A method of determining whether a protein kinase C (PKC) has been activated, the method comprising determining whether or to what extent a phosphorylatable site on the said protein kinase C, which site is associated with activation of said protein kinase C, has been phosphorylated. A reagent which is capable of distinguishing between the presence or absence of a phosphate moiety at a phosphorylatable site in a protein kinase C, which site is associated with activation of said protein kinase C. Preferably, the reagent is an antibody.

Protein Kinase C

1.1. Discovery of the Phospholipase A2 Superfamily
Phospholipases represent one of the earliest enzyme activities to be identified and studied and the phospholipase A2 (PLA2) superfamily (see defining specificity1 in Figure 1) traces its roots to the identification of lytic actions of snake venom at the end of the 19th century. The enzyme was first purified and characterized from cobra venom and later from rattlesnake venom. As protein sequencing methodologies advanced in the 1970’s, it became apparent that these enzymes had an unusually large number of cysteines (over 10% of the amino acids) and as secreted enzymes, that they were all in the form of disulfide bonds. It was further recognized that in the case of PLA2, cobras and rattlesnakes had six disulfides in common, but one disulfide bond is located in distinctly different locations. This led to the designation of Type 1 and Type 2 for cobras (old world snakes) and rattlesnakes (new world snakes), respectively.2 During that same period, studies on the porcine pancreatic digestive enzyme that hydrolyzes phospholipids led to the determination that this mammalian enzyme (and also the human pancreatic enzyme) had the same disulfide bonding pattern as cobras and hence the designation as IB with the cobra enzyme as IA.






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Figure 1


The specific reaction catalyzed by phospholipase A2 at the sn-2 position of the glycerol backbone is shown. X, any of a number of polar headgroups; R1, fatty acids, or alkyl, or alkenyl groups and R2, fatty acids or acyl moieties.

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Phospholipase A2 enzymes: physical structure, biological function, disease implication, chemical inhibition, and therapeutic intervention.

Type 2 diabetes is a complex and heterogeneous disorder presently affecting more than 100 million people worldwide and causing serious socio-economic problems. Appropriate experimental models are essential tools for understanding the pathogenesis, complications, and genetic or environmental influences that increase the risks of type 2 diabetes and testing of various therapeutic agents. The animal models of type 2 diabetes can be obtained either spontaneously or induced by chemicals or dietary or surgical manipulations and/or by combination thereof. In recent years, large number of new genetically modified animal models including transgenic, generalized knock-out and tissue-specific knockout mice have been engineered for the study of diabetes. This review gives an overview on the animal models of type 2 diabetes with reference to their origin/source, characteristic features, underlying causes/mechanism(s), advantages and disadvantages to the investigators in diabetes research. In addition, it especially describes the appropriate selection and usefulness of different animal models in preclinical testing of various new chemical entities (NCEs) for the treatment of type 2 diabetes.

Animal models in type 2 diabetes research: an overview.

Nanoparticles and microparticles for skin drug delivery

Plasmalogens: biosynthesis and functions

https://febs.onlinelibrary.wiley.com/doi/pdf/10.1016/0014-5793%2880%2980633-8

Jean-Jacques Godfroid

Papers

Platelet activating factor (PAF-acether): total synthesis of 1-O-octadecyl 2-O-acetyl sn-glycero-3-phosphoryl choline

New total synthesis and high resolution 1H NMR spectrum of platelet-activating factor, its enantiomer and racemic mixtures.

Structural analogs of platelet-activating factor (PAF-acether)

Alkyl analogs of diacylglycerol as activators of protein kinase C.

4-Alkoxybenzamidines as new potent phospholipase A2 inhibitors