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Platelet-activating Factor Family Related Drug Discovery Products

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One of the most potent and diverse mediators known in mammals is platelet-activating factor (PAF). It was initially referred to as "a soluble factor" that influenced the release of histamine and serotonin from platelets in a leukocyte-dependent manner. PAF is currently recognized as an alkyl phosphoglyceride, a class of biologically active, structurally related phospholipids with a wide range of physiological effects. Cell-to-cell communication, which can act as an intracellular or intercellular messenger, is assumed to be mediated by PAF.

The alkylacylglycerophosphocholine remodeling pathway. Fig.1. The alkylacylglycerophosphocholine remodeling pathway. (Mazereeuw, 2013)

Creative Biolabs is proud to offer our clients a series of platelet-activating factor family in vitro assays and products with the best quality:

Overview of Platelet-activating Factor Family

Following PAF production and delivery, the PAF receptor interacts, which causes a range of signals depending on the target cell. The PAF receptor is highly expressed, and two promoters that flank two 5' noncoding exons regulate it differently. Selective interaction of the PAF receptor with heterotrimeric G proteins boosts the production of inositol 1,4,5-trisphosphate and the release of arachidonic acid, mobilizes calcium, and reduces the buildup of cyclic AMP. Through the activation of phospholipases A2, C, and D, the PAF receptor mediates signaling by enlisting the assistance of several second messengers. Both pertussis toxin-sensitive and -insensitive G proteins link to the PAF receptor. As a result, different types of G proteins are engaged in different situations. For example, activation of phospholipase C (PLC) is likely mediated by Gαq/11 and partially by Gαo, activation of p38 by Gαq/11, and activation of ERK by Gαq/11, Gαo, and Gβγ.

Signal transduction of PAF receptor. Fig.2. Signal transduction of PAF receptor. (Montrucchio, 2000)

Platelet-activating Factor Family Drug Discovery

Despite mounting evidence linking PAF to a number of clinical disorders, this mediator is still lacking a clear physiological function. Due to its angiogenic capabilities and ability to enhance the effects of specific polypeptide mediators, PAF may have a function in the cardiovascular system's embryogenesis. PAF has also been linked to physiological blood pressure regulation, primarily through its impact on renal vascular circulation. The fact that the human heart is capable of producing PAF, expresses PAF receptors, and is susceptible to the detrimental inotropic effects of PAF, in particular, implies that this mediator may play a function in the local response of the heart to damage.

References

  1. Mazereeuw, G.; et al. Platelet activating factors in depression and coronary artery disease: a potential biomarker related to inflammatory mechanisms and neurodegeneration. Neuroscience & Biobehavioral Reviews. 2013, 37(8): 1611-1621.
  2. Montrucchio, G.; et al. Role of platelet-activating factor in cardiovascular pathophysiology. Physiological Reviews. 2000, 80(4): 1669-1699.

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