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PR-171

An epoxomicin derivate with potential antineoplastic activity. PR-171 irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S… 
National Institutes of Health

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Broader (1)

Oligopeptides
carfilzomib

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
2016
2016
Phase 1 trial of carfilzomib (PR-171) in combination with vorinostat (SAHA) in patients with relapsed or refractory B-cell lymphomas
Abstract A phase 1 study with carfilzomib and vorinostat was conducted in 20 B-cell lymphoma patients. Vorinostat was given… 
2010
2010
Inhibitors Active Site Specificity of Proteasome Nature of Pharmacophore Influences Protein Synthesis and Degradation :
2009
2009
High coagulant factors & venous thrombosis.
In this issue of Blood, results from the Longitudinal Investigation of Thromboembolism (LITE) 1 show that, of the coagulant… 
2009
2009
Induction of sequential G1 arrest and synchronous S phase entry by reversible CDK4/CDK6 inhibition sensitizes myeloma cells for cytotoxic killing through loss of IRF-4.
Abstract 299 Dysregulation of the cell cycle is a hallmark of cancer. However, targeting the cell cycle in cancer therapy has… 
2009
2009
Selective inhibition of CDK4/CDK6 sensitizes bone marrow myeloma cells for killing by proteasome inhibitors carfilzomib and PR-047 through cell cycle-dependent expression of pro-apoptotic Noxa and…
Abstract 2854 Poster Board II-830 Targeting the cell cycle in combination with cytotoxic killing is a rational approach to cancer… 
2009
2009
Cancer Therapy : Clinical A Phase 1 Dose Escalation Study of the Safety and Pharmacokinetics of the Novel Proteasome Inhibitor Carfilzomib ( PR-171 ) in Patients with Hematologic Malignancies
Purpose: Carfilzomib (formerly PR-171) is a novel proteasome inhibitor of the epoxyketone class that is selective and… 
2007
2007
Phase I evaluation of carfilzomib (PR-171) in hematological malignancies: Responses in multiple myeloma and Waldenstrom’s macroglobulinemia at well-tolerated doses
8003 Background: Carfilzomib is a novel, irreversible tetrapeptide proteasome inhibitor derived from the natural product… 
2006
2006
Multicenter Phase I Studies To Evaluate the Safety, Tolerability, and Clinical Response to Intensive Dosing with the Proteasome Inhibitor PR-171 in Patients with Relapsed or Refractory Hematological…
INTRODUCTION: PR-171 is a novel, irreversible proteasome inhibitor under investigation for the treatment of hematological… 
2006
2006
The Novel, Irreversible Proteasome Inhibitor PR-171 Demonstrates Potent Anti-Tumor Activity in Pre-Clinical Models of Multiple Myeloma, and Overcomes Bortezomib Resistance.
Introduction: The ubiquitin-proteasome pathway has been validated as a therapeutic target with the approval of the small molecule… 
2005
2005
Pharmacokinetics, Pharmacodynamics and Anti-Tumor Efficacy of PR-171, a Novel Inhibitor of the 20S Proteasome.
Clinical studies using the boronic acid-based proteasome inhibitor bortezomib (VelcadeTM) have validated the proteasome as a… 
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