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Figure 2 | BMC Biochemistry

Figure 2

From: Identification of critical residues in loop E in the 5-HT3ASR binding site

Figure 2

Changes in K i or K d (for binding of [3H]granisetron) as a result of alanine mutations. The values shown are the ratio of the Kd or Ki for wildtype and mutant receptors. The length of each bar illustrates the magnitude of change in either the Kd or Ki relative to wildtype while the direction indicates an increase (up) or decrease (down) in the Kd or Ki. A. Most alanine mutations produced little change in Kd. No binding was detected for the G147A and V149A receptors therefore no Kd could be determined. B. Changes in Ki were small for most receptors although large changes were observed for select ligands at Y140A, Y142A and Y152A receptors. The relative increases in Ki for these amino acids are as follows: 5-HT: Y140A 1.3 ± 0.30 fold, Y142A 110 ± 25 fold, Y152A 24 ± 5.6 fold m CPBG: Y140A 7.3 ± 1.7 fold, Y142A 160 ± 36 fold, Y152A 24 ± 5.6 fold d -tc: Y140A 50 ± 12 fold, Y142A 6.5 ± 1.5, Y152A 10.0 ± 2.3 fold lerisetron: Y140A 4.6 ± 1.1 fold, Y142A 160 ± 37 fold, Y152A 190 ± 43 fold

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