Skip to main content

View full-text article in PMC

. Author manuscript; available in PMC: 2018 Oct 11.

Published in final edited form as: Chem Rev. 2017 Sep 27;117(19):12415–12474. doi: 10.1021/acs.chemrev.7b00283

Table 8.

Inhibition Assay of AIP Analogs^a

			AgrC				Hemolysis Assay
		Sequence	I	II	III	IV	I	II	III	IV
329	AIP-I	YST(CDFIM)	ag	8.00	0.522	nd	nd	3.34	6.12	189
330	AIP-II	GVNA(CSSLF)	1.62	ag	0.532	0.396	0.89	nd	3.59	1.19
331	AIP-III	IN(CDFLL)	5.05	5.63	ag	8.53	8.07	0.456	nd	23.8
332	AIP-IV	YST(CYFIM)	ND	0.373	0.46	ag	nd	0.0897	1.49	nd
333	I1A	AN(CDFLL)	17.9	4.26	194	7.85	4.61	1.29	nd	12.5
334	N2A	IA(CDFLL)	3.6	0.732	nd	3.53	1.02	0.137	nd	2.64
335	D4A	IN(CAFLL)	0.485	0.429	0.0506	0.0349	0.082	0.0596	0.163	0.106
336	I1A/N2A	AA(CDFLL)	7.4	4.38	2.6	5.41	nd	nd	nd	nd
337	I1A/D4A	AN(CAFLL)	0.328	2.35	0.28	0.101	0.0103	0.793	0.551	0.284
338	N2A/D4A	IA(CAFLL)	0.331	0.204	0.0657	0.0221	0.0362	0.0661	0.216	0.122
339	I1A/N2A/D4A	AA(CAFLL)	0.304	0.604	0.0734	0.0161	0.0411	0.0606	0.243	0.14
340	tD2A	Ac(CAFLL)	0.257	0.9	0.329	0.0957	0.332	0.711	0.197	0.306
341	tD2A/F3Y	Ac(CAYLL)	0.279	1.15	0.387	0.0306	0.279	0.204	0.265	0.134

^a

IC₅₀ in nM. Parentheses indicate the cyclic portion within the sequence. ag = agonist; nd = not determined. x-fold change measured relative to APPEL.