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Human GPRC6A Mediates Testosterone-Induced Mitogen-Activated Protein Kinases and mTORC1 Signaling in Prostate Cancer Cells.

Ruisong Ye, Min Pi, Mohammed M Nooh, Suleiman W Bahout, L Darryl Quarles,

G protein-coupled receptor family C group 6 member A (GPRC6A) is activated by testosterone and modulates prostate cancer progression. Most humans have a GPRC6A variant that contains a recently evolved KGKY insertion/deletion in the third intracellular loop (ICL3) (designated as GPRC6AICL3_KGKY) that replaces the ancestral KGRKLP sequence (GPRC6AICL3_RKLP) present in ... Read more >>

Mol. Pharmacol. (Molecular pharmacology)
[2019, 95(5):563-572]

Cited: 0 times

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Cardiovascular Interactions between Fibroblast Growth Factor-23 and Angiotensin II.

Min Pi, Ruisong Ye, Xiaobin Han, Benjamin Armstrong, Xue Liu, Yuanjian Chen, Yao Sun, L Darryl Quarles,

Both the activation of the renin angiotensin aldosterone system (RAAS) and elevations of circulating Fibroblast Growth Factor-23 (FGF-23) have been implicated in the pathogenesis of left ventricular hypertrophy (LVH) in chronic kidney disease. To investigate potential cross-talk between RAAS and FGF-23, we administered angiotensin II (Ang II) to wild-type rodents ... Read more >>

Sci Rep (Scientific reports)
[2018, 8(1):12398]

Cited: 3 times

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GPCR6A Is a Molecular Target for the Natural Products Gallate and EGCG in Green Tea.

Min Pi, Karan Kapoor, Ruisong Ye, Jeremy C Smith, Jerome Baudry, Leigh D Quarles,

SCOPE:The molecular mechanisms whereby gallates in green tea exert metabolic effects are poorly understood. METHODS AND RESULTS:We found that GPRC6A, a multi-ligand-sensing G-protein-coupled receptor that regulates energy metabolism, sex hormone production, and prostate cancer progression, is a target for gallates. Sodium gallate (SG), gallic acid (GA) > ethyl gallate (EG) ... Read more >>

Mol Nutr Food Res (Molecular nutrition & food research)
[2018, 62(8):e1700770]

Cited: 1 time

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Cardiovascular Effects of Renal Distal Tubule Deletion of the FGF Receptor 1 Gene.

Xiaobin Han, Jed Ross, Ganesh Kolumam, Min Pi, Junichiro Sonoda, Gwendalyn King, L Darryl Quarles,

The bone-derived hormone fibroblast growth factor-23 (FGF-23) activates complexes composed of FGF receptors (FGFRs), including FGFR1, and α-Klotho in the kidney distal tubule (DT), leading to increased sodium retention and hypertension. However, the role of FGFR1 in regulating renal processes linked to hypertension is unclear. Here, we investigated the effects ... Read more >>

J. Am. Soc. Nephrol. (Journal of the American Society of Nephrology : JASN)
[2018, 29(1):69-80]

Cited: 6 times

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CRISPR/Cas9 targeting of GPRC6A suppresses prostate cancer tumorigenesis in a human xenograft model.

Ruisong Ye, Min Pi, John V Cox, Satoru K Nishimoto, L Darryl Quarles,

GPRC6A is implicated in the pathogenesis of prostate cancer, but its role remains uncertain because of a purported tolerant gene variant created by substitution of a K..Y polymorphism in the 3rd intracellular loop (IL) that evolved in the majority of humans and replaces the ancestral RKLP present in 40% of ... Read more >>

J. Exp. Clin. Cancer Res. (Journal of experimental & clinical cancer research : CR)
[2017, 36(1):90]

Cited: 5 times

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GPRC6A: Jack of all metabolism (or master of none).

Min Pi, Satoru Kenneth Nishimoto, L Darryl Quarles,

BACKGROUND:GPRC6A, a widely expressed G-protein coupled receptor, is proposed to be a master regulator of complex endocrine networks and metabolic processes. GPRC6A is activated by multiple ligands, including osteocalcin (Ocn), testosterone (T), basic amino acids, and various cations. SCOPE OF REVIEW:We review the controversy surrounding GPRC6A functions. In mice, GPRC6A ... Read more >>

Mol Metab (Molecular metabolism)
[2017, 6(2):185-193]

Cited: 8 times

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[The "regulating conception-governor vessel" acupuncture method for infertility of polycystic ovarian syndrome].

