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Items: 1 to 50 of 99

1.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

2.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

3.

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance.

O'Neill PM, Amewu RK, Charman SA, Sabbani S, Gnädig NF, Straimer J, Fidock DA, Shore ER, Roberts NL, Wong MH, Hong WD, Pidathala C, Riley C, Murphy B, Aljayyoussi G, Gamo FJ, Sanz L, Rodrigues J, Cortes CG, Herreros E, Angulo-Barturén I, Jiménez-Díaz MB, Bazaga SF, Martínez-Martínez MS, Campo B, Sharma R, Ryan E, Shackleford DM, Campbell S, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Palmer MJ, Copple IM, Mercer AE, Ruecker A, Delves MJ, Sinden RE, Siegl P, Davies J, Rochford R, Kocken CHM, Zeeman AM, Nixon GL, Biagini GA, Ward SA.

Nat Commun. 2017 May 24;8:15159. doi: 10.1038/ncomms15159.

4.

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Martínez MS, Bolscher JM, Woodland A, Luksch T, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2016 Sep 1;537(7618):122. doi: 10.1038/nature18280. Epub 2016 May 25. No abstract available.

5.

A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Erratum in: Nature. 2016 Sep 1;537(7618):122.

6.

Evaluation of the QT effect of a combination of piperaquine and a novel anti-malarial drug candidate OZ439, for the treatment of uncomplicated malaria.

Darpo B, Ferber G, Siegl P, Laurijssens B, Macintyre F, Toovey S, Duparc S.

Br J Clin Pharmacol. 2015 Oct;80(4):706-15. doi: 10.1111/bcp.12680. Epub 2015 Jul 14.

7.

Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum.

Vaidya AB, Morrisey JM, Zhang Z, Das S, Daly TM, Otto TD, Spillman NJ, Wyvratt M, Siegl P, Marfurt J, Wirjanata G, Sebayang BF, Price RN, Chatterjee A, Nagle A, Stasiak M, Charman SA, Angulo-Barturen I, Ferrer S, Belén Jiménez-Díaz M, Martínez MS, Gamo FJ, Avery VM, Ruecker A, Delves M, Kirk K, Berriman M, Kortagere S, Burrows J, Fan E, Bergman LW.

Nat Commun. 2014 Nov 25;5:5521. doi: 10.1038/ncomms6521.

8.

Quinolone-3-diarylethers: a new class of antimalarial drug.

Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE, Morrisey JM, Steuten J, Mutka T, Li Y, Wirjanata G, Ryan E, Duffy S, Kelly JX, Sebayang BF, Zeeman AM, Noviyanti R, Sinden RE, Kocken CHM, Price RN, Avery VM, Angulo-Barturen I, Jiménez-Díaz MB, Ferrer S, Herreros E, Sanz LM, Gamo FJ, Bathurst I, Burrows JN, Siegl P, Guy RK, Winter RW, Vaidya AB, Charman SA, Kyle DE, Manetsch R, Riscoe MK.

Sci Transl Med. 2013 Mar 20;5(177):177ra37. doi: 10.1126/scitranslmed.3005029.

9.

Drug attrition during pre-clinical and clinical development: understanding and managing drug-induced cardiotoxicity.

Ferri N, Siegl P, Corsini A, Herrmann J, Lerman A, Benghozi R.

Pharmacol Ther. 2013 Jun;138(3):470-84. doi: 10.1016/j.pharmthera.2013.03.005. Epub 2013 Mar 15. Review.

PMID:
23507039
10.

Safety pharmacology in 2010 and beyond: survey of significant events of the past 10 years and a roadmap to the immediate-, intermediate- and long-term future in recognition of the tenth anniversary of the Safety Pharmacology Society.

Bass AS, Vargas HM, Valentin JP, Kinter LB, Hammond T, Wallis R, Siegl PK, Yamamoto K.

J Pharmacol Toxicol Methods. 2011 Jul-Aug;64(1):7-15. doi: 10.1016/j.vascn.2011.05.006. Epub 2011 Jun 12. Review.

PMID:
21689769
11.

Comparison of electrocardiographic analysis for risk of QT interval prolongation using safety pharmacology and toxicological studies.

Guth BD, Bass AS, Briscoe R, Chivers S, Markert M, Siegl PK, Valentin JP.

J Pharmacol Toxicol Methods. 2009 Sep-Oct;60(2):107-16. doi: 10.1016/j.vascn.2009.05.006. Epub 2009 May 24. Review.

PMID:
19470407
12.

