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Items: 44


Differentiating the SGLT1 inhibition capacity of canagliflozin vs. dapagliflozin and empagliflozin using quantitative systems pharmacology modeling.

Sokolov V, Yakovleva T, Chu L, Tang W, Greasley PJ, Johansson S, Peskov K, Helmlinger G, Boulton DW, Penland RC.

CPT Pharmacometrics Syst Pharmacol. 2020 Feb 16. doi: 10.1002/psp4.12498. [Epub ahead of print]


Safety, Tolerability, and Pharmacokinetics of the Mineralocorticoid Receptor Modulator AZD9977 in Healthy Men: A Phase I Multiple Ascending Dose Study.

Whittaker A, Kragh ÅM, Hartleib-Geschwindner J, Albayaty M, Backlund A, Greasley PJ, Heijer M, Kjaer M, Forte P, Unwin R, Wernevik L, Ericsson H.

Clin Transl Sci. 2019 Oct 4. doi: 10.1111/cts.12705. [Epub ahead of print]


Comparison of the urinary glucose excretion contributions of SGLT2 and SGLT1: A quantitative systems pharmacology analysis in healthy individuals and patients with type 2 diabetes treated with SGLT2 inhibitors.

Yakovleva T, Sokolov V, Chu L, Tang W, Greasley PJ, Peilot Sjögren H, Johansson S, Peskov K, Helmlinger G, Boulton DW, Penland RC.

Diabetes Obes Metab. 2019 Dec;21(12):2684-2693. doi: 10.1111/dom.13858. Epub 2019 Sep 9.


Effects of the sodium-glucose co-transporter-2 inhibitor dapagliflozin on estimated plasma volume in patients with type 2 diabetes.

Dekkers CCJ, Sjöström CD, Greasley PJ, Cain V, Boulton DW, Heerspink HJL.

Diabetes Obes Metab. 2019 Dec;21(12):2667-2673. doi: 10.1111/dom.13855. Epub 2019 Sep 17.


Development of Human Target Validation Classification that Predicts Future Clinical Efficacy.

Karlsson C, Greasley PJ, Gustafsson D, Wåhlander K.

J Pharmacol Exp Ther. 2019 Feb;368(2):255-261. doi: 10.1124/jpet.118.250894. Epub 2018 Nov 27.


Inhibition of sodium/hydrogen exchanger 3 in the gastrointestinal tract by tenapanor reduces paracellular phosphate permeability.

King AJ, Siegel M, He Y, Nie B, Wang J, Koo-McCoy S, Minassian NA, Jafri Q, Pan D, Kohler J, Kumaraswamy P, Kozuka K, Lewis JG, Dragoli D, Rosenbaum DP, O'Neill D, Plain A, Greasley PJ, Jönsson-Rylander AC, Karlsson D, Behrendt M, Strömstedt M, Ryden-Bergsten T, Knöpfel T, Pastor Arroyo EM, Hernando N, Marks J, Donowitz M, Wagner CA, Alexander RT, Caldwell JS.

Sci Transl Med. 2018 Aug 29;10(456). pii: eaam6474. doi: 10.1126/scitranslmed.aam6474.


Evaluation of renal and cardiovascular protection mechanisms of SGLT2 inhibitors: model-based analysis of clinical data.

Hallow KM, Greasley PJ, Helmlinger G, Chu L, Heerspink HJ, Boulton DW.

Am J Physiol Renal Physiol. 2018 Nov 1;315(5):F1295-F1306. doi: 10.1152/ajprenal.00202.2018. Epub 2018 Jul 18.


Contemporary rates and predictors of fast progression of chronic kidney disease in adults with and without diabetes mellitus.

Go AS, Yang J, Tan TC, Cabrera CS, Stefansson BV, Greasley PJ, Ordonez JD; Kaiser Permanente Northern California CKD Outcomes Study.

BMC Nephrol. 2018 Jun 22;19(1):146. doi: 10.1186/s12882-018-0942-1.


The effects of tenapanor on serum fibroblast growth factor 23 in patients receiving hemodialysis with hyperphosphatemia.

Block GA, Rosenbaum DP, Yan A, Greasley PJ, Chertow GM, Wolf M.

Nephrol Dial Transplant. 2019 Feb 1;34(2):339-346. doi: 10.1093/ndt/gfy061.


Why do SGLT2 inhibitors reduce heart failure hospitalization? A differential volume regulation hypothesis.

Hallow KM, Helmlinger G, Greasley PJ, McMurray JJV, Boulton DW.

Diabetes Obes Metab. 2018 Mar;20(3):479-487. doi: 10.1111/dom.13126. Epub 2017 Nov 15.


A common NHE3 single-nucleotide polymorphism has normal function and sensitivity to regulatory ligands.

Yin J, Tse CM, Cha B, Sarker R, Zhu XC, Walentinsson A, Greasley PJ, Donowitz M.

