Pfizer, BioTherapeutics, Biocorrections Research Unit, 200 CambridgePark Drive, Cambridge, MA 02140, USA.
Expert Opin Ther Pat. 2010 Jun;20(6):781-93. doi: 10.1517/13543771003767468.
Selectins play a significant and well-documented role in inflammation and immune response. They initiate tethering and rolling of blood borne leukocytes leading to their activation, adhesion and subsequent extravazation into tissues. This is important for healthy immune response and tissue repair. However, dysregulation of selectins leads to exacerbation of disease. Atherosclerosis, restenosis, deep venous thrombosis and tumor metastasis are just a few of the diseases in which selectin blockade has been demonstrated to ameliorate disease pathology. Thus, selectins remain attractive targets for amelioration of disease.
Summarized here are new patents/patent applications on selectin inhibition published since our last review in 2003 and any significant changes or progress made in demonstrating clinical safety and efficacy of therapeutics covered by patents/patent applications reviewed in 2003.
A comprehensive review of new developments in the field of selectin inhibition through discussion of patents/patent applications from 2003 to August 2009, reports on clinical results where available and selected literature.
The field of selectin inhibition has matured significantly in recent years in the ability to inhibit selectin/ligand interactions with drug-like molecules and to demonstrate disease modification in human trials.
选择素在炎症和免疫反应中起着重要的作用，这一点已得到充分的证明。它们启动了血液白细胞的连接和滚动，导致它们的激活、黏附和随后的渗出到组织中。这对于健康的免疫反应和组织修复是很重要的。然而，选择素的失调会导致疾病恶化。动脉粥样硬化、再狭窄、深静脉血栓形成和肿瘤转移只是几种已经证明通过选择素阻断可以改善疾病病理的疾病。因此，选择素仍然是改善疾病的有吸引力的靶点。
总结了自 2003 年我们上次综述以来发表的关于选择素抑制的新专利/专利申请，以及在 2003 年审查的专利/专利申请中所涵盖的治疗方法的临床安全性和疗效方面取得的任何重大变化或进展。
通过讨论 2003 年至 2009 年 8 月的专利/专利申请，以及可用的临床结果和精选文献，全面了解选择素抑制领域的最新进展。
近年来，选择素抑制领域在使用类似药物的分子抑制选择素/配体相互作用以及在人体试验中证明疾病改善方面取得了显著进展。
