Target Validation Information
TTD ID	T11253
Target Name	HSPB1 messenger RNA (HSPB1 mRNA)
Type of Target	Discontinued
Drug Potency against Target	SB-242235	Drug Info	IC50 = 160 nM	[1]
Action against Disease Model	OGX-427	Drug Info	H uMan KU-7 bladder t uMour cells were treated with OGX-427 or a mismatch (MM) control oligodeoxynucleotide (ODN) in vitro and were assessed for HSP27 expression, proliferation and apoptosis. In vitro, OGX-427 significantly decreased HSP27 protein levels and cellular viability. While naked OGX-427 showed only a trend in t uMour suppression compared with MM ODN, OGX-427 complexed with chitosan significantly inhibited orthotopic t uMour growth. The chitosan preparation induced some haematuria compared to naked ASO, but this formulation had superior tissue uptake of oligonucleotides and suppressed HSP27 tissue levels by 75%.	[2]
References
REF 1	Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4433-7.
REF 2	Origin, structure, and activity in vitro and in vivo of dalbavancin. J Antimicrob Chemother. 2005 Mar;55 Suppl 2:ii15-20.

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