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Items: 1 to 20 of 94

1.

Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.

Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS.

ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11.

2.

An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.

Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN.

Sci Transl Med. 2012 Nov 7;4(159):159ra148. doi: 10.1126/scitranslmed.3004276.

3.

Analysis of responses to the TRPV4 agonist GSK1016790A in the pulmonary vascular bed of the intact-chest rat.

Pankey EA, Zsombok A, Lasker GF, Kadowitz PJ.

Am J Physiol Heart Circ Physiol. 2014 Jan 1;306(1):H33-40. doi: 10.1152/ajpheart.00303.2013. Epub 2013 Nov 1.

4.

Role of Transient Receptor Potential Vanilloid 4 in Neutrophil Activation and Acute Lung Injury.

Yin J, Michalick L, Tang C, Tabuchi A, Goldenberg N, Dan Q, Awwad K, Wang L, Erfinanda L, Nouailles G, Witzenrath M, Vogelzang A, Lv L, Lee WL, Zhang H, Rotstein O, Kapus A, Szaszi K, Fleming I, Liedtke WB, Kuppe H, Kuebler WM.

Am J Respir Cell Mol Biol. 2016 Mar;54(3):370-83. doi: 10.1165/rcmb.2014-0225OC.

PMID:
26222277
5.

Transient receptor potential vanilloid 4-mediated disruption of the alveolar septal barrier: a novel mechanism of acute lung injury.

Alvarez DF, King JA, Weber D, Addison E, Liedtke W, Townsley MI.

Circ Res. 2006 Oct 27;99(9):988-95. Epub 2006 Sep 28.

6.

Transient receptor potential vanilloid 4 activation constricts the human bronchus via the release of cysteinyl leukotrienes.

McAlexander MA, Luttmann MA, Hunsberger GE, Undem BJ.

J Pharmacol Exp Ther. 2014 Apr;349(1):118-25. doi: 10.1124/jpet.113.210203. Epub 2014 Feb 6.

7.

Emerging roles of calcium-activated K channels and TRPV4 channels in lung oedema and pulmonary circulatory collapse.

Simonsen U, Wandall-Frostholm C, Oliván-Viguera A, Köhler R.

Acta Physiol (Oxf). 2017 Jan;219(1):176-187. doi: 10.1111/apha.12768. Epub 2016 Sep 16. Review.

PMID:
27497091
8.

Activation of TRPV4 Regulates Respiration through Indirect Activation of Bronchopulmonary Sensory Neurons.

Gu QD, Moss CR 2nd, Kettelhut KL, Gilbert CA, Hu H.

Front Physiol. 2016 Feb 29;7:65. doi: 10.3389/fphys.2016.00065. eCollection 2016.

9.

Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2.

Willette RN, Bao W, Nerurkar S, Yue TL, Doe CP, Stankus G, Turner GH, Ju H, Thomas H, Fishman CE, Sulpizio A, Behm DJ, Hoffman S, Lin Z, Lozinskaya I, Casillas LN, Lin M, Trout RE, Votta BJ, Thorneloe K, Lashinger ES, Figueroa DJ, Marquis R, Xu X.

J Pharmacol Exp Ther. 2008 Aug;326(2):443-52. doi: 10.1124/jpet.107.134551. Epub 2008 May 22. Erratum in: J Pharmacol Exp Ther. 2011 Jul;338(1):408-9.

PMID:
18499744
10.

Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).

Brnardic EJ, Ye G, Brooks C, Donatelli C, Barton L, McAtee J, Sanchez RM, Shu A, Erhard K, Terrell L, Graczyk-Millbrandt G, He Y, Costell MH, Behm DJ, Roethke T, Stoy P, Holt DA, Lawhorn BG.

J Med Chem. 2018 Nov 8;61(21):9738-9755. doi: 10.1021/acs.jmedchem.8b01317. Epub 2018 Oct 18.

PMID:
30335378
11.

GSK2193874 treatment at heatstroke onset reduced cell apoptosis in heatstroke mice.

