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Items: 1 to 50 of 109

1.

The Hippo pathway effector TAZ induces TEAD-dependent liver inflammation and tumors.

Hagenbeek TJ, Webster JD, Kljavin NM, Chang MT, Pham T, Lee HJ, Klijn C, Cai AG, Totpal K, Ravishankar B, Yang N, Lee DH, Walsh KB, Hatzivassiliou G, de la Cruz CC, Gould SE, Wu X, Lee WP, Yang S, Zhang Z, Gu Q, Ji Q, Jackson EL, Lim DS, Dey A.

Sci Signal. 2018 Sep 11;11(547). pii: eaaj1757. doi: 10.1126/scisignal.aaj1757.

PMID:
30206136
2.

Translational pharmacokinetic/pharmacodynamic analysis in cancer pharmacology: a tool to maximize the value of antitumor efficacy from tumor bearing mice.

Wong H, Gould SE.

Drug Discov Today Technol. 2016 Sep - Dec;21-22:51-56. doi: 10.1016/j.ddtec.2016.08.003. Epub 2016 Oct 21. Review.

PMID:
27978988
3.

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma.

Salphati L, Alicke B, Heffron TP, Shahidi-Latham S, Nishimura M, Cao T, Carano RA, Cheong J, Greve J, Koeppen H, Lau S, Lee LB, Nannini-Pepe M, Pang J, Plise EG, Quiason C, Rangell L, Zhang X, Gould SE, Phillips HS, Olivero AG.

Drug Metab Dispos. 2016 Dec;44(12):1881-1889. Epub 2016 Sep 16.

4.

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.

Blake JF, Burkard M, Chan J, Chen H, Chou KJ, Diaz D, Dudley DA, Gaudino JJ, Gould SE, Grina J, Hunsaker T, Liu L, Martinson M, Moreno D, Mueller L, Orr C, Pacheco P, Qin A, Rasor K, Ren L, Robarge K, Shahidi-Latham S, Stults J, Sullivan F, Wang W, Yin J, Zhou A, Belvin M, Merchant M, Moffat J, Schwarz JB.

J Med Chem. 2016 Jun 23;59(12):5650-60. doi: 10.1021/acs.jmedchem.6b00389. Epub 2016 Jun 7.

PMID:
27227380
5.

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD, Lewis C, Nonomiya J, Pang J, Plise EG, Sideris S, Wallin J, Wang L, Zhang X, Olivero AG.

ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. doi: 10.1021/acsmedchemlett.6b00005. eCollection 2016 Apr 14.

6.

MAP Kinase Inhibition Promotes T Cell and Anti-tumor Activity in Combination with PD-L1 Checkpoint Blockade.

Ebert PJR, Cheung J, Yang Y, McNamara E, Hong R, Moskalenko M, Gould SE, Maecker H, Irving BA, Kim JM, Belvin M, Mellman I.

Immunity. 2016 Mar 15;44(3):609-621. doi: 10.1016/j.immuni.2016.01.024. Epub 2016 Mar 2.

7.

Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.

Ndubaku CO, Crawford TD, Chen H, Boggs JW, Drobnick J, Harris SF, Jesudason R, McNamara E, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Vitorino P, Wang L, Wu P, Yeung S, Chen J, Chen K, Ding CZ, Wang T, Xu Z, Gould SE, Murray LJ, Ye W.

ACS Med Chem Lett. 2015 Jun 29;6(8):913-8. doi: 10.1021/acsmedchemlett.5b00174. eCollection 2015 Aug 13.

8.

Translational value of mouse models in oncology drug development.

Gould SE, Junttila MR, de Sauvage FJ.

Nat Med. 2015 May;21(5):431-9. doi: 10.1038/nm.3853.

PMID:
25951530
9.

Prediction of drug distribution in subcutaneous xenografts of human tumor cell lines and healthy tissues in mouse: application of the tissue composition-based model to antineoplastic drugs.

Poulin P, Chen YH, Ding X, Gould SE, Hop CE, Messick K, Oeh J, Liederer BM.

J Pharm Sci. 2015 Apr;104(4):1508-21. doi: 10.1002/jps.24336. Epub 2015 Jan 14.

PMID:
25615572
10.

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.

Ren L, Grina J, Moreno D, Blake JF, Gaudino JJ, Garrey R, Metcalf AT, Burkard M, Martinson M, Rasor K, Chen H, Dean B, Gould SE, Pacheco P, Shahidi-Latham S, Yin J, West K, Wang W, Moffat JG, Schwarz JB.