Am J Physiol Gastrointest Liver Physiol. 2017 Aug 1;313(2):G129-G137. doi: 10.1152/ajpgi.00044.2017. Epub 2017 May 11.


Differential Effects of Dapagliflozin on Cardiovascular Risk Factors at Varying Degrees of Renal Function.

Petrykiv S, Sjöström CD, Greasley PJ, Xu J, Persson F, Heerspink HJL.

Clin J Am Soc Nephrol. 2017 May 8;12(5):751-759. doi: 10.2215/CJN.10180916. Epub 2017 Mar 16.


Deletion of Gpr55 Results in Subtle Effects on Energy Metabolism, Motor Activity and Thermal Pain Sensation.

Bjursell M, Ryberg E, Wu T, Greasley PJ, Bohlooly-Y M, Hjorth S.

PLoS One. 2016 Dec 12;11(12):e0167965. doi: 10.1371/journal.pone.0167965. eCollection 2016.


Effect of Tenapanor on Interdialytic Weight Gain in Patients on Hemodialysis.

Block GA, Rosenbaum DP, Leonsson-Zachrisson M, Stefansson BV, Rydén-Bergsten T, Greasley PJ, Johansson SA, Knutsson M, Carlsson BC.

Clin J Am Soc Nephrol. 2016 Sep 7;11(9):1597-605. doi: 10.2215/CJN.09050815. Epub 2016 Jun 23.


Insulin resistance, endothelial function, angiogenic factors and clinical outcome in non-diabetic patients with chest pain without myocardial perfusion defects.

Westergren HU, Svedlund S, Momo RA, Blomster JI, Wåhlander K, Rehnström E, Greasley PJ, Fritsche-Danielson R, Oscarsson J, Gan LM.

Cardiovasc Diabetol. 2016 Feb 19;15:36. doi: 10.1186/s12933-016-0353-1.


Pharmacological profiling of the hemodynamic effects of cannabinoid ligands: a combined in vitro and in vivo approach.

Walsh SK, Hepburn CY, Keown O, Åstrand A, Lindblom A, Ryberg E, Hjorth S, Leslie SJ, Greasley PJ, Wainwright CL.

Pharmacol Res Perspect. 2015 Jun;3(3):e00143. doi: 10.1002/prp2.143. Epub 2015 May 8.


Pharmacologic inhibition of intestinal sodium uptake: a gut centric approach to sodium management.

Spencer AG, Greasley PJ.

Curr Opin Nephrol Hypertens. 2015 Sep;24(5):410-6. doi: 10.1097/MNH.0000000000000154. Review.


Succinate receptor GPR91, a Gα(i) coupled receptor that increases intracellular calcium concentrations through PLCβ.

Sundström L, Greasley PJ, Engberg S, Wallander M, Ryberg E.

FEBS Lett. 2013 Aug 2;587(15):2399-404. doi: 10.1016/j.febslet.2013.05.067. Epub 2013 Jun 13.


Big pharma screening collections: more of the same or unique libraries? The AstraZeneca-Bayer Pharma AG case.

Kogej T, Blomberg N, Greasley PJ, Mundt S, Vainio MJ, Schamberger J, Schmidt G, Hüser J.

Drug Discov Today. 2013 Oct;18(19-20):1014-24. doi: 10.1016/j.drudis.2012.10.011. Epub 2012 Nov 3. Review.


N-arachidonoyl-L-serine is neuroprotective after traumatic brain injury by reducing apoptosis.

Cohen-Yeshurun A, Trembovler V, Alexandrovich A, Ryberg E, Greasley PJ, Mechoulam R, Shohami E, Leker RR.

J Cereb Blood Flow Metab. 2011 Aug;31(8):1768-77. doi: 10.1038/jcbfm.2011.53. Epub 2011 Apr 20.


International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB₁ and CB₂.

Pertwee RG, Howlett AC, Abood ME, Alexander SP, Di Marzo V, Elphick MR, Greasley PJ, Hansen HS, Kunos G, Mackie K, Mechoulam R, Ross RA.

Pharmacol Rev. 2010 Dec;62(4):588-631. doi: 10.1124/pr.110.003004. Review.


Novel thioamide derivatives as neutral CB1 receptor antagonists.

Boström J, Olsson RI, Tholander J, Greasley PJ, Ryberg E, Nordberg H, Hjorth S, Cheng L.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):479-82. doi: 10.1016/j.bmcl.2009.11.125. Epub 2009 Nov 27.


The putative cannabinoid receptor GPR55 affects osteoclast function in vitro and bone mass in vivo.

Whyte LS, Ryberg E, Sims NA, Ridge SA, Mackie K, Greasley PJ, Ross RA, Rogers MJ.

Proc Natl Acad Sci U S A. 2009 Sep 22;106(38):16511-6. doi: 10.1073/pnas.0902743106. Epub 2009 Sep 3.


