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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
2003 2
2005 7
2006 7
2007 10
2008 10
2009 15
2010 15
2011 14
2012 18
2013 8
2014 18
2015 20
2016 14
2017 17
2018 20
2019 26
2020 22
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2023 21
2024 9

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270 results

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The niacin receptor HCAR2 modulates microglial response and limits disease progression in a mouse model of Alzheimer's disease.
Moutinho M, Puntambekar SS, Tsai AP, Coronel I, Lin PB, Casali BT, Martinez P, Oblak AL, Lasagna-Reeves CA, Lamb BT, Landreth GE. Moutinho M, et al. Sci Transl Med. 2022 Mar 23;14(637):eabl7634. doi: 10.1126/scitranslmed.abl7634. Epub 2022 Mar 23. Sci Transl Med. 2022. PMID: 35320002 Free PMC article.
Increased dietary intake of niacin has been correlated with reduced risk of Alzheimer's disease (AD). Niacin serves as a high-affinity ligand for the receptor HCAR2 (GPR109A). In the brain, HCAR2 is expressed selectively by microglia and is robustly induced by amylo …
Increased dietary intake of niacin has been correlated with reduced risk of Alzheimer's disease (AD). Niacin serves as a high-affinity ligan …
Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation.
Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z. Zhao C, et al. Mol Cell. 2023 Sep 7;83(17):3171-3187.e7. doi: 10.1016/j.molcel.2023.07.030. Epub 2023 Aug 18. Mol Cell. 2023. PMID: 37597514
HCAR2 mediates distinct pathophysiological events by activating G(i/o) protein or beta-arrestin effectors. Here, we characterize compound 9n as a G(i)-biased allosteric modulator (BAM) of HCAR2 and exhibit anti-inflammatory efficacy in RAW264.7 macrophages via a spe
HCAR2 mediates distinct pathophysiological events by activating G(i/o) protein or beta-arrestin effectors. Here, we characterize comp
Activation of HCAR2 by niacin: benefits beyond lipid lowering.
Tuteja S. Tuteja S. Pharmacogenomics. 2019 Nov;20(16):1143-1150. doi: 10.2217/pgs-2019-0092. Epub 2019 Oct 16. Pharmacogenomics. 2019. PMID: 31617441 Review.
Niacin (nicotinic acid) is a potent lipid-lowering agent that has been used for prevention of coronary heart disease. Niacin activates the HCAR2 receptor found on adipocytes, macrophages and various immune cells throughout the body. Activation of the HCAR2 receptor …
Niacin (nicotinic acid) is a potent lipid-lowering agent that has been used for prevention of coronary heart disease. Niacin activates the …
The Promise of Niacin in Neurology.
Wuerch E, Urgoiti GR, Yong VW. Wuerch E, et al. Neurotherapeutics. 2023 Jul;20(4):1037-1054. doi: 10.1007/s13311-023-01376-2. Epub 2023 Apr 21. Neurotherapeutics. 2023. PMID: 37084148 Free article. Review.
Niacin also has roles outside of metabolism, largely through engaging hydroxycarboxylic acid receptor 2 (Hcar2). These receptor-mediated activities of niacin include regulation of immune responses, phagocytosis of myelin debris after demyelination or of amyloid beta in mod …
Niacin also has roles outside of metabolism, largely through engaging hydroxycarboxylic acid receptor 2 (Hcar2). These receptor-media …
Ebola Virus Infection Induces HCAR2 Expression Leading to Cell Death.
Kuroda M, Halfmann PJ, Kawaoka Y. Kuroda M, et al. J Infect Dis. 2023 Nov 13;228(Suppl 7):S508-S513. doi: 10.1093/infdis/jiad344. J Infect Dis. 2023. PMID: 37578011
Phosphatidylserine externalization and cell membrane permeabilization by HCAR2 overexpression was also observed. Interestingly, coexpression of HCAR2 with EBOV VP40 further reduced cell viability in transfected cells compared to HCAR2 coexpression with other …
Phosphatidylserine externalization and cell membrane permeabilization by HCAR2 overexpression was also observed. Interestingly, coexp …
Potential role of the hydroxyl carboxylic acid receptor type 2 (HCAR2) in microglia pathophysiology: A possible cross-talk with C-X-C chemokine receptor 1 (CXCR1).