J Med Chem. 2015 Feb 26;58(4):1976-91. doi: 10.1021/jm501921k. Epub 2015 Feb 11.

PMID:
25603482
11.

Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.

Wang L, Stanley M, Boggs JW, Crawford TD, Bravo BJ, Giannetti AM, Harris SF, Magnuson SR, Nonomiya J, Schmidt S, Wu P, Ye W, Gould SE, Murray LJ, Ndubaku CO, Chen H.

Bioorg Med Chem Lett. 2014 Sep 15;24(18):4546-4552. doi: 10.1016/j.bmcl.2014.07.071. Epub 2014 Aug 2.

PMID:
25139565
12.

Discovery and preclinical development of vismodegib.

Gould SE, Low JA, Marsters JC Jr, Robarge K, Rubin LL, de Sauvage FJ, Sutherlin DP, Wong H, Yauch RL.

Expert Opin Drug Discov. 2014 Aug;9(8):969-84. doi: 10.1517/17460441.2014.920816. Epub 2014 May 23. Review.

PMID:
24857041
13.

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.

Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB.

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068. Epub 2014 Apr 29.

PMID:
24813737
14.

Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.

Crawford TD, Ndubaku CO, Chen H, Boggs JW, Bravo BJ, Delatorre K, Giannetti AM, Gould SE, Harris SF, Magnuson SR, McNamara E, Murray LJ, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Stanley M, Vitorino P, Wang L, West K, Wu P, Ye W.

J Med Chem. 2014 Apr 24;57(8):3484-93. doi: 10.1021/jm500155b. Epub 2014 Apr 9.

PMID:
24673130
15.

PTEN loss mitigates the response of medulloblastoma to Hedgehog pathway inhibition.

Metcalfe C, Alicke B, Crow A, Lamoureux M, Dijkgraaf GJ, Peale F, Gould SE, de Sauvage FJ.

Cancer Res. 2013 Dec 1;73(23):7034-42. doi: 10.1158/0008-5472.CAN-13-1222. Epub 2013 Oct 23.

16.

Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist.

Wong H, Gould SE, Budha N, Darbonne WC, Kadel EE 3rd, La H, Alicke B, Halladay JS, Erickson R, Portera C, Tolcher AW, Infante JR, Mamounas M, Flygare JA, Hop CE, Fairbrother WJ.

Drug Metab Dispos. 2013 Dec;41(12):2104-13. doi: 10.1124/dmd.113.053926. Epub 2013 Sep 16.

17.

Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier.

Salphati L, Heffron TP, Alicke B, Nishimura M, Barck K, Carano RA, Cheong J, Edgar KA, Greve J, Kharbanda S, Koeppen H, Lau S, Lee LB, Pang J, Plise EG, Pokorny JL, Reslan HB, Sarkaria JN, Wallin JJ, Zhang X, Gould SE, Olivero AG, Phillips HS.

Clin Cancer Res. 2012 Nov 15;18(22):6239-48. doi: 10.1158/1078-0432.CCR-12-0720. Epub 2012 Sep 19.

18.

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

Heffron TP, Salphati L, Alicke B, Cheong J, Dotson J, Edgar K, Goldsmith R, Gould SE, Lee LB, Lesnick JD, Lewis C, Ndubaku C, Nonomiya J, Olivero AG, Pang J, Plise EG, Sideris S, Trapp S, Wallin J, Wang L, Zhang X.

J Med Chem. 2012 Sep 27;55(18):8007-20. Epub 2012 Sep 11.

PMID:
22946614
19.

Dogs are more sensitive to antagonists of inhibitor of apoptosis proteins than rats and humans: a translational toxicokinetic/toxicodynamic analysis.

Wong H, Budha NR, West K, Blackwood E, Ware JA, Yu R, Darbonne WC, Gould SE, Steigerwalt R, Erickson R, Hop CE, LoRusso P, Eckhardt SG, Wagner A, Chan IT, Mamounas M, Flygare JA, Fairbrother WJ.

Toxicol Sci. 2012 Nov;130(1):205-13. doi: 10.1093/toxsci/kfs235. Epub 2012 Jul 28.

PMID:
22843607
20.

Antitumor activity of targeted and cytotoxic agents in murine subcutaneous tumor models correlates with clinical response.

Wong H, Choo EF, Alicke B, Ding X, La H, McNamara E, Theil FP, Tibbitts J, Friedman LS, Hop CE, Gould SE.

