RRC ID 48850
Author Kurdi A, Cleenewerck M, Vangestel C, Lyssens S, Declercq W, Timmermans JP, Stroobants S, Augustyns K, De Meyer GRY, Van Der Veken P, Martinet W.
Title ATG4B inhibitors with a benzotropolone core structure block autophagy and augment efficiency of chemotherapy in mice.
Journal Biochem. Pharmacol.
Abstract Foxn1nu mice bearing HT29 colorectal tumor xenografts. Moreover, addition of UAMC-2526 to the chemotherapy drug oxaliplatin significantly improved inhibition of tumor growth. Our data indicate that suppression of autophagy via ATG4B inhibition is a feasible strategy to augment existing chemotherapy efficacy and to halt tumor progression.
Volume 138
Pages 150-162
Published 2017-8-15
DOI 10.1016/j.bcp.2017.06.119
PII S0006-2952(17)30442-2
PMID 28642033
MeSH Adenocarcinoma / drug therapy* Adenocarcinoma / pathology Animals Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology Antineoplastic Agents / therapeutic use* Antineoplastic Combined Chemotherapy Protocols / therapeutic use Autophagy / drug effects* Autophagy-Related Proteins / antagonists & inhibitors* Autophagy-Related Proteins / genetics Autophagy-Related Proteins / metabolism Cell Proliferation / drug effects Colonic Neoplasms / drug therapy* Colonic Neoplasms / pathology Cysteine Endopeptidases / genetics Cysteine Endopeptidases / metabolism Cysteine Proteinase Inhibitors / chemistry Cysteine Proteinase Inhibitors / pharmacology Cysteine Proteinase Inhibitors / therapeutic use* Drug Design* Drug Stability Forkhead Transcription Factors / genetics Forkhead Transcription Factors / metabolism HEK293 Cells HT29 Cells Humans Jurkat Cells Mice, Knockout Mice, Transgenic Microtubule-Associated Proteins / antagonists & inhibitors Microtubule-Associated Proteins / genetics Microtubule-Associated Proteins / metabolism Organoplatinum Compounds / therapeutic use Recombinant Proteins / chemistry Recombinant Proteins / metabolism Tropolone / analogs & derivatives* Tropolone / chemistry Tropolone / pharmacology Tropolone / therapeutic use Xenograft Model Antitumor Assays
IF 4.235
Mice GFP-LC3#53(RBRC00806)