Perrone M, Pagano M, Belardo C, Ricciardi F, Ricciardi F, Fusco A, Trotta MC, Infantino R, Gargano F, Parente A, Giacca R, Pieretti G, Luongo L, Maione S, Boccella S, Guida F. Perrone M, et al. Neuropharmacology. 2023 May 1;228:109456. doi: 10.1016/j.neuropharm.2023.109456. Epub 2023 Feb 14. Neuropharmacology. 2023. PMID: 36796675 Free article. Review.
In a similar fashion, the treatment with MK 1903, a potent full agonist of HCAR2, increased the receptor protein levels. Moreover, HCAR2 stimulation prevented i) cells viability ii) morphological activation iii) pro/anti-inflammatory mediators production in LPS-trea …
In a similar fashion, the treatment with MK 1903, a potent full agonist of HCAR2, increased the receptor protein levels. Moreover, …
β-Hydroxybutyrate suppresses colorectal cancer.
Dmitrieva-Posocco O, Wong AC, Lundgren P, Golos AM, Descamps HC, Dohnalová L, Cramer Z, Tian Y, Yueh B, Eskiocak O, Egervari G, Lan Y, Liu J, Fan J, Kim J, Madhu B, Schneider KM, Khoziainova S, Andreeva N, Wang Q, Li N, Furth EE, Bailis W, Kelsen JR, Hamilton KE, Kaestner KH, Berger SL, Epstein JA, Jain R, Li M, Beyaz S, Lengner CJ, Katona BW, Grivennikov SI, Thaiss CA, Levy M. Dmitrieva-Posocco O, et al. Nature. 2022 May;605(7908):160-165. doi: 10.1038/s41586-022-04649-6. Epub 2022 Apr 27. Nature. 2022. PMID: 35477756 Free PMC article.
These properties of ketogenic diets are recapitulated by the ketone body beta-hydroxybutyrate (BHB), which reduces the proliferation of colonic crypt cells and potently suppresses intestinal tumour growth. We find that BHB acts through the surface receptor Hcar2 and induce …
These properties of ketogenic diets are recapitulated by the ketone body beta-hydroxybutyrate (BHB), which reduces the proliferation of colo …
Orthosteric ligand selectivity and allosteric probe dependence at Hydroxycarboxylic acid receptor HCAR2.
Cheng L, Sun S, Wang H, Zhao C, Tian X, Liu Y, Fu P, Shao Z, Chai R, Yan W. Cheng L, et al. Signal Transduct Target Ther. 2023 Sep 25;8(1):364. doi: 10.1038/s41392-023-01625-y. Signal Transduct Target Ther. 2023. PMID: 37743365 Free PMC article.
However, the mechanism underlying the signaling of HCAR2 induced by various types of ligands remains elusive. In this study, we elucidate the cryo-electron microscopy (cryo-EM) structure of G(i)-coupled HCAR2 in complex with a selective agonist, MK-6892, resolved to …
However, the mechanism underlying the signaling of HCAR2 induced by various types of ligands remains elusive. In this study, we eluci …
The ketone metabolite β-hydroxybutyrate blocks NLRP3 inflammasome-mediated inflammatory disease.
Youm YH, Nguyen KY, Grant RW, Goldberg EL, Bodogai M, Kim D, D'Agostino D, Planavsky N, Lupfer C, Kanneganti TD, Kang S, Horvath TL, Fahmy TM, Crawford PA, Biragyn A, Alnemri E, Dixit VD. Youm YH, et al. Nat Med. 2015 Mar;21(3):263-9. doi: 10.1038/nm.3804. Epub 2015 Feb 16. Nat Med. 2015. PMID: 25686106 Free PMC article.
BHB blocks the NLRP3 inflammasome without undergoing oxidation in the TCA cycle, and independently of uncoupling protein-2 (UCP2), sirtuin-2 (SIRT2), the G protein-coupled receptor GPR109A or hydrocaboxylic acid receptor 2 (HCAR2). BHB reduces NLRP3 inflammasome-mediated i …
BHB blocks the NLRP3 inflammasome without undergoing oxidation in the TCA cycle, and independently of uncoupling protein-2 (UCP2), sirtuin-2 …
270 results