Opportunities for functional selectivity in GPCR antibodies.
Opportunities for functional selectivity in GPCR antibodies.
复制标题
DOI：
10.1016/j.bcp.2012.08.021
复制
发表时间：
2013-01-15
影响因子：
5.8
通讯作者：
Stevens, Raymond C.
中科院分区：
文献类型：
--
作者：
Webb, David R.;Handel, Tracy M.;Kretz-Rommel, Anke;Stevens, Raymond C.
几十年来，单克隆抗体（mab）一直被用作探测细胞和组织中受体的生物学和药理学的工具。它们也越来越多地被开发用于临床目的，针对广泛的靶标，尽管相对于其他治疗靶标，G蛋白偶联受体（gpcr）的作用程度较低。最近的药理学、结构和生物物理数据为GPCR功能的分子细节、复杂性和调控提供了大量新的见解。尽管过去认为gpcr具有“开”或“关”构象状态，但现在认识到它们的结构可能被配体和其他相互作用的蛋白质精细调节，从而导致特定信号通路的选择性激活。这些信息与选择靶向gpcr的单克隆抗体的新技术将越来越多地用于开发识别构象决定因素的高选择性单克隆抗体，从而产生新的治疗方法。
Monoclonal antibodies (mAbs) have been used for decades as tools to probe the biology and pharmacology of receptors in cells and tissues. They are also increasingly being developed for clinical purposes against a broad range of targets, albeit to a lesser extent for G protein-coupled receptors (GPCRs) relative to other therapeutic targets. Recent pharmacological, structural and biophysical data have provided a great deal of new insight into the molecular details, complexity and regulation of GPCR function. Whereas GPCRs used to be viewed as having either “on” or “off” conformational states, it is now recognized that their structures may be finely tuned by ligands and other interacting proteins, leading to the selective activation of specific signaling pathways. This information coupled with new technologies for the selection of mAbs targeting GPCRs will be increasingly deployed for the development of highly selective mAbs that recognize conformational determinants leading to novel therapeutics.
登录
查看更多内容
影响因子：
46.9
作者：
通讯作者：
--
DOI：
10.1073/pnas.0812952106
发表时间：
2009-03-03
影响因子：
11.1
作者：
Gao, Junjun;Sidhu, Sachdev S.;Wells, James A.
通讯作者：
Wells, James A.
影响因子：
4.8
作者：
de Haard, HJ;van Neer, N;Hoogenboom, HR
通讯作者：
Hoogenboom, HR
影响因子：
8
作者：
Bailey, BW;Mumey, B;Dratz, EA
通讯作者：
Dratz, EA
影响因子：
3.2
作者：
HICKS, D;BARNSTABLE, CJ
通讯作者：
BARNSTABLE, CJ