RP101 Inhibition of Chemoresistance and Metastasis PDF Print E-mail
RP101 is the first small molecule known to bind to the heat shock protein Hsp27 and to modulate its effect.
 Hsp27 is known to control the following cellular key functions:
  • Resistance against treatment with cytotoxic drugs
  • Development of metastases
  • Prevention of apoptosis

  hsp27_binding_schema_small.png

Figure: Modulation of apoptotic pathways by Hsp27. At the mitochondrial level, Hsp27, through Bid inhibits the mitochondrial release of pro-apoptotic proteins. At the postmitochondrial level, Hsp27 binds to cytochrome c resulting in the inhibition of apoptosome formation and thereby prevention of caspase activation and apoptosis. Hsp27 can also interact with and inhibit Daxx apoptotic pathway.  Interaction of Hsp27 and Pro-caspase-3 has been described as well .

 

Item description

TNF

TUMOR NECROSIS FACTOR

TNFR

TUMOR NECROSIS FACTOR RECEPTOR SUPERFAMILY

FADD

FAS-ASSOCIATED VIA DEATH DOMAIN

RIP

REV-INTERACTING PROTEIN

Smac

SECOND MITOCHONDRIA-DERIVED ACTIVATOR OF CASPASE

Cyt c

CYTOCHROME C, SOMATIC

Apaf 1

APOPTOTIC PROTEASE ACTIVATING FACTOR 1

Casp 3

CASPASE 3, APOPTOSIS-RELATED CYSTEINE PROTEASE

Casp 8

CASPASE 8, APOPTOSIS-RELATED CYSTEINE PROTEASE

Casp 9

CASPASE 9, APOPTOSIS-RELATED CYSTEINE PROTEASE

Bax

BCL2-ASSOCIATED X PROTEIN

Bad

BCL2 ANTAGONIST OF CELL DEATH

Bid

BH3-INTERACTING DOMAIN DEATH AGONIST