4.4 Determination of Pharmacokinetics of Drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18
4.5 Fluorescence Prodrug Conjugates . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19
5 Future Perspectives . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 24
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 25
Abstract The process of new drug discovery and development is a lengthy, highrisk, and costly task. Fluorescent molecular imaging (FMI) has tremendous potential
for improving the efficiency of drug screening, evaluating drug effects, accelerating
the process, and markedly reducing the cost of new drug development from initial
target validation and high-throughput screening identification campaigns to the final
human translation phases. FMI can help evaluate the role of new candidate drugs
under the influence of complex biological responses in living subjects and better
understand the mechanism between drug activity and disease, which can help select
candidates that seem most likely to succeed or prevent the development of drugs that
seem to fail in the end. Hence, in this chapter, FMI was described for its application
in drug discovery, including identification of tumor-specific markers, candidate drug
screening, determination of pharmacokinetics of drugs, and preparation of prodrugs.
Keywords Cancer, Drug discovery, Fluorescent molecular imaging, Medicinal
chemistry
Abbreviations
BBTD
Benzobisthiadiazole
BEM
Boundary element method
BLI
Bioluminescence imaging
BODIPY Boron dipyrromethene
Cy
Cyanine
D-A-D
Donor-acceptor-donor scaffold
DE
Diffusion equation
FDM
Finite difference method
FEM
Finite element method
FITC
Fluorescein isothiocyanate
FMI
Fluorescence molecular imaging
FMT
Fluorescence molecular tomography
GFP
Green fluorescent protein
HDACs
Histone deacetylases
ICG
Indocyanine green
MM
Meshless method
NIR
Near-infrared
ROS
Reactive oxygen species
SBR
Signal-to-background ratio
2
J. Tian et al.
4.5 Fluorescence Prodrug Conjugates . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19
5 Future Perspectives . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 24
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 25
Abstract The process of new drug discovery and development is a lengthy, highrisk, and costly task. Fluorescent molecular imaging (FMI) has tremendous potential
for improving the efficiency of drug screening, evaluating drug effects, accelerating
the process, and markedly reducing the cost of new drug development from initial
target validation and high-throughput screening identification campaigns to the final
human translation phases. FMI can help evaluate the role of new candidate drugs
under the influence of complex biological responses in living subjects and better
understand the mechanism between drug activity and disease, which can help select
candidates that seem most likely to succeed or prevent the development of drugs that
seem to fail in the end. Hence, in this chapter, FMI was described for its application
in drug discovery, including identification of tumor-specific markers, candidate drug
screening, determination of pharmacokinetics of drugs, and preparation of prodrugs.
Keywords Cancer, Drug discovery, Fluorescent molecular imaging, Medicinal
chemistry
Abbreviations
BBTD
Benzobisthiadiazole
BEM
Boundary element method
BLI
Bioluminescence imaging
BODIPY Boron dipyrromethene
Cy
Cyanine
D-A-D
Donor-acceptor-donor scaffold
DE
Diffusion equation
FDM
Finite difference method
FEM
Finite element method
FITC
Fluorescein isothiocyanate
FMI
Fluorescence molecular imaging
FMT
Fluorescence molecular tomography
GFP
Green fluorescent protein
HDACs
Histone deacetylases
ICG
Indocyanine green
MM
Meshless method
NIR
Near-infrared
ROS
Reactive oxygen species
SBR
Signal-to-background ratio
2
J. Tian et al.