Yuanyuan Zhuo, Jiaman Wu, Wanshan Lin, Min Pi, Pengdian Chen, Zhuoxin Yang,

To compare clinical efficacy differences between"regulating conception-governor vessel" acupuncture method and clomiphene for infertility of polycystic ovarian syndrome (PCOS).One hundred patients of PCOS were randomly assigned into an observation group and a control group, 50 cases in each one. The patients in the observation group were treated with"regulating Conception-Governor Vessel" ... Read more >>

Zhongguo Zhen Jiu (Zhongguo zhen jiu = Chinese acupuncture & moxibustion)
[2016, 36(12):1237-1241]

Cited: 0 times

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Differential Regulatory Role of Soluble Klothos on Cardiac Fibrogenesis in Hypertension.

Xue Liu, Yuanjian Chen, Cody W McCoy, Tieqiang Zhao, Darryl L Quarles, Min Pi, Syamal K Bhattacharya, Gwendalyn King, Yao Sun,

Soluble Klotho functions as an endocrine factor that plays important roles in a variety of pathophysiological processes. Soluble Klotho contains 130 KDa and 65 KDa isoforms. However, their distinct individual functional heterogeneity remains uncertain. Herein, we investigated the regulatory role of two soluble Klothos on cardiac fibrogenic responses.The effect of ... Read more >>

Am. J. Hypertens. (American journal of hypertension)
[2016, 29(10):1140-1147]

Cited: 9 times

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Evidence for Osteocalcin Binding and Activation of GPRC6A in β-Cells.

Min Pi, Karan Kapoor, Ruisong Ye, Satoru Kenneth Nishimoto, Jeremy C Smith, Jerome Baudry, Leigh Darryl Quarles,

The possibility that G protein-coupled receptor family C member A (GPRC6A) is the osteocalcin (Ocn)-sensing G protein-coupled receptor that directly regulates pancreatic β-cell functions is controversial. In the current study, we found that Ocn and an Ocn-derived C-terminal hexapeptide directly activate GPRC6A-dependent ERK signaling in vitro. Computational models probe the ... Read more >>

Endocrinology (Endocrinology)
[2016, 157(5):1866-1880]

Cited: 23 times

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Structural and Functional Evidence for Testosterone Activation of GPRC6A in Peripheral Tissues.

Min Pi, Karan Kapoor, Yunpeng Wu, Ruisong Ye, Susan E Senogles, Satoru K Nishimoto, Dong-Jin Hwang, Duane D Miller, Ramesh Narayanan, Jeremy C Smith, Jerome Baudry, L Darryl Quarles,

G protein-coupled receptor (GPCR) family C group 6 member A (GPRC6A) is a multiligand GPCR that is activated by cations, L-amino acids, and osteocalcin. GPRC6A plays an important role in the regulation of testosterone (T) production and energy metabolism in mice. T has rapid, transcription-independent (nongenomic) effects that are mediated ... Read more >>

Mol. Endocrinol. (Molecular endocrinology (Baltimore, Md.))
[2015, 29(12):1759-1773]

Cited: 12 times

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Electro-acupuncture at Conception and Governor vessels and transplantation of umbilical cord blood-derived mesenchymal stem cells for treating cerebral ischemia/reperfusion injury.

Haibo Yu, Pengdian Chen, Zhuoxin Yang, Wenshu Luo, Min Pi, Yonggang Wu, Ling Wang,

Mesenchymal stem cell transplantation is a novel means of treating cerebral ischemia/reperfusion, and can promote angiogenesis and neurological functional recovery. Acupuncture at Conception and Governor vessels also has positive effects as a treatment for cerebral ischemia/reperfusion. Therefore, we hypothesized that electro-acupuncture at Conception and Governor vessels plus mesenchymal stem cell ... Read more >>

Neural Regen Res (Neural regeneration research)
[2014, 9(1):84-91]

Cited: 2 times

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Combinatorial effects of conception and governor vessel electroacupuncture and human umbilical cord blood-derived mesenchymal stem cells on pathomorphologic lesion and cellular apoptosis in rats with cerebral ischemia/reperfusion.

Zhuoxin Yang, Pengdian Chen, Haibo Yu, Wenshu Luo, Min Pi, Yonggang Wu, Ling Wang, Fuxia Yang, Yanhua Gou,

To investigate the combinatorial effects of conception and governor vessel electroacupuncture (EA) and human umbilical cord blood-derived mesenchymal stem cells (HUCB-MSCs) on pathomorphologic lesion and cellular apoptosis in rats with cerebral ischemia/reperfusion.With the HUCB-MSCs isolated, cultured and identified and the models of cerebral ischemia-reperfusion established, the HUCB-MSCs of passage three ... Read more >>

J Tradit Chin Med (Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan)
[2013, 33(6):779-786]

Cited: 3 times

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Novel bone endocrine networks integrating mineral and energy metabolism.

