Summary of potential residues facing the B2 and B1 agonist and antagonist binding pockets as determined by mutagenesis, cross-linking, and competition with domain-specific antibodies a

B2 B1
Domain Agonists Antagonists Agonist Antagonist
BK FR190997 NPC/Icatib.b LF16–0335 FR173657 LDBKb LDLBKb NPC18565 Compound 11
N Cys20
TM-II Trp86
TM-III Ser111 Ile110 Ser111 Ile110 Ile110 Lys118 (Lys118)c Lys118 Asn114
TM-IV Lys172
EL-III Yesd Yesd
TM-VI Phe259,Thr263 Phe259 Trp256
EC-IV Cys277,Asp266,Asp284 Yesd
TMVII Gln288 Gln288,Tyr295 Tyr295 Leu294,Phe302 Phe302 Gln295
  • a Discussion of individual residues and references are in the main text

  • b NPC, NPC17731; Icatib., Icatibant; LDBK, Lys-des-Arg9-BK; LDLBK, Lys-[Leu8]des-Arg9-BK

  • c Inferred as an important residue by extrapolating data for NPC18565

  • d Domain is important but no specific residues have been identified