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

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

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

Application of Flow Cytometry in Drug Development

2008 ◽  
pp. 141-159 ◽  
Author(s):  
Padma Narayanan ◽  
Renold J. Capocasale ◽  
Nianyu Li ◽  
Peter J. Bugelski
Keyword(s):  
Flow Cytometry ◽  
Drug Development

Precision Medicine: The Function of Receptor Occupancy in Drug Development

2020 ◽  
pp. 167-197
Author(s):  
Leanne Flye-Blakemore ◽  
Christèle Gonneau ◽  
Nithianandan Selliah ◽  
Ajay Grover ◽  
Sriram Ramanan ◽  
...  
Keyword(s):  
Drug Development ◽  
Precision Medicine ◽  
Receptor Occupancy

Critical reagents in flow cytometry, instrumentation and application in drug discovery development

Bioanalysis ◽  
2021 ◽  
Author(s):  
Vellalore N Kakkanaiah ◽  
Katie Matys ◽  
Patrick Bennett
Keyword(s):  
Flow Cytometry ◽  
Drug Discovery ◽  
Drug Development ◽  
Ligand Binding ◽  
Specific Interaction ◽  
Flow Cytometer ◽  
Analysis Tool ◽  
Binding Assays ◽  
Cellular Analysis ◽  
Main Components

Flow cytometer is a powerful cellular analysis tool consists of three main components; fluidics, optics and electronics. Flow cytometry methods have been used in all stages of drug development as like ligand binding assays (LBA). Both LBA and flow cytometry methods require specific interaction between the critical reagents and the analytes. Antibodies and their conjugates, viable dyes and permeabilizing buffer are the main critical reagents in flow cytometry methods. Similarly, antibodies, engineered proteins and their conjugates are the main critical reagents in LBA. The main difference between the two methods is the lack of true reference standards for flow cytometry cellular analysis.

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

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
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