Min Pi, L Darryl Quarles,

The skeleton is an endocrine organ that regulates energy metabolism through the release of the osteoblast-derived hormone, osteocalcin (Ocn), and phosphate and vitamin D homeostasis through the secretion by osteoblasts and osteocytes of the novel hormone, FGF23 Ocn activates a widely expressed G-protein coupled receptor, GPRC6A, to regulate insulin secretion ... Read more >>

Curr Osteoporos Rep (Current osteoporosis reports)
[2013, 11(4):391-399]

Cited: 19 times

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GPRC6A mediates the effects of L-arginine on insulin secretion in mouse pancreatic islets.

Min Pi, Yunpeng Wu, Nataliya I Lenchik, Ivan Gerling, L Darryl Quarles,

L-arginine (l-Arg) is an insulin secretagogue, but the molecular mechanism whereby it stimulates insulin secretion from β-cells is not known. The possibility that l-Arg regulates insulin secretion through a G protein-coupled receptor (GPCR)-mediated mechanism is suggested by the high expression of the nutrient receptor GPCR family C group 6 member ... Read more >>

Endocrinology (Endocrinology)
[2012, 153(10):4608-4615]

Cited: 33 times

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Multiligand specificity and wide tissue expression of GPRC6A reveals new endocrine networks.

Min Pi, L Darryl Quarles,

Emerging evidence supports the hypothesis that the skeleton is an endocrine organ that regulates energy metabolism through the release of the osteoblast-derived hormone, osteocalcin (Ocn). This bone-pancreas endocrine network is controversial because important gaps remain to be filled in our knowledge of the physiological effects of Ocn in multiple organs ... Read more >>

Endocrinology (Endocrinology)
[2012, 153(5):2062-2069]

Cited: 43 times

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Research advances in treatment of cerebral ischemic injury by acupuncture of conception and governor vessels to promote nerve regeneration.

Zhuo-xin Yang, Peng-dian Chen, Hai-bo Yu, Wen-shu Luo, Yong-gang Wu, Min Pi, Jun-hua Peng, Yong-feng Liu, Shao-yun Zhang, Yan-hua Gou,

Cerebral ischemia is one of the most common diseases treated by acupuncture therapeutics. Recent studies indicated that acupuncture treatment by needling the conception and governor vessels had positive effects in promoting neural regeneration in patients after cerebral ischemia injury. Acupuncture intervention could continuously promote the proliferation and differentiation of the ... Read more >>

Zhong Xi Yi Jie He Xue Bao (Zhong xi yi jie he xue bao = Journal of Chinese integrative medicine)
[2012, 10(1):19-24]

Cited: 4 times

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Study strategies for acupuncture treatment of chronic nonbacterial prostatitis.

Zhuo-xin Yang, Peng-dian Chen, Hai-bo Yu, Min Pi, Wen-shu Luo, Yuan-yuan Zhuo,

By retrospectively reviewing the current status of traditional Chinese medicine (TCM) and Western medicine treatments of chronic nonbacterial prostatitis (CNP), the TCM understanding of its etiologies and pathogenesis, the therapeutic principles and the mechanisms of acupuncture treatment of CNP, the clinical study strategies of acupuncture treatment for CNP were further ... Read more >>

Zhong Xi Yi Jie He Xue Bao (Zhong xi yi jie he xue bao = Journal of Chinese integrative medicine)
[2012, 10(3):293-297]

Cited: 3 times

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GPRC6A regulates prostate cancer progression.

Min Pi, L Darryl Quarles,

GPRC6A is a nutrient sensing GPCR that is activated in vitro by a variety of ligands, including amino acids, calcium, zinc, osteocalcin (OC), and testosterone. The association between nutritional factors and risk of prostate cancer, the finding of increased expression of OC in prostate cancer cells, and the association between ... Read more >>

Prostate (The Prostate)
[2012, 72(4):399-409]

Cited: 32 times

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GPRC6A mediates responses to osteocalcin in β-cells in vitro and pancreas in vivo.

