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Table 1 Estimated Inhibition Constant, Ki (nmol), for ARBs docking into several immune system receptors.

From: Common angiotensin receptor blockers may directly modulate the immune system via VDR, PPAR and CCR2b

 

Olmesartan

Telmisartan

Valsartan

Irbesartan

Candesartan

Losartan

VDR,1DB1

12, 27

0.038

14

10

35

77

VDR,1TXI

10,34

0.039

14

12

30

74

PPAR

12

0.29

12

6

61

3

CCR2b *

9*

25*

22*

9*

39*

25*

AT2R1 *

0.10*

0.10*

0.3*

0.17*

1.5*

0.50*

  1. *Note 1: CCR2b and AT2R1 are theoretical models, and may not be reliable (see text)
  2. Note 2: (conventional ligand binding data): 1,25-dihydroxyvitamin-D docks into VDR (PDB:1DB1) with Ki = 0.029 nmol and into VDR (PDB:1TXI) with Ki= 0.059 nmol
  3. TX522 docks into VDR (PDB:1DB1) with Ki = 0.071 nmol and VDR (PDB:1TXI) with Ki = 0.12 nmol
  4. TAK779 docks into putative CCR2b with Ki = 10 nmol
  5. GI262570 docks into PPAR (PDB:1FM9) with Ki = 0.040 nmol.
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Theoretical Biology and Medical Modelling

ISSN: 1742-4682