Calpain research for drug discovery: challenges and potential

Y Ono, TC Saido, H Sorimachi - Nature Reviews Drug Discovery, 2016 - nature.com
Calpains are a family of proteases that were scientifically recognized earlier than
proteasomes and caspases, but remain enigmatic. However, they are known to participate in …

[HTML][HTML] Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors

M Siklos, M BenAissa, GRJ Thatcher - Acta Pharmaceutica Sinica B, 2015 - Elsevier
Cysteine proteases continue to provide validated targets for treatment of human diseases. In
neurodegenerative disorders, multiple cysteine proteases provide targets for enzyme …

Brain neurotrauma: molecular, neuropsychological, and rehabilitation aspects

FH Kobeissy - 2015 - books.google.com
With the contribution from more than one hundred CNS neurotrauma experts, this book
provides a comprehensive and up-to-date account on the latest developments in the area of …

Development of α-helical calpain probes by mimicking a natural protein–protein interaction

H Jo, N Meinhardt, Y Wu, S Kulkarni, X Hu… - Journal of the …, 2012 - ACS Publications
We have designed a highly specific inhibitor of calpain by mimicking a natural protein–
protein interaction between calpain and its endogenous inhibitor calpastatin. To enable this …

Structure–function relationships in calpains

RL Campbell, PL Davies - Biochemical Journal, 2012 - portlandpress.com
Calpains are a family of complex multi-domain intracellular enzymes that share a calcium-
dependent cysteine protease core. These are not degradative enzymes, but instead carry …

Disruption of the axon initial segment cytoskeleton is a new mechanism for neuronal injury

DP Schafer, S Jha, F Liu, T Akella… - Journal of …, 2009 - Soc Neuroscience
Many factors contribute to nervous system dysfunction and failure to regenerate after injury
or disease. Here, we describe a previously unrecognized mechanism for nervous system …

Functional imaging of proteases: recent advances in the design and application of substrate-based and activity-based probes

LE Edgington, M Verdoes, M Bogyo - Current opinion in chemical biology, 2011 - Elsevier
Proteases are enzymes that cleave peptide bonds in protein substrates. This process can be
important for regulated turnover of a target protein but it can also produce protein fragments …

Concerted multi-pronged attack by calpastatin to occlude the catalytic cleft of heterodimeric calpains

T Moldoveanu, K Gehring, DR Green - Nature, 2008 - nature.com
The Ca2+-dependent cysteine proteases, calpains, regulate cell migration, cell death,
insulin secretion, synaptic function and muscle homeostasis. Their endogenous inhibitor …

De novo design of tyrosine and serine kinase-driven protein switches

NB Woodall, Z Weinberg, J Park, F Busch… - Nature Structural & …, 2021 - nature.com
Kinases play central roles in signaling cascades, relaying information from the outside to the
inside of mammalian cells. De novo designed protein switches capable of interfacing with …

Calpains for dummies: What you need to know about the calpain family

S Spinozzi, S Albini, H Best, I Richard - Biochimica et Biophysica Acta (BBA …, 2021 - Elsevier
This review was written in memory of our late friend, Dr. Hiroyuki Sorimachi, who, following
the steps of his mentor Koichi Suzuki, a pioneer in calpain research, has made tremendous …