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Items: 1 to 20 of 27

1.

Targeting the tumor-promoting microenvironment in MET-amplified NSCLC cells with a novel inhibitor of pro-HGF activation.

Owusu BY, Thomas S, Venukadasula P, Han Z, Janetka JW, Galemmo RA Jr, Klampfer L.

Oncotarget. 2017 May 29. doi: 10.18632/oncotarget.18260. [Epub ahead of print]

2.

Hepatocyte Growth Factor, a Key Tumor-Promoting Factor in the Tumor Microenvironment.

Owusu BY, Galemmo R, Janetka J, Klampfer L.

Cancers (Basel). 2017 Apr 17;9(4). pii: E35. doi: 10.3390/cancers9040035. Review.

3.

Inhibition of pro-HGF activation by SRI31215, a novel approach to block oncogenic HGF/MET signaling.

Owusu BY, Bansal N, Venukadasula PK, Ross LJ, Messick TE, Goel S, Galemmo RA, Klampfer L.

Oncotarget. 2016 May 17;7(20):29492-506. doi: 10.18632/oncotarget.8785.

4.

Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.

Venukadasula PK, Owusu BY, Bansal N, Ross LJ, Hobrath JV, Bao D, Truss JW, Stackhouse M, Messick TE, Klampfer L, Galemmo RA Jr.

ACS Med Chem Lett. 2015 Dec 22;7(2):177-81. doi: 10.1021/acsmedchemlett.5b00357. eCollection 2016 Feb 11.

5.

Unique functional and structural properties of the LRRK2 protein ATP-binding pocket.

Liu Z, Galemmo RA Jr, Fraser KB, Moehle MS, Sen S, Volpicelli-Daley LA, DeLucas LJ, Ross LJ, Valiyaveettil J, Moukha-Chafiq O, Pathak AK, Ananthan S, Kezar H, White EL, Gupta V, Maddry JA, Suto MJ, West AB.

J Biol Chem. 2014 Nov 21;289(47):32937-51. doi: 10.1074/jbc.M114.602318. Epub 2014 Sep 16.

6.

LRRK2 secretion in exosomes is regulated by 14-3-3.

Fraser KB, Moehle MS, Daher JP, Webber PJ, Williams JY, Stewart CA, Yacoubian TA, Cowell RM, Dokland T, Ye T, Chen D, Siegal GP, Galemmo RA, Tsika E, Moore DJ, Standaert DG, Kojima K, Mobley JA, West AB.

Hum Mol Genet. 2013 Dec 15;22(24):4988-5000. doi: 10.1093/hmg/ddt346. Epub 2013 Jul 25.

7.

Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain.

Aubele DL, Hom RK, Adler M, Galemmo RA Jr, Bowers S, Truong AP, Pan H, Beroza P, Neitz RJ, Yao N, Lin M, Tonn G, Zhang H, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Diep L, Fitzgerald K, Hoffman J, Motter R, Fauss D, Tanaka P, Dappen M, Jagodzinski J, Chan W, Konradi AW, Latimer L, Zhu YL, Sham HL, Anderson JP, Bergeron M, Artis DR.

ChemMedChem. 2013 Aug;8(8):1295-313. doi: 10.1002/cmdc.201300166. Epub 2013 Jun 21.

PMID:
23794260
8.

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.

Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA Jr, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M.

Bioorg Med Chem Lett. 2013 May 1;23(9):2743-9. doi: 10.1016/j.bmcl.2013.02.065. Epub 2013 Feb 24.

PMID:
23522834
9.

Oral coadministration of β-glucuronidase to increase exposure of extensively glucuronidated drugs that undergo enterohepatic recirculation.

Eichenbaum G, Hsu CP, Subrahmanyam V, Chen J, Scicinski J, Galemmo RA Jr, Tuman RW, Johnson DL.

J Pharm Sci. 2012 Jul;101(7):2545-56. doi: 10.1002/jps.23113. Epub 2012 Mar 30.

PMID:
22473491
10.

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.

Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7.

PMID:
21813278
11.

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.

Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1838-43. doi: 10.1016/j.bmcl.2011.01.046. Epub 2011 Jan 20.

PMID:
21316234
12.

Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.

Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA Jr, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):315-9. doi: 10.1016/j.bmcl.2010.11.010. Epub 2010 Nov 5.

PMID:
21112785
13.

Studies with an orally bioavailable alpha V integrin antagonist in animal models of ocular vasculopathy: retinal neovascularization in mice and retinal vascular permeability in diabetic rats.

Santulli RJ, Kinney WA, Ghosh S, Decorte BL, Liu L, Tuman RW, Zhou Z, Huebert N, Bursell SE, Clermont AC, Grant MB, Shaw LC, Mousa SA, Galemmo RA Jr, Johnson DL, Maryanoff BE, Damiano BP.

J Pharmacol Exp Ther. 2008 Mar;324(3):894-901. Epub 2007 Dec 14.

14.

Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.

Qiao JX, Cheng X, Smallheer JM, Galemmo RA, Drummond S, Pinto DJ, Cheney DL, He K, Wong PC, Luettgen JM, Knabb RM, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1432-7. Epub 2006 Dec 1.

PMID:
17174550
15.

Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.

Pinto DJ, Galemmo RA Jr, Quan ML, Orwat MJ, Clark C, Li R, Wells B, Woerner F, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, He K, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5584-9. Epub 2006 Sep 11.

PMID:
16963264
16.

The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.

Moriarty KJ, Koblish HK, Garrabrant T, Maisuria J, Khalil E, Ali F, Petrounia IP, Crysler CS, Maroney AC, Johnson DL, Galemmo RA Jr.

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5778-83. Epub 2006 Sep 1.

PMID:
16949284
17.

1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.

Pinto DJ, Orwat MJ, Quan ML, Han Q, Galemmo RA Jr, Amparo E, Wells B, Ellis C, He MY, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, Mersinger L, Kettner C, Bai S, He K, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4141-7. Epub 2006 May 30.

PMID:
16730984
18.

Dihydroquinone ansamycins: toward resolving the conflict between low in vitro affinity and high cellular potency of geldanamycin derivatives.

Maroney AC, Marugan JJ, Mezzasalma TM, Barnakov AN, Garrabrant TA, Weaner LE, Jones WJ, Barnakova LA, Koblish HK, Todd MJ, Masucci JA, Deckman IC, Galemmo RA Jr, Johnson DL.

Biochemistry. 2006 May 2;45(17):5678-85.

PMID:
16634649
19.

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.

Ho CY, Ludovici DW, Maharoof US, Mei J, Sechler JL, Tuman RW, Strobel ED, Andraka L, Yen HK, Leo G, Li J, Almond H, Lu H, DeVine A, Tominovich RM, Baker J, Emanuel S, Gruninger RH, Middleton SA, Johnson DL, Galemmo RA Jr.

J Med Chem. 2005 Dec 29;48(26):8163-73.

PMID:
16366598
20.

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