83103-21-3Relevant articles and documents
RGDV-modified gemcitabine: A nano-medicine capable of prolonging half-life, overcoming resistance and eliminating bone marrow toxicity of gemcitabine
Liu, Wenchao,Mao, Yujia,Zhang, Xiaoyi,Wang, Yaonan,Wu, Jianhui,Zhao, Shurui,Peng, Shiqi,Zhao, Ming
, p. 7263 - 7279 (2019)
Background: Gemcitabine has been widely used as a chemotherapeutic drug. However, drug resistance, short half-life and side effects seriously decrease its chemotherapeutic efficacy. Purpose: The object of preparing RGDV-gemcitabine was to prolong the half
IQCA-TASS: a nano-scaled P-selectin inhibitor capable of targeting thrombus and releasing IQCA/TARGD(S)S in vivo
Wu, Jianhui,Zhu, Haimei,Zhao, Ming,Wang, Yuji,Yang, Guodong,Wang, Yaonan,Zhao, Shurui,Gui, Lin,Zhang, Xiaoyi,Peng, Shiqi
, p. 917 - 927 (2017/02/10)
Thrombosis is a serious threat to human health worldwide. Tetrahydroisoquinoline-3-carboxylic acid (IQCA) is an antithrombotic agent, while Thr-Ala-Arg-Gly-Asp(Ser)-Ser (TASS) can target thrombus. Herein, tetrahydro-isoquinoline-3-carbonyl-Thr-Ala-Arg-Gly-Asp(Ser)-Ser (IQCA-TASS) was designed with the aim towards the discovery of a nano-delivery system for targeting thrombus. In vitro, IQCA-TASS acted on P-selectin and down-regulated P-selectin expression. The IC50 values of IQCA-TASS against the platelet aggregation induced by four aggregators were less than 0.45 nM. In vivo, IQCA-TASS targeted thrombus, released IQCA and TASS inside the thrombus, showed dose-dependent anti-thrombotic action, of which the minimal effective dose was 1 nmol kg-1, and showed anti-inflammatory action. Even with the dose up to 1 μmol kg-1, a dose of 1000 times the minimal effective dose, IQCA-TASS still induced no toxic reaction. In rat plasma, IQCA-TASS formed nanoparticles with diameters of less than 41 nm. The interactions of the nanoparticles with both resting and activated platelets were imaged. IQCA-TASS should be a safe nano-medicine capable of targeting thrombus and releasing anti-thrombotic/anti-inflammatory pharmacophores in disease sites.
RGD-fatty alcohol-modified docetaxel liposomes improve tumor selectivity in vivo
Li, Yinghuan,Zheng, Xuelian,Sun, Yi,Ren, Zhao,Li, Xuemei,Cui, Guohui
, p. 133 - 141 (2014/05/20)
The tripeptide arginine-glycine-aspartate (RGD) was conjugated with various fatty alcohols to obtain RGDOCnH2n + 1 (n = 8, 10, 12, 14, 16, 18), which were incorporated into the bilayer of docetaxel liposomes to improve their tumor sp