Table 2.
Mutation of residues 8–18
| Residue | Mutation | Effect | Comment | Reference |
|---|---|---|---|---|
| Val8 | Deletion (CGRP9–37) | No change in affinity | Guinea pig atria | (Mimeault et al., 1991) |
| Val8 | [Pro8]-CGRP8–37 | No change in affinity | Rat pulmonary artery | (Wisskirchen et al., 2000) |
| Val8 | [Gly8]-CGRP8–37 | No change in affinity | Rat pulmonary artery | (Wisskirchen et al., 2000) |
| Thr9 | Deletion (CGRP10–37) | Fivefold decrease in affinity | Guinea pig atria | (Mimeault et al., 1991) |
| Thr9 | [Ala8]-CGRP8–37 | Threefold decrease in affinity | Guinea pig atria | (Mimeault et al., 1992) |
| Thr9His10 | Deletion (CGRP11–37) | Further twofold decrease in affinity compared with CGRP9–37 | Guinea pig atria | (Mimeault et al., 1991) |
| His10 | [Ala10]-CGRP8–37 | Threefold decrease in affinity | Guinea pig atria | (Mimeault et al., 1992) |
| His10 | Benzoylation of His | 50-fold increase in affinity of CGRP8–37 | Porcine coronary artery | (Smith et al., 2003) |
| Val8His10Gly14 | [Pro8Glu10Glu14]-CGRP8–37 | >100-fold decrease in affinity | Rat pulmonary artery | (Wisskirchen et al., 2000) |
| Thr9His10Arg11 | Deletion (CGRP12–37) | Further twofold decrease in affinity compared with CGRP11–37 | Guinea pig atria | (Mimeault et al., 1991) |
| Arg11 | [Ala11]-CGRP8–37 | Fivefold decrease in affinity | Guinea pig atria | (Mimeault et al., 1992) |
| Arg11 | [Ala11]-CGRP8–37 | Sixfold decrease in affinity | L6 myocytes | (Howitt and Poyner, 1997) |
| Arg11 | [Glu11]-CGRP8–37 | 60-fold decrease in affinity | SK-N-MC cells | (Howitt et al., 2003) |
| Arg11 | Long-chain acylation | Threefold decrease in affinity | CGRP receptor-expressing cell line | Patent WO/2011/051312 |
| Leu12 | Replacement by Bpa [Bpa12]-CGRP8–37 | 30-fold decrease in affinity | SK-N-MC cells | (Howitt et al., 2003) |
| Gly14 | [Ala14]-CGRP8–37 | No decrease in affinity | Porcine coronary artery | (Li et al., 1997) |
| Gly14 | Replacement by Aib [Aib14]-CGRP8–37 | Twofold decrease in affinity | Porcine coronary artery | (Li et al., 1997) |
| Gly14 | [Asp14]-CGRP8–37 | Twofold decrease in affinity | Porcine coronary artery | (Li et al., 1997) |
| Gly14 | [Asn14]-CGRP8–37 | Threefold decrease in affinity | Porcine coronary artery | (Li et al., 1997) |
| Gly14 | [Pro14]-CGRP8–37 | 100-fold decrease in affinity | Porcine coronary artery | (Li et al., 1997) |
| Leu15 | Replacement by Bpa [Bpa15]-CGRP8–37 | Fivefold decrease in affinity | SK-N-MC cells | (Howitt et al., 2003) |
| Leu16 | Replacement by Bpa [Bpa16]-CGRP8–37 | 700-fold decrease in affinity | SK-N-MC cells | (Howitt et al., 2003) |
| Leu16 | [Pro16]-CGRP8–37 | >1000-fold decrease in affinity | Rat pulmonary artery | (Wisskirchen et al., 2000) |
| Leu16 | [Ala16]-CGRP8–37 | Fivefold decrease in affinity | Rat pulmonary artery | (Wisskirchen et al., 2000) |
| Ser17 | [Ala17]-CGRP8–37 | Twofold increase in affinity | Guinea pig atrium | (Boulanger et al., 1996) |
| Arg18 | [Ala18]-CGRP8–37 | No decrease in affinity | L6 myocytes | (Howitt and Poyner, 1997) |
| Arg18 | [Glu18]-CGRP8–37 | 60-fold decrease in affinity | SK-N-MC cells | (Howitt et al., 2003) |
| Arg11,18 | [Ala11,18]-CGRP8–37 | 300-fold decrease in affinity | L6 myocytes | (Howitt and Poyner, 1997) |
| Arg11,18 | [Ser11,18]-CGRP8–37 | 1000-fold decrease in affinity | SK-N-MC cells | (Howitt et al., 2003) |
All differences are with respect to human α-CGRP8–37.
Bpa, 3-(4-benzoylphenyl)alanine.