scholarly journals Receptor occupancy assessment by flow cytometry as a pharmacodynamic biomarker in biopharmaceutical development

2015 ◽  
Vol 90 (2) ◽  
pp. 117-127 ◽  
Author(s):  
Meina Liang ◽  
Martin Schwickart ◽  
Amy K. Schneider ◽  
Inna Vainshtein ◽  
Christopher Del Nagro ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Receptor Occupancy

A Simple and Rapid Method to Determine GPIIb/IIIa-Receptor Inhibitor Activity in Whole Blood

1999 ◽  
Vol 19 (03) ◽  
pp. 134-138
Author(s):  
Gitta Kühnel ◽  
A. C. Matzdorff
Keyword(s):  
Flow Cytometry ◽  
Platelet Count ◽  
Blood Sample ◽  
Platelet Activation ◽  
Whole Blood ◽  
Receptor Occupancy ◽  
Aggregate Formation ◽  
Inhibitor Activity ◽  
Receptor Inhibitor

SummaryWe studied the effect of GPIIb/IIIa-inhibitors on platelet activation with flow cytometry in vitro. Citrated whole blood was incubated with increasing concentrations of three different GPIIb/IIIa-inhibitors (c7E3, DMP728, XJ757), then thrombin or ADP were added and after 1 min the sample was fixed. Samples without c7E3 but with 0.1 U/ml thrombin had a decrease in platelet count. Samples with increasing concentrations of c7E3 had a lesser or no decrease in platelet count. The two other inhibitors (DMP 725, XJ757) gave similar results. GPIIb/IIIa-inhibitors prevent aggregate formation and more single platelets remain in the blood sample. The agonist-induced decrease in platelet count correlates closely with the concentration of the GPIIb/IIIa inhibitor and receptor occupancy. This correlation may be used as a simple measure for inhibitor activity in whole blood.

scholarly journals Flow cytometry and receptor occupancy in immune-oncology therapy

2021 ◽  
Author(s):  
Alessandra Audia ◽  
Gregory Bannish ◽  
Rachel Bunting ◽  
Chelsea Riveley
Keyword(s):  
Flow Cytometry ◽  
Receptor Occupancy ◽  
Immune Oncology

scholarly journals Recommendations for the development and validation of flow cytometry-based receptor occupancy assays

2016 ◽  
Vol 90 (2) ◽  
pp. 141-149 ◽  
Author(s):  
Cherie L. Green ◽  
Jennifer J. Stewart ◽  
Carl-Magnus Högerkorp ◽  
Alan Lackey ◽  
Nicholas Jones ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Receptor Occupancy ◽  
Development And Validation

Small molecule LFA-1 antagonists compete with an anti-LFA-1 monoclonal antibody for binding to the CD11a I domain: development of a flow-cytometry-based receptor occupancy assay

2003 ◽  
Vol 277 (1-2) ◽  
pp. 101-115 ◽  
Author(s):  
Joseph R. Woska ◽  
Kathleen Last-Barney ◽  
Robert Rothlein ◽  
Rachel R. Kroe ◽  
Patricia L. Reilly ◽  
...  
Keyword(s):  
Monoclonal Antibody ◽  
Flow Cytometry ◽  
Small Molecule ◽  
Receptor Occupancy

Receptor occupancy by flow cytometry

2016 ◽  
Vol 90 (2) ◽  
pp. 108-109 ◽  
Author(s):  
Virginia Litwin ◽  
Cherie Green ◽  
Jennifer J. Stewart
Keyword(s):  
Flow Cytometry ◽  
Receptor Occupancy

Validation of a flow cytometry-based assay to assess C5aR receptor occupancy on neutrophils and monocytes for use in drug development

2015 ◽  
Vol 90 (2) ◽  
pp. 177-190 ◽  
Author(s):  
Karen J. Quadrini ◽  
Anne Charlotte Hegelund ◽  
Kasia E. Cortes ◽  
Chengsen Xue ◽  
Susan M. Kennelly ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Drug Development ◽  
Receptor Occupancy

Best practices for optimization and validation of flow cytometry‐based receptor occupancy assays

2020 ◽  
Author(s):  
Ed Hilt ◽  
Yongliang S. Sun ◽  
Thomas W. McCloskey ◽  
Steve Eck ◽  
Thomas McIntosh ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Best Practices ◽  
Receptor Occupancy

scholarly journals Role of receptor occupancy assays by flow cytometry in drug development

2016 ◽  
Vol 90 (2) ◽  
pp. 110-116 ◽  
Author(s):  
Jennifer J. Stewart ◽  
Cherie L. Green ◽  
Nicholas Jones ◽  
Meina Liang ◽  
Yuanxin Xu ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Drug Development ◽  
Receptor Occupancy
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