An updated patent review of calpain inhibitors (2012-2014)

Research output: Contribution to journalReview article

20 Citations (Scopus)

Abstract

Calpain is a family of cysteine proteases found in eukaryotes and a few bacteria. There is considerable interest in the search for calpain inhibitors because the enzyme has been implicated in several diseases including ocular disorders, neurodegenerative disorders, metabolic disorders and cancer. Areas covered: An overview of calpain inhibitors disclosed between 2012 and 2014 is presented. Among these are epoxysuccinates, dipeptide imaging agents, macrocyclic inhibitors, α-helical peptidomimetic inhibitors, carboxamides, 5-azolones and α-mercaptoacrylates. Additionally, preclinical studies of calpain inhibitors in pathologies such blood disorders, ocular disorders, neurological disorders and muscle disorders are discussed. Expert opinion: Major advances made in calpain inhibitor research between 2012 and 2014 include: i) the discovery of cytosolic-stable carboxamide calpain inhibitors; ii) synthesis of epoxysuccinates with excellent bioavailability; iii) disclosure of the X-ray crystal structures of novel α-mercaptoacrylates bound to the pentaEF hand region from human calpain; and iv) disclosure of calpain inhibitors as anti-sickling agents. Several calpain inhibitors were reported but limited effort was directed towards the discovery of calpain isoform selective agents, which continues to dampen the therapeutic potential of calpain inhibitors.

Original languageEnglish (US)
Pages (from-to)17-31
Number of pages15
JournalExpert Opinion on Therapeutic Patents
Volume25
Issue number1
DOIs
StatePublished - Jan 1 2015

Fingerprint

Calpain
Disclosure
Peptidomimetics
Cysteine Proteases
calpain inhibitors
Dipeptides
Expert Testimony
Muscular Diseases
Nervous System Diseases
Eukaryota
Neurodegenerative Diseases
Biological Availability
Protein Isoforms
Hand
X-Rays
Pathology
Bacteria
Enzymes
Research
Neoplasms

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery

Cite this

An updated patent review of calpain inhibitors (2012-2014). / Donkor, Isaac.

In: Expert Opinion on Therapeutic Patents, Vol. 25, No. 1, 01.01.2015, p. 17-31.

Research output: Contribution to journalReview article

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