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tosedostat

Known as: 2-(2-(hydroxy(hydroxycarbamoyl)methyl)-4-methylpentanoylamino)-2-phenylethanoic acid cyclopentyl ester, Aminopeptidase inhibitor CHR-2797, Cyclopentyl (2S)-2-{(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4- methylpentanamido}-2-phenylacetate 
A proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Aminopeptidase inhibitor CHR… 
National Institutes of Health

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CHR-2797

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GlycineHydroxamic Acids
analogs & derivatives

Papers overview

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2017
2017
A phase I/II study combining tosedostat with capecitabine in patients with metastatic pancreatic ductal adenocarcinoma (PDAC).
410Background: Recent advances in front-line therapy have improved survival in patients with advanced PDAC. A fluorouracil-based… 
2016
2016
A Phase I Dose-Escalation Study of the Class 1 Selective Histone Deacetylase Inhibitor CHR-3996 in Combination with Tosedostat for Patients with Relapsed, Refractory Multiple Myeloma: Results of the…
Introduction: Histone deacetylase inhibitors (HDACis) have demonstrated clinical efficacy in multiple myeloma, particularly in… 
2015
2015
Tosedostat Plus Low Dose Cytarabine Induces a High Rate of Responses That Can be Predicted By Genetic Profiling in Elderly AML
Background: Older (age ≥60 years) patients with acute myeloid leukemia (AML) have poor outcomes and intensive induction… 
2015
2015
In Vitro Radiosensitization of Esophageal Cancer Cells with the Aminopeptidase Inhibitor CHR-2797
With the increased incidence of esophageal cancer, chemoradiotherapy continues to play an important role in the management of… 
2012
2012
Targeting Aminopeptidases by Tosedostat (TST) (CHR2797), Alone and with LBH589, Induces Significant Cytotoxicity Against Human Multiple Myeloma (MM) Cells
Abstract 1847 Aminopeptidases (AP) are necessary for the growth and development of malignant cells and have a selectively… 
2011
2011
Results of the OPAL Study: A Phase II Study to Evaluate the Efficacy, Safety and Tolerability of Tosedostat (CHR-2797) in Elderly Subjects with Treatment Refractory or Relapsed Acute Myeloid Leukemia
Abstract 767 Background: Tosedostat is a novel oral inhibitor of the M1/17 family of aminopeptidases which induces an amino acid… 
2011
2011
Interim results of OPAL, a study of tosedostat in elderly relapsed/refractory AML.
6517 Background: Tosedostat is a novel oral aminopeptidase inhibitor which has shown promising efficacy in elderly relapsed… 
2010
2010
The OPAL study: A phase II study to evaluate the efficacy, safety, and tolerability of tosedostat (CHR-2797) in elderly subjects with treatment refractory or relapsed acute myeloid leukemia.
TPS277 Background: Tosedostat (CHR-2797) is a novel oral aminopeptidase inhibitor. Aminopeptidases catalyze hydrolysis of… 
2009
2009
Inhibition of HDACs and Aminopeptidases Is Highly Synergistic in Myeloma Cells Resulting in Cell Death Via the Upregulation of BIRC3, a Key Mediator of NF-KappaB Signalling.
Abstract 607 Myeloma cells rely on a number of mechanisms to maintain their survival, including the silencing of genes that would… 
1992
1992
Structure-function relationships for analogues ofl-2-amino-4-phosphonobutanoic acid on the quisqualic acid-sensitive AP4 receptor of the rat hippocampus
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