Clin Cancer Res. 2012 Jul 15;18(14):3846-55. doi: 10.1158/1078-0432.CCR-12-0738. Epub 2012 May 30.

21.

Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.

Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J.

J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29.

PMID:
22335519
22.

Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathway activation.

Wong H, Alicke B, West KA, Pacheco P, La H, Januario T, Yauch RL, de Sauvage FJ, Gould SE.

Clin Cancer Res. 2011 Jul 15;17(14):4682-92. doi: 10.1158/1078-0432.CCR-11-0975. Epub 2011 May 24.

23.

Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Wenglowsky S, Ren L, Ahrendt KA, Laird ER, Aliagas I, Alicke B, Buckmelter AJ, Choo EF, Dinkel V, Feng B, Gloor SL, Gould SE, Gross S, Gunzner-Toste J, Hansen JD, Hatzivassiliou G, Liu B, Malesky K, Mathieu S, Newhouse B, Raddatz NJ, Ran Y, Rana S, Randolph N, Risom T, Rudolph J, Savage S, Selby LT, Shrag M, Song K, Sturgis HL, Voegtli WC, Wen Z, Willis BS, Woessner RD, Wu WI, Young WB, Grina J.

ACS Med Chem Lett. 2011 Mar 8;2(5):342-7. doi: 10.1021/ml200025q. eCollection 2011 May 12.

24.

Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449).

Giannetti AM, Wong H, Dijkgraaf GJ, Dueber EC, Ortwine DF, Bravo BJ, Gould SE, Plise EG, Lum BL, Malhi V, Graham RA.

J Med Chem. 2011 Apr 28;54(8):2592-601. doi: 10.1021/jm1008924. Epub 2011 Mar 25.

PMID:
21438527
25.

Small molecule inhibition of GDC-0449 refractory smoothened mutants and downstream mechanisms of drug resistance.

Dijkgraaf GJ, Alicke B, Weinmann L, Januario T, West K, Modrusan Z, Burdick D, Goldsmith R, Robarge K, Sutherlin D, Scales SJ, Gould SE, Yauch RL, de Sauvage FJ.

Cancer Res. 2011 Jan 15;71(2):435-44. doi: 10.1158/0008-5472.CAN-10-2876. Epub 2010 Dec 1.

26.

X chromosome-linked inhibitor of apoptosis regulates cell death induction by proapoptotic receptor agonists.

Varfolomeev E, Alicke B, Elliott JM, Zobel K, West K, Wong H, Scheer JM, Ashkenazi A, Gould SE, Fairbrother WJ, Vucic D.

J Biol Chem. 2009 Dec 11;284(50):34553-60. doi: 10.1074/jbc.M109.040139. Epub 2009 Oct 23.

27.

Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma.

Yauch RL, Dijkgraaf GJ, Alicke B, Januario T, Ahn CP, Holcomb T, Pujara K, Stinson J, Callahan CA, Tang T, Bazan JF, Kan Z, Seshagiri S, Hann CL, Gould SE, Low JA, Rudin CM, de Sauvage FJ.

Science. 2009 Oct 23;326(5952):572-4. doi: 10.1126/science.1179386. Epub 2009 Sep 2.

28.

Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449.

Rudin CM, Hann CL, Laterra J, Yauch RL, Callahan CA, Fu L, Holcomb T, Stinson J, Gould SE, Coleman B, LoRusso PM, Von Hoff DD, de Sauvage FJ, Low JA.

N Engl J Med. 2009 Sep 17;361(12):1173-8. doi: 10.1056/NEJMoa0902903. Epub 2009 Sep 2.

29.

GDC-0449-a potent inhibitor of the hedgehog pathway.

Robarge KD, Brunton SA, Castanedo GM, Cui Y, Dina MS, Goldsmith R, Gould SE, Guichert O, Gunzner JL, Halladay J, Jia W, Khojasteh C, Koehler MF, Kotkow K, La H, Lalonde RL, Lau K, Lee L, Marshall D, Marsters JC Jr, Murray LJ, Qian C, Rubin LL, Salphati L, Stanley MS, Stibbard JH, Sutherlin DP, Ubhayaker S, Wang S, Wong S, Xie M.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5576-81. doi: 10.1016/j.bmcl.2009.08.049. Epub 2009 Aug 15. Erratum in: Bioorg Med Chem Lett. 2010 Jan 15;20(2):771.

PMID:
19716296
30.

A paracrine requirement for hedgehog signalling in cancer.

