Comparison of human B cell activation by TLR7 and TLR9 agonists

BMC Immunology

Table 1 Potency of small molecule TLR agonists in activating TLR7- and TLR8-mediated NF-κB activity in transfected human HEK293 cells.

Compound	Minimum effective concentration (MEC, μM) for NFκB activation (a)		TLR selectivity (b)
	TLR7	TLR8
3M-006	Inactive (100)	Inactive (100)	None
3M-003	0.1	1	TLR7/8 @ 1 μM
852A	3	100	TLR7 @ 3 μM
3M-002	10	1	TLR8 @ 5 μM

(a) Transfection of HEK293 cells with TLR7 or TLR8, and assessment of IRM-induced NFκB activation was performed as previously described [6]. Potency is defined as the concentration required to induce an increase in NFκB activation. MEC, minimal effective concentration, is the lowest concentration required to observe a 2-fold increase above the vehicle control.
(b) Selectivity is defined as preferential signaling through TLR7 or TLR8 at a specified concentration of the TLR agonists.

ISSN: 1471-2172