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 …

The alpha keto amide moiety as a privileged motif in medicinal chemistry: current insights and emerging opportunities

M Robello, E Barresi, E Baglini, S Salerno… - Journal of Medicinal …, 2021 - ACS Publications
Over the years, researchers in drug discovery have taken advantage of the use of privileged
structures to design innovative hit/lead molecules. The α-ketoamide motif is found in many …

[HTML][HTML] Calpain activation and progression of inflammatory cycles in Parkinson's disease

A Gao, HM McCoy, V Zaman, DC Shields… - Frontiers in …, 2022 - ncbi.nlm.nih.gov
Parkinson's disease (PD) is a progressive, neurodegenerative condition of the central
nervous system (CNS) affecting 6.3 million people worldwide with no curative treatments …

The cell-permeable mitochondrial calcium uniporter inhibitor Ru265 preserves cortical neuron respiration after lethal oxygen glucose deprivation and reduces hypoxic …

RJ Novorolsky, M Nichols, JS Kim… - Journal of Cerebral …, 2020 - journals.sagepub.com
The mitochondrial calcium (Ca2+) uniporter (MCU) mediates high-capacity mitochondrial
Ca2+ uptake implicated in ischemic/reperfusion cell death. We have recently shown that …

The signaling symphony: T cell receptor tunes cytokine-mediated T cell differentiation

W Huang, A August - Journal of Leucocyte Biology, 2015 - academic.oup.com
T cell development, differentiation, and maintenance are orchestrated by 2 key signaling
axes: the antigen-specific TCR and cytokine-mediated signals. The TCR signals the …

Ageing and myeloid-derived suppressor cells: possible involvement in immunosenescence and age-related disease

V Bueno, OA Sant'Anna, JM Lord - Age, 2014 - Springer
Infections, cancer and autoimmune diseases occur more frequently in the elderly, and
although many factors contribute to this, the age-related remodelling of the immune system …

Oxidative stress: a possible trigger for pelvic organ prolapse

RD Marcu, DLD Mischianu, L Iorga… - Journal of …, 2020 - Wiley Online Library
Pelvic organ prolapse is a frequent health problem in women, encountered worldwide, its
physiopathology being still incompletely understood. The integrity of the pelvic‐supportive …

Axonal degeneration in multiple sclerosis: can we predict and prevent permanent disability?

JY Lee, K Taghian, S Petratos - Acta neuropathologica communications, 2014 - Springer
Axonal degeneration is a major determinant of permanent neurological impairment during
multiple sclerosis (MS). Due to the variable course of clinical disease and the heterogeneity …

Compromised axon initial segment integrity in EAE is preceded by microglial reactivity and contact

KC Clark, A Josephson, SD Benusa, RK Hartley… - Glia, 2016 - Wiley Online Library
Axonal pathology is a key contributor to long‐term disability in multiple sclerosis (MS), an
inflammatory demyelinating disease of the central nervous system (CNS), but the …