Zhu YH, Pei ZM.

Cell Mol Biol (Noisy-le-grand). 2018 May 30;64(7):36-42.

PMID:
29974844
12.

High vascular pressure-induced lung injury requires P450 epoxygenase-dependent activation of TRPV4.

Jian MY, King JA, Al-Mehdi AB, Liedtke W, Townsley MI.

Am J Respir Cell Mol Biol. 2008 Apr;38(4):386-92. Epub 2007 Oct 25.

13.

Differential modulation of transendothelial electrical resistance by TRPV4 agonists is mediated by apoptosis and/or necrosis.

Pairet N, Mang S, Kiechle T, Laufhäger N, Dietl P, Lamb DJ.

Biochem Biophys Rep. 2019 Sep 19;20:100672. doi: 10.1016/j.bbrep.2019.100672. eCollection 2019 Dec.

14.

Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema.

Hilfiker MA, Hoang TH, Cornil J, Eidam HS, Matasic DS, Roethke TJ, Klein M, Thorneloe KS, Cheung M.

ACS Med Chem Lett. 2013 Jan 27;4(2):293-6. doi: 10.1021/ml300449k. eCollection 2013 Feb 14.

15.

TRPV4 channel activation leads to endothelium-dependent relaxation mediated by nitric oxide and endothelium-derived hyperpolarizing factor in rat pulmonary artery.

Sukumaran SV, Singh TU, Parida S, Narasimha Reddy ChE, Thangamalai R, Kandasamy K, Singh V, Mishra SK.

Pharmacol Res. 2013 Dec;78:18-27. doi: 10.1016/j.phrs.2013.09.005. Epub 2013 Sep 25.

PMID:
24075884
16.

TRPV4 inhibition counteracts edema and inflammation and improves pulmonary function and oxygen saturation in chemically induced acute lung injury.

Balakrishna S, Song W, Achanta S, Doran SF, Liu B, Kaelberer MM, Yu Z, Sui A, Cheung M, Leishman E, Eidam HS, Ye G, Willette RN, Thorneloe KS, Bradshaw HB, Matalon S, Jordt SE.

Am J Physiol Lung Cell Mol Physiol. 2014 Jul 15;307(2):L158-72. doi: 10.1152/ajplung.00065.2014. Epub 2014 May 16.

17.

Functional transient receptor potential vanilloid 1 and transient receptor potential vanilloid 4 channels along different segments of the renal vasculature.

Chen L, Kaßmann M, Sendeski M, Tsvetkov D, Marko L, Michalick L, Riehle M, Liedtke WB, Kuebler WM, Harteneck C, Tepel M, Patzak A, Gollasch M.

Acta Physiol (Oxf). 2015 Feb;213(2):481-91. doi: 10.1111/apha.12355. Epub 2014 Aug 21.

PMID:
25069877
18.

Transient receptor potential vanilloid type 4-deficient mice exhibit impaired endothelium-dependent relaxation induced by acetylcholine in vitro and in vivo.

Zhang DX, Mendoza SA, Bubolz AH, Mizuno A, Ge ZD, Li R, Warltier DC, Suzuki M, Gutterman DD.

Hypertension. 2009 Mar;53(3):532-8. doi: 10.1161/HYPERTENSIONAHA.108.127100. Epub 2009 Feb 2.

19.

Opposing actions of TRPV4 channel activation in the lung vasculature.

Ke SK, Chen L, Duan HB, Tu YR.

Respir Physiol Neurobiol. 2015 Dec;219:43-50. doi: 10.1016/j.resp.2015.08.003. Epub 2015 Aug 14.

PMID:
26282788
20.

Modulation of the TRPV4 ion channel as a therapeutic target for disease.

Grace MS, Bonvini SJ, Belvisi MG, McIntyre P.

Pharmacol Ther. 2017 Sep;177:9-22. doi: 10.1016/j.pharmthera.2017.02.019. Epub 2017 Feb 12. Review.

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