TABLE 4.
Conservation of residues involved in the FK506-binding pocket of human FKBP12
| FKBP | Residuea at:
|
||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| β4 (Y26) | β4 (G28) | β5 (F36) | β5 (D37) | Bulge (R42) | β5 (F46) | Q53 | E54 | V55 | α (I56) | α (W59) | Flap (Y82) | Flap (H87) | β3 (I91) | β3 (F99) | |
| ecSlyDb (—)c | Y | V | V | D | S | L | G | S | L | I | L | Y | E | Q | F |
| ecTIGd (—) | F | G | F | E | F | G | R | M | I | F | Y | E | F | ||
| MTFK (250) | Y | G | F | D | E | L | G | Q | L | I | F | Y | E | Q | F |
| ecFKBYe (Ki = 25) | Y | G | F | D | R | A | G | V | I | W | Y | A | I | F | |
| lpMIPf (45) | Y | G | F | D | T | A | V | I | W | Y | V | I | F | ||
| ncFKBPg (20) | Y | G | F | D | R | L | G | R | V | I | W | Y | V | I | F |
| stcFKBPh (30–60) | Y | G | F | D | R | L | G | Q | V | I | W | Y | A | I | F |
a
The structure position (β, bulge, flap, α) indicates the positions in human FKBP12. The conserved amino acid residues compared to the residues of the human FKBP12-binding pocket are shown in boldface type.
b
E. coli FKBP homolog (15).
c
Values in parentheses show the IC50 for FK506 in nanomolar; — means that it is insensitive to FK506. In the case of ecFKBY, sensitivity to FK506 is expressed by a Ki value.
d
E. coli trigger factor (34).
e
E. coli 22-kDa FKBP (28).
f
L. pneumophila FKBP (9).
g
N. crassa FKBP (38).
h
Streptomyces chrysomallus FKBP (26).