Ligand Bias by the Endogenous Agonists of CCR

نویسنده

  • David A. Zidar
چکیده

Ligand Bias by the Endogenous Agonists of CCR7 by David A. Zidar, MD Department of Immunology Duke University Date:_______________________ Approved: ___________________________ Robert J. Lefkowitz, MD, Supervisor ___________________________ Garnett Kelsoe, D.Sc., Chair ___________________________ Yuan Zhuang, Ph. D. ___________________________ Weiguo Zhang, Ph.D. ___________________________ Marc Caron, Ph.D. An abstract of a dissertation submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the Department of Immunology in the Graduate School of Duke University 2009

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Ligand bias at metabotropic glutamate 1a receptors: molecular determinants that distinguish β-arrestin-mediated from G protein-mediated signaling.

The metabotropic glutamate 1a (mGlu1a) receptor is a G protein-coupled receptor linked with phosphoinositide (PI) hydrolysis and with β-arrestin-1-mediated sustained extracellular signal-regulated kinase (ERK) phosphorylation and cytoprotective signaling. Previously, we reported the existence of ligand bias at this receptor, inasmuch as glutamate induced both effects, whereas quisqualate induce...

متن کامل

Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands.

CCL19 and CCL21 are endogenous agonists for the seven-transmembrane receptor CCR7. They are equally active in promoting G protein stimulation and chemotaxis. Yet, we find that they result in striking differences in activation of the G protein-coupled receptor kinase (GRK)/ss-arrestin system. CCL19 leads to robust CCR7 phosphorylation and beta-arrestin2 recruitment catalyzed by both GRK3 and GRK...

متن کامل

The Effective Application of Biased Signaling to New Drug Discovery.

The ability of agonists to selectively activate some but not all signaling pathways linked to pleiotropically signaling receptors has opened the possibility of obtaining molecules that emphasize beneficial signals, de-emphasize harmful signals, and concomitantly deemphasize harmful signals while blocking the harmful signals produced by endogenous agonists. The detection and quantification of bi...

متن کامل

Special issue: Allosterism and Collateral Efficacy b-Arrestin-biased ligands at seven-transmembrane receptors

Agonist: a ligand that, by binding a receptor, increases that receptor’s activity. Antagonist: a ligand that binds a receptor without stimulating any activity. Also known as a ’blocker’ because of its ability to prevent binding of other ligands and, therefore, block agonist-induced activity. Correlated efficacies: when ligand binding stimulates or inhibits all receptor functions to an equal ext...

متن کامل

A novel method for analyzing extremely biased agonism at G protein-coupled receptors.

Seven transmembrane receptors were originally named and characterized based on their ability to couple to heterotrimeric G proteins. The assortment of coupling partners for G protein-coupled receptors has subsequently expanded to include other effectors (most notably the βarrestins). This diversity of partners available to the receptor has prompted the pursuit of ligands that selectively activa...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:

دوره   شماره 

صفحات  -

تاریخ انتشار 2009