Ticagrelor binds to human P2Y(12) independently from ADP but antagonizes ADP-induced receptor signaling and platelet aggregation.

VAN Giezen JJ, Nilsson L, Berntsson P, Wissing BM, Giordanetto F, Tomlinson W, Greasley PJ.

J Thromb Haemost. 2009 Sep;7(9):1556-65. doi: 10.1111/j.1538-7836.2009.03527.x. Epub 2009 Jun 23.


High-quality cost-effective compound management support for HTS.

Zaragoza-Sundqvist M, Eriksson H, Rohman M, Greasley PJ.

J Biomol Screen. 2009 Jun;14(5):509-14. doi: 10.1177/1087057109336589. Epub 2009 Jun 1.


The orphan receptor GPR55 is a novel cannabinoid receptor.

Ryberg E, Larsson N, Sjögren S, Hjorth S, Hermansson NO, Leonova J, Elebring T, Nilsson K, Drmota T, Greasley PJ.

Br J Pharmacol. 2007 Dec;152(7):1092-101. Epub 2007 Sep 17.


Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.

Boström J, Berggren K, Elebring T, Greasley PJ, Wilstermann M.

Bioorg Med Chem. 2007 Jun 15;15(12):4077-84. Epub 2007 Mar 30.


Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge worth pursuing?

Greasley PJ, Clapham JC.

Eur J Pharmacol. 2006 Dec 28;553(1-3):1-9. Epub 2006 Sep 26. Review.


G-protein-coupled receptor screening technologies.

Greasley PJ, Jansen FP.

Drug Discov Today Technol. 2005 Summer;2(2):163-70. doi: 10.1016/j.ddtec.2005.05.009.


Identification and characterisation of a novel splice variant of the human CB1 receptor.

Ryberg E, Vu HK, Larsson N, Groblewski T, Hjorth S, Elebring T, Sjögren S, Greasley PJ.

FEBS Lett. 2005 Jan 3;579(1):259-64.


Mutagenesis and modelling of the alpha(1b)-adrenergic receptor highlight the role of the helix 3/helix 6 interface in receptor activation.

Greasley PJ, Fanelli F, Rossier O, Abuin L, Cotecchia S.

Mol Pharmacol. 2002 May;61(5):1025-32.


Co- and posttranslational modification of the alpha(1B)-adrenergic receptor: effects on receptor expression and function.

Björklöf K, Lundström K, Abuin L, Greasley PJ, Cotecchia S.

Biochemistry. 2002 Apr 2;41(13):4281-91.


Mutational and computational analysis of the alpha(1b)-adrenergic receptor. Involvement of basic and hydrophobic residues in receptor activation and G protein coupling.

Greasley PJ, Fanelli F, Scheer A, Abuin L, Nenniger-Tosato M, DeBenedetti PG, Cotecchia S.

J Biol Chem. 2001 Dec 7;276(49):46485-94. Epub 2001 Oct 3.


Myc induces the nucleolin and BN51 genes: possible implications in ribosome biogenesis.

Greasley PJ, Bonnard C, Amati B.

Nucleic Acids Res. 2000 Jan 15;28(2):446-53.


Bovine inositol monophosphatase: metal-binding interactions at two different sites.

Thorne MR, Rees-Milton KJ, Greasley PJ, Gore MG.

Biochem Soc Trans. 1997 Feb;25(1):39S. No abstract available.


Bovine inositol monophosphatase. Ligand binding to pyrene-maleimide-labelled enzyme.

Greasley PJ, Hunt LG, Gore MG.

Eur J Biochem. 1994 Jun 1;222(2):453-60.


Bovine inositol monophosphatase. The identification of a histidine residue reactive to diethylpyrocarbonate.

Rees-Milton KJ, Greasley PJ, Ragan CI, Gore MG.

FEBS Lett. 1993 Apr 19;321(1):37-40.


Bovine inositol monophosphatase: proteolysis and structural studies.

Greasley PJ, Gore MG, Rees-Milton KJ, Ragan CI.

FEBS Lett. 1993 Mar 15;319(1-2):49-53.


Bovine inositol monophosphatase: development of a continuous fluorescence assay of enzyme activity.

Gore MG, Greasley PJ, Ragan CI.

J Biochem Biophys Methods. 1992 Aug;25(1):55-60.


Bovine inositol monophosphatase; observation of the modification of a cysteine residue using protein fluorescence.

Greasley PJ, Gore MG, Ragan CI, Knowles MR, Gee NS, McAllister G.

Biochem Soc Trans. 1992 Aug;20(3):290S. No abstract available.


Bovine inositol monophosphatase. Modification, identification and mutagenesis of reactive cysteine residues.

Knowles MR, Gee N, McAllister G, Ragan CI, Greasley PJ, Gore MG.

Biochem J. 1992 Jul 15;285 ( Pt 2):461-8.

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