Table 1. Interactions of GPCR peptides with the core BBSome.
| GPCR | Uniprot accession number |
Tested residues |
BBSome binding: trend from microarray |
Validated peptides |
Peptide sequences | KD [µM] |
|---|---|---|---|---|---|---|
| 5-HT-6 | P50406 | 195–440 | 3ICL: weak | not tested | ||
| CT: strong | 5HT6 CT | RDFKRALGRFLPCPRCPRER | 44.2 ± 10.9 | |||
| MCH-R1 | Q99705 | 288–422 | 3ICL: strong | MCH 3ICL | RILQRMTSSVAPASQRSIRLRTKRVTRT | 68.8 ± 11.3 |
| CT: weak | not tested | |||||
| NMU-R1 | Q9HB89 | 243–426 | 3ICL: strong | NMU 3ICL1 NMU 3ICL2 |
LLIGLRLRRERLLLMQEAKGRG GRGSAAARSRYTCRLQQHDRGRRQ |
18.1 ± 1.6 >100 |
| CT: weak | not tested | |||||
| SSTR3 | P32745 | 44–418 | 3ICL: strong | SSTR3 3ICL | VKVRSAGRRVWAPSCQRRRRSERRVTRM | 12.8 ± 1.07 |
| CT: medium | SSTR3 CT1 SSTR3 CT2 SSTR3 CT3 SSTR3 CT4 SSTR3 CT5 SSTR3 CT6 SSTR3 CT7 SSTR3 CT8 SSTR3 CT9 |
RFKQGFRRVLLRPSR
GFLSYRFKQGFRRVLLRPSRRVRS GFLSAAFKQGFRRVLLRPSRRVRS GFLSYRAAQGFRRVLLRPSRRVRS GFLSYRFKQGAARVLLRPSRRVRS GFLSAAFKQGAARVLLRPSRRVRS GFLSAAAAQGFRRVLLRPSRRVRS GFLSAAAAQGAARVLLRPSRRVRS GFLSYRFKQGFRRVLLRPSEEVES |
22.1 ± 1.4 0.11 ± 0.02 1.1 ± 0.2 0.40 ± 0.08 1.5 ± 0.3 4.5 ± 1.1 1.0 ± 0.2 11.0 ± 3.3 4.7 ± 1.4 |
|||
| Smo | Q99835 | 234–787 | 3ICL: weak | not tested | ||
| CT: strong | Smo CT1 Smo CT2 Smo CT3 Smo CT4 Smo CT5 Smo CT6 Smo CT7 Smo CT8 Smo (R546-L665) |
TLLIWRRTWCRLTGQ KRIKKSKMIAKAFSK TLLIWRRTWCRLTGQSDDEPKRIKKSKMIAKAFSKRH TLLIWRRTWCRLTGQSDDE TLLIAARTWCRLTGQSDDE TLLIWRRTAARLTGQSDDE TLLIAARTAARLTGQSDDE KRLGRKKKRRKRKKE R546-L665 |
1.8 ± 0.5 >100 1.4 ± 0.5 1.1 ± 0.5 9.7 ± 3.3 12.5 ± 3.0 14.3 ± 4.7 6.8 ± 2.5 36.1 ± 3.9 |
|||
| GPR161 | Q8N6U8 | 31–529 | 3ICL: strong | GPR161 3ICL | FIFRVARVKARKVHCG | 6.3 ± 1.5 |
| CT: strong | GPR161 CT1 GPR161 CT2 |
NKTVRKELLGMCFGDRYYREPFVQRQR VTARTVPGGGFGGRRGSRTLVS |
67.4 ± 7.3 >100 |
Summary of qualitative and quantitative analysis of binding data for peptides, indicated by their sequence, from those GPCRs for which significant BBSome interactions were found in the peptide microarrays and analyzed for affinity by fluorescence polarization. Basic/aromatic residues in SSTR3 and Smo were mutated to alanine are shown in red, and the corresponding wild type sequences in purple. Previously described CTS sequences are marked in blue (; Mukhopadhyay et al., 2013; Zhang et al., 2012a).