- RGD-peptides modifying dexamethasone: to enhance the anti-inflammatory efficacy and limit the risk of osteoporosis
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Dexamethasone (Dex) is one of the most effective anti-inflammatory glucocorticoids, while the side effect, osteoporosis seriously limits its clinical use. Cell adhesion is involved in the onset of inflammation and osteoporosis, and RGD-peptides are well k
- Yu, Hualong,Mei, Shenghui,Zhao, Li,Zhao, Ming,Wang, Yuji,Zhu, Haimei,Wang, Yaonan,Wu, Jianhui,Cui, Chunying,Xu, Wenyun,Peng, Shiqi
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p. 1345 - 1351
(2015/07/15)
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- Improved anti-osteoporosis potency and reduced endometrial membrane hyperplasia during hormone replacement therapy with estrogen-RGD peptide conjugates
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To improve the specificity and potency of estrogen replacement therapy therapeutics while also minimizing the side effects such as bone resorption and thickening of the uterine wall, a series of novel estrogen-derived conjugates estradiol-3-RGD, estradiol
- Xiong, Yu,Zhao, Ming,Wang, Chao,Heng, Wei Chang,Peng, Shiqi
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p. 3340 - 3353
(2008/02/12)
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- Dual-acting agents that possess free radical scavenging and antithrombotic activities: Design, synthesis, and evaluation of phenolic tetrahydro-β-carboline RGD peptide conjugates
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A new approach to construct a single dual-acting agent is described. Compounds 6a-c are potent free radical scavengers as demonstrated by the EC50 values in PC12 cell survival assay in term of NO, H2O2, and {radical dot}OH scavenging activity. The Ach-induced vaso-relaxation assay further confirms the potent NO scavenging activity of compounds 6a-c. In addition, 6a-c are efficacious in a rat arterial thrombosis, and are active in ADP- or PAF-induced in vitro platelet aggregation assay, suggesting that compounds 6a-c also possess anti-thrombotic activities. Since both free radical and thrombogenesis are important risk factors in myocardial ischemic/reperfusion injuries, these dual-acting agents having both free radical scavenging and antithrombolic activities may potentially be beneficial toward their treatment.
- Bi, Wei,Bi, Lanrong,Cai, Jianhui,Liu, Sanguang,Peng, Shiqi,Fischer, Nicholas O.,Tok, Jeffrey B.-H.,Wang, Guohua
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p. 4523 - 4527
(2007/10/03)
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- Synthesis and antithrombotic activity of carbolinecarboxyl RGD sequence.
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3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid, RGDS, RGDV, RGDF and their linkers were synthesized. The anti-aggregation and adhesion of platelet indicated that the in vitro activities of the linkers remained at the same level as RGDS, RGDV, and
- Lin,Zhao, Ming,Wang, Chao,Peng, Shiqi
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p. 585 - 587
(2007/10/03)
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- Studies on Hybrid Peptides of Fragments from Fibrinogen
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In the present paper the hybrid peptides of P6A and RGD, namely ARPAKRGDS 17, ARPAKRGDV19, ARPAKRGDF 21, QRPAKRGDS 18, QRPAKRGDV 20 and QRPAKRGDF 22, were synthesized via the solution method, segment condensation and TFA/TFMS A-catalyzed deprotection (in
- Zhao, Ming,Peng, Shiqi
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p. 668 - 676
(2007/10/03)
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