C1 domains: structure and ligand-binding properties

J Das, GM Rahman - Chemical reviews, 2014 - ACS Publications
C1 domains are small zinc-binding structural units of approximately 50 amino acid residues,
originally discovered as lipid-binding modules in protein kinase C (PKC) isoforms. Although …

Protein kinase C activation as a potential therapeutic strategy in Alzheimer's disease: is there a role for embryonic lethal abnormal vision‐like proteins?

V Talman, A Pascale, M Jäntti… - Basic & clinical …, 2016 - Wiley Online Library
Abstract Alzheimer's disease (AD), the most common cause of dementia, is an irreversible
and progressive neurodegenerative disorder. It affects predominantly brain areas that are …

Synthesis and evaluation of DAG-lactone derivatives with HIV-1 latency reversing activity

T Ishii, T Kobayakawa, K Matsuda, K Tsuji… - European journal of …, 2023 - Elsevier
Cells latently infected with human immunodeficiency virus type 1 (HIV-1) prevent people
living with HIV-1 from obtaining a cure to the infectious disease. Latency reversing agents …

Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C

GB af Gennas, V Talman, O Aitio… - Journal of medicinal …, 2009 - ACS Publications
Protein kinase C (PKC) is a widely studied molecular target for the treatment of cancer and
other diseases. We have approached the issue of modifying PKC function by targeting the …

[HTML][HTML] Natural and synthetic lactones possessing antitumor activities

Y Kim, S Sengupta, T Sim - International Journal of Molecular Sciences, 2021 - mdpi.com
Cancer is one of the leading causes of death globally, accounting for an estimated 8 million
deaths each year. As a result, there have been urgent unmet medical needs to discover …

[HTML][HTML] Differential regulation of gene expression in lung cancer cells by diacyglycerol-lactones and a phorbol ester via selective activation of protein kinase C …

M Cooke, V Casado-Medrano, J Ann, J Lee… - Scientific reports, 2019 - nature.com
Despite our extensive knowledge on the biology of protein kinase C (PKC) and its
involvement in disease, limited success has been attained in the generation of PKC isozyme …

[HTML][HTML] Phosphorylation of α6-tubulin by protein kinase Cα activates motility of human breast cells

TP Abeyweera, X Chen, SA Rotenberg - Journal of Biological Chemistry, 2009 - ASBMB
Engineered overexpression of protein kinase Cα (PKCα) was previously shown to endow
nonmotile MCF-10A human breast cells with aggressive motility. A traceable mutant of PKCα …

[HTML][HTML] Characterization of AJH-836, a diacylglycerol-lactone with selectivity for novel PKC isozymes

M Cooke, X Zhou, V Casado-Medrano… - Journal of Biological …, 2018 - ASBMB
Diacylglycerol (DAG) is a key lipid second messenger downstream of cellular receptors that
binds to the C1 domain in many regulatory proteins. Protein kinase C (PKC) isoforms …

Activation of Munc13-1 by Diacylglycerol (DAG)-Lactones

J Das, Y You, K Mathukumalli, J Ann, J Lee… - Biochemistry, 2023 - ACS Publications
Munc13-1 is a key protein necessary for vesicle fusion and neurotransmitter release in the
brain. Diacylglycerol (DAG)/phorbol ester binds to its C1 domain in the plasma membrane …

Current status and future prospects of C1 domain ligands as drug candidates

G Boije af Gennas, V Talman… - Current topics in …, 2011 - ingentaconnect.com
The second messenger diacylglycerol (DAG) plays a central role in the signal transduction
of G-protein coupled receptors and receptor tyrosine kinases by binding to C1 domain of …