WK6 - Anticancer 2

Question 1

Pgp Inhibitors

Answer 1

over expression of Pgp drug efflux pump in tumor cells -> increase drug efflux -> decrease intra-tumor [drug] -> decrease therapeutic effect; Potential solution to this is combining Pgp inhibitors + cytotoxic drug

Question 2

Bcl-2 Antisense

Answer 2

marks mRNA (Bcl-2) for destruction -> down regulate Bcl-2 protein expression via Bcl-2 antisense therapy -> decrease block of cyt-c release -> increase apoptosis -> decrease resistance.

Question 3

TK Inhibitors

Answer 3

small molecules compete with ATP binding at TK domain -> no ATP binding at TK domain ->no phosphorylation -> no signalling -> no response

Question 4

Antibodies vs TK receptor (extracellular portion of receptor)

Answer 4

Competitive inhibition of ligand binding -> no ligand binding -> no receptor dimerization or cross phosphorylation -> no signalling -> no response

Question 5

Antibodies vs TK ligand

Answer 5

neutralizes the ligand -> no ligand binding -> no receptor dimerization or cross phosphorylation -> no signalling -> no response

Question 6

Antiangiogenic blockade of EC activation

Answer 6

Blocks endothelial cell activation (ex block VGEF, key ‘activator’ molecule produced in abundance by many cancer cells that activate endothelial cells to create MMF to degrade ECM & migrate)

Question 7

MMP Inhibitors

Answer 7

Blocks endothelial cell migration by inhibiting MMPs -> prevents breakdown of the extracellular matrix