Phospholipase C
Phospholipase C (PLC) hydrolyzes PI(4,5)P2 to generate IP3 and DAG, positioning PLC as a central enzyme in phosphoinositide metabolism and intracellular signal transduction[1]. Mechanistically, IP3 regulates intracellular Ca2+ release, while DAG supports protein kinase C activation, linking receptor stimulation to calcium signaling, proliferation, differentiation, and motility[1][2]. In mammals, PLC enzymes form structurally defined isozyme classes with shared catalytic activity but distinct activation mechanisms and physiological functions[1][3]. Compared with PLCβ, which couples strongly to G-protein-coupled receptor signaling, PLCγ functions downstream of receptor and non-receptor tyrosine kinases and contains γ-specific regulatory domains that support isoform-specific signaling[4]. Disease-focused studies link PLCγ dysfunction to immune disorders and cancer, while PLCγ2 mutations connect immune dysregulation, malignancy, and neurodegeneration models[4][5]. For experimental applications, U73122 has been widely used to probe PLC-dependent signaling, but purified-enzyme studies showed direct PLC activation by U73122, so inhibitor-based experiments require careful controls[6][7].
Referencias:
- [1]. Kadamur G, et al. Mammalian phospholipase C. Annu Rev Physiol. 2013;75:127-54. [Content Brief]
- [2]. Kanemaru K, et al. Activation Mechanisms and Diverse Functions of Mammalian Phospholipase C. Biomolecules. 2023 May 31;13(6):915. [Content Brief]
- [3]. Nakamura Y, et al. Regulation and physiological functions of mammalian phospholipase C. J Biochem. 2017 Apr 1;161(4):315-321. [Content Brief]
- [4]. Koss H, et al. Dysfunction of phospholipase Cγ in immune disorders and cancer. Trends Biochem Sci. 2014 Dec;39(12):603-11. [Content Brief]
- [5]. Jackson JT, et al. The role of PLCγ2 in immunological disorders, cancer, and neurodegeneration. J Biol Chem. 2021 Aug;297(2):100905. [Content Brief]
- [6]. Bleasdale JE, et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther. 1990 Nov;255(2):756-68. [Content Brief]
- [7]. Klein RR, et al. Direct activation of human phospholipase C by its well known inhibitor u73122. J Biol Chem. 2011 Apr 8;286(14):12407-16. [Content Brief]
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