Table 2D.

Peptides Influencing Aβ Aggregation and Toxicity. β-sheet Breaking Peptides Based on Methyl-Amino Acids

Name	Sequence	Description	D/L	Results	Reference
none	N-methylated GSNKGAIIGLM	First methylated β-sheet breakers	L	Prevent Aβ aggregation in vitro, inhibit cell toxicity	Hughes et al., 2000 [93, 94]
Aβ16-22m Aβ16-20m	KLVFF based e.g. KNmeLVNMEFFNMeAE	Methylated β-sheet breaker, N-methyl groups in alternating positions	L	Prevent Aβ fibril forming, disassemble fibrils in vitro	Gordon et al., 2001, 2002 [78, 95]
inL (all L) in D (all D) inrD (retro-inverso)	LKLVFF based, N-methyl-20F	Methylated β-sheet breaker, single N-methyl-amino acids	L/D	Reduces Aβ toxicity in cell culture	Cruz et al., 2004; Grillo-Bosch et al., 2009 [96, 97]
PPI-1019 “Apan”	Methyl-LVFFL	Methylated β-sheet breaker	D	Completed phase I and II human clinical trials	Jhee et al., 2003 [98, 99]
e.g. SEN304	e.g. D-chGly-D-Tyr-D-chGly-D-chGly-D-mLeu	“meptide”, methylated β-sheet breaker	D	Highly active inhibitors of Aβ aggregation and toxicity	Kokkoni et al., 2006 [100]

D/L: describes peptide conformation. chGly: cyclohexylglycine; mLeu: N-methylleucine; NMe: N-methylated amino acids. Aβ-derived peptide sequences are written in bold.