206210 doi 15 Ma M, Zhao J L, Wang S

11、 J, et al. Bromophenols coupled with nucleoside bases and brominated tetrahydroisoquinolines from the red alga Rhodomela confervoides. J Nat Prod, 2007, 70: 337341 doi 16 Liu G. Technology evaluation: ISIS-113715. Isis Curr Opin Mol Ther, 2004, 6: 331336 17 Shen K, Keng Y F, Wu L, et al. Acquisition

12、 of a specific and potent PTP1B inhibitor from a novel combinatorial library and screening procedure. J Biol Chem, 2001, 276(50): 4731147319 doi 18 Xie L P, Zhang Z Y, Andersen J N, et al. Cellular effects of small molecule PTP1B inhibitors on insulin signaling. Biochemistry, 2003, 42(44): 1279212804 doi 19 Wiesmann C, Barr K J, Kung J, et al. Allosteric inhibition of protein tyrosine phosphatase 1B. Nat Struct Mol Biol, 2004, 11: 730737doi

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