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Ga-q proteins: molecular pharmacology and therapeutic potential
Kamato, Danielle1; Mitra, Partha1; Davis, Felicity1; Osman, Narin1,2,3; Chaplin, Rebecca1; Cabot, Peter J.1; Afroz, Rizwana4; Thomas, Walter5; Zheng, Wenhua6; Kaur, Harveen7; Brimble, Margaret7; Little, Peter J.1,2,8

Seven transmembrane G protein-coupled receptors (GPCRs) have gained much interest in recent years as it is the largest class among cell surface receptors. G proteins lie in the heart of GPCRs signalling and therefore can be therapeutically targeted to overcome complexities in GPCR responses and signalling. G proteins are classified into four families (G(i), G(s), G(12/13) and G(q)); G(q) is further subdivided into four classes. Among them G(alpha q) and G(alpha q/11) isoforms are most crucial and ubiquitously expressed; these isoforms are almost 88% similar at their amino acid sequence but may exhibit functional divergences. However, uncertainties often arise about G(alpha q) and G(alpha q/11) inhibitors, these G proteins might also have suitability to the invention of novel-specific inhibitors for each isoforms. YM-254890 and UBO-QIC are discovered as potent inhibitors of G(alpha q) functions and also investigated in thrombin protease-activated receptor (PAR)-1 inhibitors and platelet aggregation inhibition. The most likely G protein involved in PAR-1 stimulates responses is one of the G(alpha q) family isoforms. In this review, we highlight the molecular structures and pharmacological responses of G(alpha q) family which may reflect the biochemical and molecular role of G(alpha q) and G(alpha q/11). The advanced understanding of G(alpha q) and G(alpha q/11) role in GPCR signalling may shed light on our understanding on cell biology, cellular physiology and pathophysiology and also lead to the development of novel therapeutic agents for a number of diseases.

Keywordg Proteins Isoforms g Protein-coupled Receptors Gpcrs Par-1 Hyperelongation Atherosclerosis g Alpha q
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Indexed BySCI
WOS Research AreaBiochemistry & Molecular Biology ; Cell Biology
WOS SubjectBiochemistry & Molecular Biology ; Cell Biology
WOS IDWOS:000398508000002
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Cited Times [WOS]:16   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.School of Pharmacy, Pharmacy Australia Centre of Excellence, The University of Queensland, 20 Cornwall Street, Woolloongabba, QLD 4102, Australia
2.School of Medical Sciences, RMIT University, Bundoora, VIC 3083, Australia
3.Department of Immunology, Monash University, Melbounre, VIC 3004, Australia
4.Department of Biochemistry, Primeasia University, Banani 1213, Bangladesh
5.School of Biomedical Sciences, The University of Queensland, St. Lucia, QLD 4102, Australia
6.Faculty of Health Sciences, University of Macau, Taipa, Macau, China
7.Department of Chemistry, School of Biological Sciences, University of Auckland, Auckland, New Zealand
8.Xinhua College of Sun Yat-sen University, Tianhe District, Guangzhou 510520, China
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GB/T 7714
Kamato, Danielle,Mitra, Partha,Davis, Felicity,et al. Ga-q proteins: molecular pharmacology and therapeutic potential[J]. CELLULAR AND MOLECULAR LIFE SCIENCES,2017,74(8):1379-1390.
APA Kamato, Danielle.,Mitra, Partha.,Davis, Felicity.,Osman, Narin.,Chaplin, Rebecca.,...&Little, Peter J..(2017).Ga-q proteins: molecular pharmacology and therapeutic potential.CELLULAR AND MOLECULAR LIFE SCIENCES,74(8),1379-1390.
MLA Kamato, Danielle,et al."Ga-q proteins: molecular pharmacology and therapeutic potential".CELLULAR AND MOLECULAR LIFE SCIENCES 74.8(2017):1379-1390.
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