Yauch RL, Gould SE, Scales SJ, Tang T, Tian H, Ahn CP, Marshall D, Fu L, Januario T, Kallop D, Nannini-Pepe M, Kotkow K, Marsters JC, Rubin LL, de Sauvage FJ.

Nature. 2008 Sep 18;455(7211):406-10. doi: 10.1038/nature07275. Epub 2008 Aug 27.

PMID:
18754008
31.

BMP-7 regulates chemokine, cytokine, and hemodynamic gene expression in proximal tubule cells.

Gould SE, Day M, Jones SS, Dorai H.

Kidney Int. 2002 Jan;61(1):51-60.

32.

Cellular contribution of bone graft to fusion.

Gould SE, Rhee JM, Tay BK-B, Otsuka NY, Bradford DS.

J Orthop Res. 2000 Nov;18(6):920-7.

PMID:
11192252
33.

Histochemical and molecular analyses of distraction osteogenesis in a mouse model.

Tay BK, Le AX, Gould SE, Helms JA.

J Orthop Res. 1998 Sep;16(5):636-42.

PMID:
9820290
34.

Neural induction and antero-posterior patterning in the amphibian embryo: past, present and future.

Gould SE, Grainger RM.

Cell Mol Life Sci. 1997 Apr;53(4):319-38. Review.

PMID:
9137624
35.
37.

A screening programme for hypertension in general practice.

Taylor FR, Gould SE, Taylor NA.

J Hum Hypertens. 1990 Aug;4(4):350-2.

PMID:
2258871
38.

The effects of ketanserin on ventricular ectopic activity in humans.

Marks C, Dews I, Gould SE, Stephens J, VandenBurg M.

Cardiovasc Drugs Ther. 1990 Jan;4 Suppl 1:93-5.

PMID:
2285656
39.

Could the increased antihypertensive efficacy of ketanserin in the elderly be due to altered pharmacokinetics?

Gould SE, Silas JH, Hosie J.

Cardiovasc Drugs Ther. 1990 Jan;4 Suppl 1:89-92.

PMID:
2285655
40.

A placebo-controlled crossover study of ketanserin in elderly hypertensive patients.

McCarthy ST, McCarthy GL, John SM, Gould SE.

Cardiovasc Drugs Ther. 1990 Jan;4 Suppl 1:115-7.

PMID:
2285640
41.

Serotonin antagonism reduces the adverse symptoms of beta blockade.

Korlipara K, Gould SE, Taylor NA, Chandler A.

Cardiovasc Drugs Ther. 1990 Jan;4 Suppl 1:127-31.

PMID:
1981022
42.

Comparative study of ketanserin and hydrochlorothiazide in essential hypertension. Janssen Research Group.

Bayman IW, Gould SE, Turner JF.

Drugs. 1988;36 Suppl 1:140-3. No abstract available.

PMID:
3240728
43.

Ketanserin, an effective third-line agent in primary hypertension.

Murphy JJ, Whincup PH, Gould SE, Wilcox RG.

Drugs. 1988;36 Suppl 1:135-9. No abstract available.

PMID:
3071457
44.

Comparative trial of ketanserin or bendrofluazide as add-on therapy in hypertensive patients uncontrolled on a beta-blocker alone.

Korlipara K, Gould SE, Taylor NA, Chandler TC.

Drugs. 1988;36 Suppl 1:130-4. No abstract available.

PMID:
3071456
45.

A comparative study of ketanserin and metoprolol in essential hypertension.

Kane JA, Tooley M, Sibbald B, Gould SE.

J Hypertens Suppl. 1986 Apr;4(1):S63-5.

PMID:
2939215
46.

Serum and cyst concentrations of mebendazole and flubendazole in hydatid disease.

Morris DL, Gould SE.

Br Med J (Clin Res Ed). 1982 Jul 17;285(6336):175. No abstract available.

47.

The uptake of kynurenine, a tryptophan metabolite, into mouse brain [proceedings].

Gould SE.

Br J Pharmacol. 1979 Jul;66(3):484P-485P. No abstract available.

48.
49.

Coronary heart disease and stroke. Atherosclerosis in Japanese men in Hiroshima, Japan and Honolulu, Hawaii.

Gould SE, Hayashi T, Tashiro T, Tanimura A, Nakashima T, Shohoji T.

Arch Pathol. 1972 Feb;93(2):98-102. No abstract available.

PMID:
5009022
50.

IV. Degenerative changes. Cardiovascular disease.

Gould SE, Anderson RE.

Hum Pathol. 1971 Dec;2(4):547-9. No abstract available.

PMID:
5111826

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