Complement dependent cytotoxicity (CDC) activity of a humanized anti Lewis-Y antibody: FACS-based assay versus the 'classical' radioactive method -- qualification, comparison and application of the FACS-based approach.

Nechansky A, Szolar OH, Siegl P, Zinoecker I, Halanek N, Wiederkum S, Kircheis R.

J Pharm Biomed Anal. 2009 May 1;49(4):1014-20. doi: 10.1016/j.jpba.2009.01.029. Epub 2009 Feb 4.

PMID:
19250790
13.

Torcetrapib-induced blood pressure elevation is independent of CETP inhibition and is accompanied by increased circulating levels of aldosterone.

Forrest MJ, Bloomfield D, Briscoe RJ, Brown PN, Cumiskey AM, Ehrhart J, Hershey JC, Keller WJ, Ma X, McPherson HE, Messina E, Peterson LB, Sharif-Rodriguez W, Siegl PK, Sinclair PJ, Sparrow CP, Stevenson AS, Sun SY, Tsai C, Vargas H, Walker M 3rd, West SH, White V, Woltmann RF.

Br J Pharmacol. 2008 Aug;154(7):1465-73. doi: 10.1038/bjp.2008.229. Epub 2008 Jun 9.

14.

Compensation of endogenous IgG mediated inhibition of antibody-dependent cellular cytotoxicity by glyco-engineering of therapeutic antibodies.

Nechansky A, Schuster M, Jost W, Siegl P, Wiederkum S, Gorr G, Kircheis R.

Mol Immunol. 2007 Mar;44(7):1815-7. Epub 2006 Oct 2.

PMID:
17011625
15.

Immunization of Rhesus monkeys with a SialylTn-mAb17-1A conjugate vaccine co-formulated with QS-21 induces a temporary systemic cytokine release and NK cytotoxicity against tumor cells.

Kircheis R, Siegl P, Grunt S, Halanek N, Loibner H, Mudde GC, Nechansky A.

Cancer Immunol Immunother. 2007 Jun;56(6):863-73. Epub 2006 Sep 29.

PMID:
17009044
16.

New preclinical guidelines on drug effects on ventricular repolarization: safety pharmacology comes of age.

Kinter LB, Siegl PK, Bass AS.

J Pharmacol Toxicol Methods. 2004 May-Jun;49(3):153-8. Review. No abstract available.

PMID:
15172011
17.

Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.

Friesen RW, Ducharme Y, Ball RG, Blouin M, Boulet L, Côté B, Frenette R, Girard M, Guay D, Huang Z, Jones TR, Laliberté F, Lynch JJ, Mancini J, Martins E, Masson P, Muise E, Pon DJ, Siegl PK, Styhler A, Tsou NN, Turner MJ, Young RN, Girard Y.

J Med Chem. 2003 Jun 5;46(12):2413-26.

PMID:
12773045
18.

Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development.

Redfern WS, Carlsson L, Davis AS, Lynch WG, MacKenzie I, Palethorpe S, Siegl PK, Strang I, Sullivan AT, Wallis R, Camm AJ, Hammond TG.

Cardiovasc Res. 2003 Apr 1;58(1):32-45. Review.

PMID:
12667944
19.

Methods for assessing endothelin ETA-receptor antagonists in preclinical studies.

Okada M, Siegl PK, Nishikibe M.

Methods Find Exp Clin Pharmacol. 2002 Jul-Aug;24(6):361-70. Review.

PMID:
12224443
20.

Antihypertensive effects of a mixed endothelin-A- and -B-receptor antagonist, J-104132, were augmented in the presence of an AT1 -receptor antagonist, MK-954.

Ikeda T, Ohta H, Okada M, Kawai N, Nakao R, Siegl PK, Kobayashi T, Miyauchi T, Nishikibe M.

J Cardiovasc Pharmacol. 2000 Nov;36(5 Suppl 1):S337-41.

PMID:
11078414
21.

[Changes in psychophysiologic status during inpatient rehabilitation in the orthopedics service--a preliminary study].

Siegl P, Franke A, Häusler H, Kühne JH.

Rehabilitation (Stuttg). 1999 Nov;38(4):249-53. German.

PMID:
10627971
22.

Pathophysiological roles of endothelin-1 in Dahl salt-sensitive hypertension.

Ikeda T, Ohta H, Okada M, Kawai N, Nakao R, Siegl PK, Kobayashi T, Maeda S, Miyauchi T, Nishikibe M.

Hypertension. 1999 Sep;34(3):514-9.

PMID:
10489403
23.

Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.

