TABLE 4

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	LDBK^b	LDLBK^b	NPC18565	Compound 11
N	Cys²⁰
TM-I
TM-II		Trp⁸⁶
EL-II
TM-III	Ser¹¹¹	Ile¹¹⁰	Ser¹¹¹	Ile¹¹⁰	Ile¹¹⁰	Lys¹¹⁸	(Lys¹¹⁸)^c	Lys¹¹⁸	Asn¹¹⁴
TM-IV	Lys¹⁷²
EL-III	Yes^d			Yes^d
TM-V
TM-VI	Phe²⁵⁹,Thr²⁶³	Phe²⁵⁹		Trp²⁵⁶
EC-IV	Cys²⁷⁷,Asp²⁶⁶,Asp²⁸⁴						Yes^d
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