Ontology highlight
ABSTRACT:
SUBMITTER: Garces AE
PROVIDER: S-EPMC7073869 | biostudies-literature | 2020 Mar
REPOSITORIES: biostudies-literature
Garces Aimie E AE Al-Hayali Mohammed M Lee Jong Bong JB Li Jiaxin J Gershkovich Pavel P Bradshaw Tracey D TD Stocks Michael J MJ
ACS medicinal chemistry letters 20190927 3
We report on the synergistic effect of PI3K inhibition with ALK inhibition for the possible treatment of EML4-ALK positive lung cancer. We have brought together ceritinib (ALK inhibitor) and pictilisib (PI3K inhibitor) into a single bivalent molecule (a codrug) with the aim of designing a molecule for slow release drug delivery that targets EML4-ALK positive lung cancer. We have joined the two drugs through a new, pH-sensitive linker where the resulting codrugs are hydrolytically stable at lower ...[more]