Lee M. Greenberger

TL;DR: It is reported that FTC almost completely reverses resistance mediated by BCRP in vitro and is a pharmacological probe for the expression and molecular action of this transporter.

TL;DR: It is suggested that fumitremorgin C is a highly selective chemosensitizing agent for the resistance pathway the authors have identified and can be used as a specific pharmacological probe to distinguish between the diverse resistance mechanisms that occur in the MDR cell.

TL;DR: A series of of 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile derivatives that function as irreversible inhibitors of EGFR and HER-2 kinases have been prepared and one compound, 5, which shows excellent oral in vivo activity, was selected for further studies and is currently in phase I clinical trials for the treatment of cancer.

TL;DR: EZN-2968 is a RNA antagonist composed of third-generation oligonucleotide, locked nucleic acid, technology that specifically binds and inhibits the expression of HIF-1α mRNA and led to reduction of its transcriptional targets and of human umbilical vein endothelial cell tube formation.

TL;DR: It is reported here that a multiarm poly(ethylene glycol) backbone linked to four SN38 molecules (PEG-SN38) has been successfully prepared with high drug loading and significantly improved water solubility, and PEG-Gly-(20)-SN38 has been selected as the lead candidate for further preclinical development.