Small molecule active site directed tools for studying human caspases

M Poreba, A Szalek, P Kasperkiewicz, W Rut… - Chemical …, 2015 - ACS Publications
Caspases are proteases of clan CD and were described for the first time more than two
decades ago. They play critical roles in the control of regulated cell death pathways …

Caspase allostery and conformational selection

AC Clark - Chemical reviews, 2016 - ACS Publications
The role of caspase proteases in regulated processes such as apoptosis and inflammation
has been studied for more than two decades, and the activation cascades are known in …

[HTML][HTML] Cacidases: caspases can cleave after aspartate, glutamate and phosphoserine residues

JE Seaman, O Julien, PS Lee, TJ Rettenmaier… - Cell Death & …, 2016 - nature.com
Caspases are a family of proteases found in all metazoans, including a dozen in humans,
that drive the terminal stages of apoptosis as well as other cellular remodeling and …

Caspase‐8 and caspase‐7 sequentially mediate proteolytic activation of acid sphingomyelinase in TNF‐R1 receptosomes

B Edelmann, U Bertsch, V Tchikov… - The EMBO …, 2011 - embopress.org
We previously demonstrated that tumour necrosis factor (TNF)‐induced ceramide production
by endosomal acid sphingomyelinase (A‐SMase) couples to apoptosis signalling via …

Caspase-3 activators as anticancer agents

N Srivastava, AK Saxena - Current Protein and Peptide Science, 2023 - ingentaconnect.com
Background: The cancer is still a major cause of death worldwide. Among different targets to
design anticancer agents, caspase-3 is an important target as its cleavage and activation …

Highly potent monomethyl auristatin E prodrug activated by caspase-3 for the chemoradiotherapy of triple-negative breast cancer

SW Chung, YS Cho, JU Choi, HR Kim, TH Won… - Biomaterials, 2019 - Elsevier
Despite the emergence of advanced therapeutics such as targeted therapy and
immunotherapy in the modern oncology, cytotoxic chemotherapy still remains as the first-line …

Reprogramming caspase-7 specificity by regio-specific mutations and selection provides alternate solutions for substrate recognition

ME Hill, DJ MacPherson, P Wu, O Julien… - ACS chemical …, 2016 - ACS Publications
The ability to routinely engineer protease specificity can allow us to better understand and
modulate their biology for expanded therapeutic and industrial applications. Here, we report …

[HTML][HTML] Proteome-wide substrate analysis indicates substrate exclusion as a mechanism to generate caspase-7 versus caspase-3 specificity

D Demon, P Van Damme, TV Berghe… - Molecular & Cellular …, 2009 - ASBMB
Caspase-3 and-7 are considered functionally redundant proteases with similar proteolytic
specificities. We performed a proteome-wide screen on a mouse macrophage lysate using …

Substrate-induced conformational changes occur in all cleaved forms of caspase-6

S Vaidya, EM Velázquez-Delgado… - Journal of molecular …, 2011 - Elsevier
Caspase-6 is an apoptotic cysteine protease that also governs disease progression in
Huntington's and Alzheimer's diseases. Caspase-6 is of great interest as a target for …

[HTML][HTML] Isoquinoline-1, 3, 4-trione derivatives inactivate caspase-3 by generation of reactive oxygen species

JQ Du, J Wu, HJ Zhang, YH Zhang, BY Qiu… - Journal of biological …, 2008 - ASBMB
Caspase-3 is an attractive therapeutic target for treatment of diseases involving disregulated
apoptosis. We report here the mechanism of caspase-3 inactivation by isoquinoline-1, 3, 4 …