ArticlePigment cell & melanoma research2009
BI-69A11-mediated inhibition of AKT leads to effective regression of xenograft melanoma.
Article in Pigment cell & melanoma research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 21 citations in OpenAlex.
- Therapeutic Opportunities in Eukaryotic Translation.Cold Spring Harbor perspectives in biology · 2018Review
- Cooperative effect of BI-69A11 and celecoxib enhances radiosensitization by modulating DNA damage repair in colon carcinoma.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2016Article
- SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex.Cancer research · 2015Article
- BI-69A11 enhances susceptibility of colon cancer cells to mda-7/IL-24-induced growth inhibition by targeting Akt.British journal of cancer · 2014Article
- Synthesis and SAR studies of dual AKT/NF-κB inhibitors against melanoma.Chemical biology & drug design · 2013Article
- Modulation of the Akt pathway reveals a novel link with PERK/eIF2α, which is relevant during hypoxia.PloS one · 2013Article
- Inhibition of melanoma development in the Nras((Q61K)) ::Ink4a(-/-) mouse model by the small molecule BI-69A11.Pigment cell & melanoma research · 2013Article
- Identification of small molecules that interfere with H1N1 influenza A viral replication.ChemMedChem · 2012Article
- Activation of the PI3K/AKT pathway in Merkel cell carcinoma.PloS one · 2012Article
- The Akt signaling pathway: an emerging therapeutic target in malignant melanoma.Cancer biology & therapy · 2011Review
- Effective inhibition of melanoma by BI-69A11 is mediated by dual targeting of the AKT and NF-κB pathways.Pigment cell & melanoma research · 2011Article
- Therapeutic Implications of Targeting AKT Signaling in Melanoma.Enzyme research · 2011Article
- Design, synthesis, and structure-activity relationships of 3-ethynyl-1H-indazoles as inhibitors of the phosphatidylinositol 3-kinase signaling pathway.Journal of medicinal chemistry · 2010Article
- The PTEN-AKT3 signaling cascade as a therapeutic target in melanoma.Pigment cell & melanoma research · 2009Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
The AKT/PKB pathway plays a central role in tumor development and progression and is often up-regulated in different tumor types, including melanomas. We have recently reported on the in silico approach to identify putative inhibitors for AKT/PKB. Of the reported hits, we selected BI-69A11, a compound which was shown to inhibit AKT activity in in vitro kinase assays. Analysis of BI-69A11 was performed in melanoma cells, a tumor type that commonly exhibits up-regulation of AKT. Treatment of the UACC903 human melanoma cells, harboring the PTEN mutation, with BI-69A11 caused efficient inhibition of AKT S473 phosphorylation with concomitant inhibition of AKT phosphorylation of PRAS40. Treatment of melanoma cells with BI-69A11 also reduced AKT protein expression, which coincided with inhibition of AKT association with HSP-90. BI-69A11 treatment not only caused cell death of melanoma, but also prostate tumor cell lines. Notably, the effect of BI-69A11 on cell death was more pronounced in cells that express an active form of AKT. Significantly, intra-peritoneal injection of BI-69A11 caused effective regression of melanoma tumor xenografts, which coincided with elevated levels of cell death. These findings identify BI-69A11 as a potent inhibitor of AKT that is capable of eliciting effective regression of xenograft melanoma tumors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.