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Thermal proteome profiling of IGUANA-1-interacting proteins

ABSTRACT: Thermal proteome profiling data for SW480 colon cancer cells treated with either the ALDH1B1 inhibitor IGUANA-1 or DMSO vehicle alone.

INSTRUMENT(S): Orbitrap Eclipse

ORGANISM(S): Homo Sapiens (ncbitaxon:9606)

SUBMITTER: James Chen

PROVIDER: MSV000088824 | MassIVE | Fri Feb 11 10:53:00 GMT 2022

SECONDARY ACCESSION(S): PXD031630

REPOSITORIES: MassIVE

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Publications

Targeting colorectal cancer with small-molecule inhibitors of ALDH1B1.

Feng Zhiping Z Hom Marisa E ME Bearrood Thomas E TE Rosenthal Zachary C ZC Fernández Daniel D Ondrus Alison E AE Gu Yuchao Y McCormick Aaron K AK Tomaske Madeline G MG Marshall Cody R CR Kline Toni T Chen Che-Hong CH Mochly-Rosen Daria D Kuo Calvin J CJ Chen James K JK

Nature chemical biology 20220704 10

Aldehyde dehydrogenases (ALDHs) are promising cancer drug targets, as certain isoforms are required for the survival of stem-like tumor cells. We have discovered selective inhibitors of ALDH1B1, a mitochondrial enzyme that promotes colorectal and pancreatic cancer. We describe bicyclic imidazoliums and guanidines that target the ALDH1B1 active site with comparable molecular interactions and potencies. Both pharmacophores abrogate ALDH1B1 function in cells; however, the guanidines circumvent an o ...[more]

PMID: 35788181

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