Nishikibe M, Ohta H, Okada M, Ishikawa K, Hayama T, Fukuroda T, Noguchi K, Saito M, Kanoh T, Ozaki S, Kamei T, Hara K, William D, Kivlighn S, Krause S, Gabel R, Zingaro G, Nolan N, O'Brien J, Clayton F, Lynch J, Pettibone D, Siegl P.

J Pharmacol Exp Ther. 1999 Jun;289(3):1262-70.

PMID:
10336515
24.

Lack of beneficial effects of growth hormone treatment in conscious dogs during development of heart failure.

Shen YT, Woltmann RF, Appleby S, Prahalada S, Krause SM, Kivilghn SD, Johnson RG, Siegl PK, Lynch JJ.

Am J Physiol. 1998 Feb;274(2):H456-66. doi: 10.1152/ajpheart.1998.274.2.H456.

PMID:
9486248
25.

Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.

Selnick HG, Liverton NJ, Baldwin JJ, Butcher JW, Claremon DA, Elliott JM, Freidinger RM, King SA, Libby BE, McIntyre CJ, Pribush DA, Remy DC, Smith GR, Tebben AJ, Jurkiewicz NK, Lynch JJ, Salata JJ, Sanguinetti MC, Siegl PK, Slaughter DE, Vyas K.

J Med Chem. 1997 Nov 21;40(24):3865-8. No abstract available.

PMID:
9397166
26.

Endothelin-B receptors in cerebral resistance arterioles and their functional significance after focal cerebral ischemia in cats.

Touzani O, Galbraith S, Siegl P, McCulloch J.

J Cereb Blood Flow Metab. 1997 Nov;17(11):1157-65.

PMID:
9390647
27.

In vivo pharmacology of an angiotensin AT1 receptor antagonist with balanced affinity for AT2 receptors.

Kivlighn SD, Zingaro GJ, Gabel RA, Broten TP, Chang RS, Ondeyka DL, Mantlo NB, Gibson RE, Greenlee WJ, Siegl PK.

Eur J Pharmacol. 1995 Dec 29;294(2-3):439-50.

PMID:
8750704
28.

In vitro pharmacology of an angiotensin AT1 receptor antagonist with balanced affinity for AT2 receptors.

Chang RS, Lotti VJ, Chen TB, O'Malley SS, Bendesky RJ, Kling PJ, Kivlighn SD, Siegl PK, Ondeyka D, Greenlee WJ, et al.

Eur J Pharmacol. 1995 Dec 29;294(2-3):429-37.

PMID:
8750703
29.

Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes.

Chang LL, Ashton WT, Flanagan KL, Chen TB, O'Malley SS, Zingaro GJ, Kivlighn SD, Siegl PK, Lotti VJ, Chang RS, et al.

J Med Chem. 1995 Sep 15;38(19):3741-58.

PMID:
7562905
30.

In vivo pharmacology of L-159,913, a new highly potent and selective nonpeptide angiotensin II receptor antagonist.

Gabel RA, Kivlighn SD, Zingaro GJ, Schorn TW, Schaffer LW, Ashton WT, Chang LL, Flanagan K, Greenlee WJ, Siegl PK.

Clin Exp Hypertens. 1995 Aug;17(6):931-53.

PMID:
7581262
31.

Pharmacology of losartan, an angiotensin II receptor antagonist, in animal models of hypertension.

Siegl PK, Kivlighn SD, Broten TP.

J Hypertens Suppl. 1995 Jul;13(1):S15-21.

PMID:
18800451
32.
33.

Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes.

Chang LL, Ashton WT, Flanagan KL, Chen TB, O'Malley SS, Zingaro GJ, Siegl PK, Kivlighn SD, Lotti VJ, Chang RS, et al.

J Med Chem. 1994 Dec 23;37(26):4464-78.

PMID:
7799397
34.

Juxtaglomerular cell hypertrophy and hyperplasia induced in rhesus monkeys by angiotensin II receptor antagonists.

Owen RA, Molon-Noblot S, Hubert MF, Siegl PK, Eydelloth RS, Keenan KP.

Lab Invest. 1994 Oct;71(4):543-51.

PMID:
7967510
35.

Effects of BQ-123 on renal function and acute cyclosporine-induced renal dysfunction.

Kivlighn SD, Gabel RA, Siegl PK.

Kidney Int. 1994 Jan;45(1):131-6.

36.

Blockers of ATP sensitive potassium current are of potential benefit in ischaemic heart disease.

Siegl P.

Cardiovasc Res. 1994 Jan;28(1):31-2. No abstract available.

PMID:
8111789
37.

Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.