Min Pi, Yunpeng Wu, L Darryl Quarles,

A bone-pancreas endocrine loop has been identified recently that involves insulin secreted from β-cells in the pancreas stimulating insulin receptors in osteoblasts, leading to osteoblastic differentiation and increased secretion of osteocalcin (Ocn), a bone-derived hormone that regulates insulin secretion in β-cells. The identity of the Ocn-sensing receptor in β-cells is ... Read more >>

J. Bone Miner. Res. (Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research)
[2011, 26(7):1680-1683]

Cited: 95 times

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1-[(Phenyl-iminio)amino]-2-naphtho-late.

Ji-Jun Xu, Jun Li, Min Pi, Chuan-Ming Jin,

In the zwitterionic title compound, C(16)H(12)N(2)O, the dihedral angle between the benzene ring and naphthalene ring system is 2.0 (1)°. The azo group adopts a trans configuration and an intra-molecular N-H⋯O hydrogen bond is found. In the crystal, the mol-ecules are packed by strong π-π inter-actions [centroid-centroid distance between aromatic rings ... Read more >>

Acta Crystallogr Sect E Struct Rep Online (Acta crystallographica. Section E, Structure reports online)
[2010, 66(Pt 7):o1752]

Cited: 0 times

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GPRC6A mediates the non-genomic effects of steroids.

Min Pi, Abby L Parrill, L Darryl Quarles,

The identity of the putative G-protein coupled receptor (GPCR) that mediates the non-genomic effects of androgens is unknown. We present in vitro and in vivo evidence that the orphan GPRC6A receptor, a widely expressed calcium and amino acid sensing GPCR, transduces the non-genomic effects of testosterone and other steroids. Overexpression ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2010, 285(51):39953-39964]

Cited: 68 times

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Impaired osteoblast function in GPRC6A null mice.

Min Pi, Lishu Zhang, Shu-Feng Lei, Min-Zhao Huang, Wenyu Zhu, Jianghong Zhang, Hui Shen, Hong-Wen Deng, L Darryl Quarles,

GPRC6A is a widely expressed orphan G protein-coupled receptor that senses extracellular amino acids, osteocalcin, and divalent cations in vitro. GPRC6A null (GPRC6A(-/-)) mice exhibit multiple metabolic abnormalities including osteopenia. To investigate whether the osseous abnormalities are a direct function of GPRC6A in osteoblasts, we examined the function of primary ... Read more >>

J. Bone Miner. Res. (Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research)
[2010, 25(5):1092-1102]

Cited: 27 times

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3-Benzyl-1-methyl-imidazolium picrate.

Min Pi, Xiu-Ling Liu, Ji-Jun Xu, Chuan-Ming Jin,

In the title salt, C(11)H(13)N(2) (+)·C(6)H(2)N(3)O(7) (-), the dihedral angles between the benzene ring in the cation and the imidazolium ring and the benzene ring of the picrate anion are 113.7 (2) and 116.3 (2)°, respectively. The imidazolium ring is nearly parallel to the benzene ring of the picrate anion, the dihedral ... Read more >>

Acta Crystallogr Sect E Struct Rep Online (Acta crystallographica. Section E, Structure reports online)
[2009, 65(Pt 10):o2386]

Cited: 0 times

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GPRC6A null mice exhibit osteopenia, feminization and metabolic syndrome.

Min Pi, Ling Chen, Min-Zhao Huang, Wenyu Zhu, Brian Ringhofer, Junming Luo, Lane Christenson, Benyi Li, Jianghong Zhang, P David Jackson, Pieter Faber, Kurt R Brunden, John J Harrington, L Darryl Quarles,

GPRC6A is a widely expressed orphan G-protein coupled receptor that senses extracellular amino acids, osteocalcin and divalent cations in vitro. The physiological functions of GPRC6A are unknown.In this study, we created and characterized the phenotype of GPRC6A(-/-) mice. We observed complex metabolic abnormalities in GPRC6A(-/-) mice involving multiple organ systems ... Read more >>

PLoS ONE (PloS one)
[2008, 3(12):e3858]

Cited: 111 times

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Parathyroid-specific interaction of the calcium-sensing receptor and G alpha q.

Min Pi, Ling Chen, MinZhao Huang, Qiang Luo, L Darryl Quarles,

The calcium-sensing receptor regulates various parathyroid gland functions, including hormone secretion, gene transcription, and chief cell hyperplasia through G alpha q- and G alpha i-dependent signaling pathways. To determine the specific function of G alpha q in these processes, we generated transgenic mice using the human parathyroid hormone promoter to ... Read more >>

Kidney Int. (Kidney international)
[2008, 74(12):1548-1556]

Cited: 7 times

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