Proteasome inhibitor patents (2010 – present)
| Autor: | Kenyon G. Daniel, Rainer Metcalf, Latanya M. Scott, Q. Ping Dou |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Drug
media_common.quotation_subject Proteolysis Pharmacology Biology Patents as Topic chemistry.chemical_compound Neoplasms Drug Discovery medicine Animals Humans Multiple myeloma media_common medicine.diagnostic_test Drug discovery Bortezomib General Medicine medicine.disease Carfilzomib chemistry Proteasome Drug Design Proteasome inhibitor Drug Therapy Combination Proteasome Inhibitors medicine.drug |
| Zdroj: | Expert Opinion on Therapeutic Patents. 24:369-382 |
| ISSN: | 1744-7674 1354-3776 |
| Popis: | Over the past 3 years, numerous patents and patent applications have been submitted and published involving compounds designed to inhibit the proteasome. Proteasome inhibition has been of great interest in cancer research since disruption of proteolysis leads to a significant buildup of cytotoxic proteins and activation of apoptotic pathways, particularly in rapidly proliferating cells. The current standards in proteasome inhibition are the only FDA-approved inhibitors, bortezomib and carfilzomib. Although these drugs are quite effective in treating multiple myeloma and other blood tumors, there are shortcomings, including toxicities and resistance. Most of the current patents attempt to improve on existing compounds, by increasing bioavailability and selectivity, while attempting to reduce toxicity. A general categorization of similar compounds was employed to evaluate and compare drug design strategies.This review focuses on novel compounds and subsequent analogs developed for proteasome inhibition, used in preventing and treating human cancers. A comprehensive description and categorization of patents related to each type of compound and its derivatives, as well as their uses and efficacies as anticancer agents is included. A review of combination therapy patents has also been included.Although there are many diverse chemical scaffolds being published, there are few patented proteasome inhibitors whose method of inhibition is genuinely novel. Most patents utilize a destructive chemical warhead to attack the catalytic threonine residue of the proteasome active sites. Few patents try to depart from this, emphasizing the need for developing new mechanisms of action and specific targeting. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|