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大鼠和人类的HARE/稳定素-2是高分子量和低分子量肝素的清除受体。

Rat and human HARE/stabilin-2 are clearance receptors for high- and low-molecular-weight heparins.

作者信息

Harris Edward N, Baggenstoss Bruce A, Weigel Paul H

机构信息

Dept. of Biochemistry, The Oklahoma Center for Medical Glycobiology, Univ. of Oklahoma Health Sciences Center, Oklahoma City, OK 73190, USA.

出版信息

Am J Physiol Gastrointest Liver Physiol. 2009 Jun;296(6):G1191-9. doi: 10.1152/ajpgi.90717.2008. Epub 2009 Apr 9.

Abstract

The human hyaluronic acid (HA) receptor for endocytosis (HARE/stabilin-2) is the primary clearance receptor for systemic HA, chondroitin sulfates, and heparin, but not for heparan sulfate or keratan sulfate (Harris EN, Weigel JA, Weigel PH. J Biol Chem 283: 17341-17350, 2008). HARE is expressed in the sinusoidal endothelial cells (SECs) of liver and lymph nodes where it acts as a scavenger for uptake and degradation of glycosaminoglycans, both as free chains and proteoglycan fragments. Unfractionated heparin (UFH; approximately 14 kDa) and low-molecular-weight heparin (LMWH; approximately 4 kDa) are commonly used in treatments for thrombosis and cancer and in surgical and dialysis procedures. The reported half-lives of UFH and LMWH in the blood are approximately 1 h and 2-6 h, respectively. In this study, we demonstrate that anti-HARE antibodies specifically block the uptake of LMWH and UFH by isolated rat liver SECs and by human 293 cells expressing recombinant human HARE (hHARE). hHARE has a significant affinity (K(d) = 10 microM) for LMWH, and higher affinity (K(d) = 0.06 microM) for the larger UFH. Rat liver SECs or cells expressing the recombinant 190-kDa HARE isoform internalized both UFH and LMWH, and both heparins cross-compete with each other, suggesting that they share the same binding sites. These cellular results were confirmed in ELISA-like assays using purified soluble 190-hHARE ectodomain. We conclude that both UFH and LMWH are cleared by HARE/Stab2 and that the differences in the affinities of HARE binding to LMWH and UFH likely explain the longer in vivo circulating half-life of LMWH compared with UFH.

摘要

人类内吞作用的透明质酸(HA)受体(HARE/稳定素-2)是全身HA、硫酸软骨素和肝素的主要清除受体,但不是硫酸乙酰肝素或硫酸角质素的清除受体(哈里斯EN,韦格尔JA,韦格尔PH。《生物化学杂志》283:17341-17350,2008年)。HARE在肝脏和淋巴结的窦状内皮细胞(SEC)中表达,在那里它作为一种清除剂,用于摄取和降解糖胺聚糖,包括游离链和蛋白聚糖片段。普通肝素(UFH;约14 kDa)和低分子量肝素(LMWH;约4 kDa)常用于血栓形成和癌症的治疗以及外科手术和透析过程。报道的UFH和LMWH在血液中的半衰期分别约为1小时和2-6小时。在本研究中,我们证明抗HARE抗体可特异性阻断分离的大鼠肝脏SEC和表达重组人HARE(hHARE)的人293细胞对LMWH和UFH的摄取。hHARE对LMWH具有显著亲和力(K(d)=10 microM),对较大的UFH具有更高亲和力(K(d)=0.06 microM)。表达重组190-kDa HARE异构体的大鼠肝脏SEC或细胞内化了UFH和LMWH,并且两种肝素相互交叉竞争,表明它们共享相同的结合位点。使用纯化的可溶性190-hHARE胞外域在类似ELISA的试验中证实了这些细胞结果。我们得出结论,UFH和LMWH均由HARE/Stab2清除,并且HARE与LMWH和UFH结合亲和力的差异可能解释了LMWH与UFH相比在体内循环半衰期更长的原因。

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