2-ANPC is a 2-aminopyrrole derivative reported to downregulate HIF-1α expression in multiple cancer cell lines and in a 4T1 mouse tumor model. The abstract also describes it as a previously shown microtubule-targeting agent.
First-pass extracted concept
2-ANPC
Aliases
2-amino-1-benzamido-5-(2-(naphthalene-2-yl)-2-oxoethylidene)-4-oxo-4,5-dihydro-1-H-pyrrole-3-carboxamide, 2-aminopyrrole derivative
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2-ANPC treatment increases cleaved caspase-3-positive apoptotic cells in 4T1 tumors.
an increase in apoptotic (i.e., cleaved caspase-3-positive) cells was detected in 4T1 tumors treated with 2-aminopyrrole derivative.
Computational analysis identified four potential binding sites for 2-ANPC to interact with HIF-1α, HIF-1β, and the p300 complex.
using various computational tools, we identified four potential binding sites for 2-ANPC to interact with HIF-1α, HIF-1β, and the p300 complex.
2-ANPC downregulates HIF-1α in vivo in the 4T1 breast cancer syngeneic model.
2-ANPC's potency in downregulating HIF-1α was also shown in vivo by using the 4T1 breast cancer syngraft model.
2-ANPC-mediated HIF-1α downregulation is due to enhanced proteasome-mediated degradation and is reversed by MG-132.
The downregulation of HIF-1α expression in 2-ANPC-treated cancer cells was due to enhanced proteasome-mediated degradation, whereas the proteasome inhibitor MG-132 effectively reversed this downregulation.
HIF-1α is presented as a novel molecular target for 2-ANPC.
we show here, for the first time, that HIF-1α is a novel molecular target for the 2-aminopyrrole derivative (2-ANPC)
2-ANPC downregulates HIF-1α expression in breast, lung, and prostate cancer cell lines.
2-ANPC ... effectively downregulates HIF-1α expression in a broad spectrum of cancer cell lines, including breast, lung, and prostate cancer.
In 4T1 tumors, 2-ANPC downregulates VEGFR1 and VEGFR3 expression and this correlates with decreased tumor weight and size.
this 2-aminopyrrole derivative also downregulated the expression of vascular endothelial growth factor receptors 1 and 3 (VEGFR1 and 3) in 4T1 tumors, which correlated with decreased tumor weight and size.