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PET determination of specific uptake
of 11C-erlotinib by different tumor types
expressing EGFR, in vivo, through
kinetic modeling
J. Ryan Petrulli1,4, Jenna M. Sullivan1,4, Ming-Qiang Zheng2,4,
Yiyun Huang2,4, Joseph N. Contessa3, Evan D. Morris1,2,4
1. Biomedical Engineering
2. Diagnostic Radiology
3. Therapeutic Radiology
4. Yale PET Center
Yale University, New Haven, CT, USA
METHODS
• Subjects: nude mice implanted with 2-3 tumor xenografts
• Human cancer cell lines: SW620, U87, HCC827, PC9, and U87∆
• Scans: Siemens Focus 220; 11C-erlotinib injections with or without
excess erlotinib
• Analysis:
– Regions of interest (ROI) drawn on summed images; regional timeactivity curves
– Kinetic modeling with SRTM to produce BP
– Statistical comparison between BP in each xenograft and drug condition
Cell Line: SW620
Mutation: No EGFR
n/a
Status:
U87
WT EGFR
Inactive
HCC827, PC9
Kinase Domain
Active
U87∆
Extracellular Domain
Active
KINASE DOMAIN MUTANT TUMORS
Tracer Experiment
Excess Cold Drug
2
2
KD Mutant
1
KD Mutant
1.5
SUV
SUV
1.5
1
0.5
0.5
no EGFR
0
0
0
50
Time (min)
100
0
50
100
Time (min)
SW620 (▲)
Muscle (○)
PC9 (♦)
HCC827 (■)
HCC827, PC9
KD Mutant
Activated EGFR
SPECIFIC BINDING
9
**
8
tracer experiment
7
excess cold drug
Mean BP
6
5
*
4
NS
3
NS
2
NS
1
0
n= 3
3
3
3
1
1
3
2
3
2
-1
HCC827
Mutation: KD
Status: Active
** p<0.05
* p=0.06
PC9
SW620
U87
U87∆
KD
Active
No EGFR
n/a
WT EGFR
Inactive
ECD
Active
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