eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 26

Quantitative Assays to Measure
Therapeutic Antibody Binding
to Fc Receptors
Interactions of antibody drugs with Fc receptors are important
factors in therapeutics
Fc Receptors, expressed on the surface of immune
cells, bind the Fc (fragment crystallizable)
portion of antibodies, and play an essential role
in modulating our immune defense system.
They also impact the efficacy of therapeutic
antibodies and therefore are of great interest in
drug development.1
a therapeutic antibody depends not only on how
tightly it binds to the intended target, but also
on how long it is present in the patient's blood
and how well it engages an appropriate immune
response through its interaction with Fc receptors.
Therapeutic antibodies represent a powerful
class of drugs used for the treatment of cancer,
immune disease, or viral infection. They include
neutralizing antibodies targeting cytokines or
cytokine receptors, as well as cytotoxic antibodies
and antibody-drug conjugates that bind to
cancer-specific targets and directly kill the tumor
cells. Antibodies against immune targets such
as anti-PD-1/PD-L1 or anti-CTLA4 antibodies are
designed to enhance immune responses within
the tumor microenvironment.
Indeed, the effectiveness of
The half-life of an antibody is controlled by binding
to the neonatal Fc receptor for IgG (FcRn), which
regulates distinct functions in IgG transport and
homeostasis. Other Fc receptors trigger immune
responses through antibody-dependent cell
mediated cytotoxicity (ADCC), a mechanism in
which a natural killer (NK) cell is activated by
antibodies bound to tumor cells, followed by the
lysis of the tumor cell.
These Fc receptors are classified based on the type
of immunoglobulin (Ig) that they recognize: Fcγ
receptors bind to IgG, Fcα receptors bind to IgA,
and Fcε receptors bind to IgE.
The development of new therapeutic antibodies
(which are mostly IgGs) may require optimization of
their interaction with FcRn or with the appropriate
FcγR. Scientists must choose cell models and assays
carefully depending on their intended goal.
Antibody Checkpoints
The
Fcγ
receptors
function
as
antibody
checkpoints. They contain multiple extracellular
26

eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development

Table of Contents for the Digital Edition of eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development

eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 1
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 2
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 3
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 4
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 5
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 6
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 7
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 8
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 9
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 10
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 11
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 12
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 13
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 14
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 15
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 16
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 17
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 18
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 19
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 20
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 21
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 22
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 23
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 24
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 25
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 26
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 27
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 28
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 29
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 30
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 31
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 32
eBook: Biochemical and Cell-Based Assays for Targeted Cancer Drug Discovery and Development - 33
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