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Table 1 Receptor densities

From: Pharmacokinetics and pharmacodynamics of VEGF-neutralizing antibodies

 

Measured parameters

Model parameters

 

Value

Unit

Value

Unit

VEGFR1

    

   Luminal EC (normal)

550

rec/EC

1.21 × 10-1

pmol/cm3 tissue

   Abluminal EC (normal)

550

rec/EC

9.86 × 10-3

pmol/cm3 tissue

   Luminal EC (diseased)

3,750

rec/EC

4.38 × 10-4

pmol/cm3 tissue

   Abluminal EC (diseased)

3,750

rec/EC

6.54 × 10-2

pmol/cm3 tissue

   Myocytes

0

rec/myocyte

0

pmol/cm3 tissue

   Tumor cells

1,100

rec/tumor cell

2.81 × 10-1

pmol/cm3 tissue

VEGFR2

    

   Luminal EC (normal)

350

rec/EC

7.70 × 10-2

pmol/cm3 tissue

   Abluminal EC (normal)

350

rec/EC

6.28 × 10-3

pmol/cm3 tissue

   Luminal EC (diseased)

300

rec/EC

3.51 × 10-5

pmol/cm3 tissue

   Abluminal EC (diseased)

300

rec/EC

5.23 × 10-3

pmol/cm3 tissue

   Myocytes

0

rec/myocyte

0

pmol/cm3 tissue

   Tumor cells

550

rec/tumor cell

1.41 × 10-1

pmol/cm3 tissue

NRP1

    

   Luminal EC (normal)

17,500

rec/EC

3.74

pmol/cm3 tissue

   Abluminal EC (normal)

17,500

rec/EC

3.05 × 10-1

pmol/cm3 tissue

   Luminal EC (diseased)

20,000†

rec/EC

2.34 × 10-3

pmol/cm3 tissue

   Abluminal EC (diseased)

20,000†

rec/EC

3.49 × 10-1

pmol/cm3 tissue

   Myocytes

34,500

rec/myocyte

2.06

pmol/cm3 tissue

   Tumor cells

39,500

rec/tumor cell

1.01 × 101

pmol/cm3 tissue

NRP2

    

   Luminal EC (normal)

0

rec/EC

0

pmol/cm3 tissue

   Abluminal EC (normal)

0

rec/EC

0

pmol/cm3 tissue

   Luminal EC (diseased)

0

rec/EC

0

pmol/cm3 tissue

   Abluminal EC (diseased)

0

rec/EC

0

pmol/cm3 tissue

   Myocytes

0

rec/myocyte

0

pmol/cm3 tissue

   Tumor cells

39,500‡

rec/tumor cell

1.02 × 101

pmol/cm3 tissue

  1. EC = endothelial cell; rec = receptors
  2. † Extrapolated from receptor density on normal ECs, accounting for different cell surface areas
  3. ‡No NRP2 quantification available; assumed to be the same as NRP1 on tumor cells
  4. Conversions of receptor densities to tissue concentrations:
  5. Abluminal EC receptors (normal): 1.79 × 10-5 (pmol/cm3 tissue)/(rec/EC);
  6. Luminal EC receptors (normal): 2.20 × 10-4 (pmol/cm3 tissue)/(rec/EC);
  7. Abluminal EC receptors (diseased): 1.74 × 10-5 (pmol/cm3 tissue)/(rec/EC);
  8. Luminal EC receptors (diseased): 1.17 × 10-7 (pmol/cm3 tissue)/(rec/EC);
  9. Myocyte receptors: 5.96 × 10-5 (pmol/cm3 tissue)/(rec/myocyte);
  10. Tumor receptors: 2.55 × 10-4 (pmol/cm3 tissue)/(rec/tumor cell);
  11. Myocyte receptor densities are expressed per myonuclear domain