Dhanoa DS, Bagley SW, Chang RS, Lotti VJ, Chen TB, Kivlighn SD, Zingaro GJ, Siegl PK, Patchett AA, Greenlee WJ.

J Med Chem. 1993 Dec 24;36(26):4239-49. Erratum in: J Med Chem 1994 Apr 1;37(7):1034.

PMID:
8277506
38.

Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.

Dhanoa DS, Bagley SW, Chang RS, Lotti VJ, Chen TB, Kivlighn SD, Zingaro GJ, Siegl PK, Patchett AA, Greenlee WJ.

J Med Chem. 1993 Dec 24;36(26):4230-8.

PMID:
8277505
39.

(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.

Dhanoa DS, Bagley SW, Chang RS, Lotti VJ, Chen TB, Kivlighn SD, Zingaro GJ, Siegl PK, Chakravarty PK, Patchett AA, et al.

J Med Chem. 1993 Nov 12;36(23):3738-42. No abstract available.

PMID:
8246245
40.

Recombinant leech antiplatelet protein prevents collagen-mediated platelet aggregation but not collagen graft thrombosis in baboons.

Schaffer LW, Davidson JT, Siegl PK, Gould RJ, Nutt RF, Brady SF, Connolly TM.

Arterioscler Thromb. 1993 Nov;13(11):1593-601.

PMID:
8218100
41.

Antithrombotic activity of recombinant tick anticoagulant peptide and heparin in a rabbit model of venous thrombosis.

Fioravanti C, Burkholder D, Francis B, Siegl PK, Gibson RE.

Thromb Res. 1993 Aug 15;71(4):317-24.

PMID:
8236160
42.

Failure of intravenous pentagastrin challenge to induce panic-like effects in rhesus monkeys.

Rupniak NM, Schaffer L, Siegl P, Iversen SD.

Neuropeptides. 1993 Aug;25(2):115-9.

PMID:
8413856
43.

Discovery of losartan, the first specific non-peptide angiotensin II receptor antagonist.

Siegl PK.

J Hypertens Suppl. 1993 Apr;11(3):S19-22. Review.

PMID:
8315513
44.

A rapid bioassay for the determination of non-nucleoside HIV-1 reverse transcriptase inhibitor plasma levels.

O'Brien JA, Ostovic D, Schorn TW, Smith SJ, Ruffing TL, Siegl PK, Goldman ME.

Life Sci. 1993;52(3):243-9.

PMID:
7678687
45.

Selective factor Xa inhibition by recombinant antistasin prevents vascular graft thrombosis in baboons.

Schaffer LW, Davidson JT, Vlasuk GP, Dunwiddie CT, Siegl PK.

Arterioscler Thromb. 1992 Aug;12(8):879-85.

PMID:
1637785
46.

Inhibitors of human renin with C-termini derived from amides and esters of alpha-mercaptoalkanoic acids.

Ashton WT, Cantone CL, Tolman RL, Greenlee WJ, Lynch RJ, Schorn TW, Strouse JF, Siegl PK.

J Med Chem. 1992 Jul 24;35(15):2772-81.

PMID:
1495010
47.

In vivo pharmacology of L-158,809, a new highly potent and selective nonpeptide angiotensin II receptor antagonist.

Siegl PK, Chang RS, Mantlo NB, Chakravarty PK, Ondeyka DL, Greenlee WJ, Patchett AA, Sweet CS, Lotti VJ.

J Pharmacol Exp Ther. 1992 Jul;262(1):139-44.

PMID:
1625193
48.

In vitro pharmacology of L-158,809, a new highly potent and selective angiotensin II receptor antagonist.

Chang RS, Siegl PK, Clineschmidt BV, Mantlo NB, Chakravarty PK, Greenlee WJ, Patchett AA, Lotti VJ.

J Pharmacol Exp Ther. 1992 Jul;262(1):133-8.

PMID:
1625192
49.

Cardiac angiotensin receptors: effects of selective angiotensin II receptor antagonists, DUP 753 and PD 121981, in rabbit heart.

Scott AL, Chang RS, Lotti VJ, Siegl PK.

J Pharmacol Exp Ther. 1992 Jun;261(3):931-5.

PMID:
1602398
50.

Renin inhibitors containing C-termini derived from mercaptoheterocycles.

Ashton WT, Cantone CL, Meurer LC, Tolman RL, Greenlee WJ, Patchett AA, Lynch RJ, Schorn TW, Strouse JF, Siegl PK.

J Med Chem. 1992 May 29;35(11):2103-12.

PMID:
1597860

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