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Items: 1 to 50 of 53

1.

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.

Drilon A, Nagasubramanian R, Blake JF, Ku N, Tuch BB, Ebata K, Smith S, Lauriault V, Kolakowski GR, Brandhuber BJ, Larsen PD, Bouhana KS, Winski SL, Hamor R, Wu WI, Parker A, Morales TH, Sullivan FX, DeWolf WE, Wollenberg LA, Gordon PR, Douglas-Lindsay DN, Scaltriti M, Benayed R, Raj S, Hanusch B, Schram AM, Jonsson P, Berger MF, Hechtman JF, Taylor BS, Andrews S, Rothenberg SM, Hyman DM.

Cancer Discov. 2017 Sep;7(9):963-972. doi: 10.1158/2159-8290.CD-17-0507. Epub 2017 Jun 3.

PMID:
28578312
2.

Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.

Dransfield PJ, Pattaropong V, Lai S, Fu Z, Kohn TJ, Du X, Cheng A, Xiong Y, Komorowski R, Jin L, Conn M, Tien E, DeWolf WE Jr, Hinklin RJ, Aicher TD, Kraser CF, Boyd SA, Voegtli WC, Condroski KR, Veniant-Ellison M, Medina JC, Houze J, Coward P.

ACS Med Chem Lett. 2016 May 23;7(7):714-8. doi: 10.1021/acsmedchemlett.6b00140. eCollection 2016 Jul 14.

3.

5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.

Kohn TJ, Du X, Lai S, Xiong Y, Komorowski R, Veniant M, Fu Z, Jiao X, Pattaropong V, Chow D, Cardozo M, Jin L, Conn M, DeWolf WE Jr, Kraser CF, Hinklin RJ, Boys ML, Medina JC, Houze J, Dransfield P, Coward P.

ACS Med Chem Lett. 2016 Jun 1;7(7):666-70. doi: 10.1021/acsmedchemlett.6b00145. eCollection 2016 Jul 14.

4.

C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.

Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB.

ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11.

5.

Discovery of 2-pyridylureas as glucokinase activators.

Hinklin RJ, Aicher TD, Anderson DA, Baer BR, Boyd SA, Condroski KR, DeWolf WE Jr, Kraser CF, McVean M, Rhodes SP, Sturgis HL, Voegtli WC, Williams L, Houze JB.

J Med Chem. 2014 Oct 9;57(19):8180-6. doi: 10.1021/jm501204z. Epub 2014 Sep 17.

PMID:
25203462
6.

Characterization of a novel glucokinase activator in rat and mouse models.

Lu M, Li P, Bandyopadhyay G, Lagakos W, Dewolf WE Jr, Alford T, Chicarelli MJ, Williams L, Anderson DA, Baer BR, McVean M, Conn M, Véniant MM, Coward P.

PLoS One. 2014 Feb 12;9(2):e88431. doi: 10.1371/journal.pone.0088431. eCollection 2014.

7.

Identification of a new class of glucokinase activators through structure-based design.

Hinklin RJ, Boyd SA, Chicarelli MJ, Condroski KR, DeWolf WE Jr, Lee PA, Lee W, Singh A, Thomas L, Voegtli WC, Williams L, Aicher TD.

J Med Chem. 2013 Oct 10;56(19):7669-78. doi: 10.1021/jm401116k. Epub 2013 Sep 25.

PMID:
24015910
8.

The kinetic model of the shikimate pathway as a tool to optimize enzyme assays for high-throughput screening.

Noble M, Sinha Y, Kolupaev A, Demin O, Earnshaw D, Tobin F, West J, Martin JD, Qiu C, Liu WS, DeWolf WE Jr, Tew D, Goryanin II.

Biotechnol Bioeng. 2006 Nov 5;95(4):560-73.

PMID:
16921527
9.

Mechanism of time-dependent inhibition of polypeptide deformylase by actinonin.

Van Aller GS, Nandigama R, Petit CM, DeWolf WE Jr, Quinn CJ, Aubart KM, Zalacain M, Christensen SB, Copeland RA, Lai Z.

Biochemistry. 2005 Jan 11;44(1):253-60.

PMID:
15628866
10.

Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF.

J Med Chem. 2003 Apr 24;46(9):1627-35.

PMID:
12699381
11.

Characterization of Streptococcus pneumoniae enoyl-(acyl-carrier protein) reductase (FabK).

Marrakchi H, Dewolf WE Jr, Quinn C, West J, Polizzi BJ, So CY, Holmes DJ, Reed SL, Heath RJ, Payne DJ, Rock CO, Wallis NG.

Biochem J. 2003 Mar 15;370(Pt 3):1055-62.

12.

Defining and combating the mechanisms of triclosan resistance in clinical isolates of Staphylococcus aureus.

Fan F, Yan K, Wallis NG, Reed S, Moore TD, Rittenhouse SF, DeWolf WE Jr, Huang J, McDevitt D, Miller WH, Seefeld MA, Newlander KA, Jakas DR, Head MS, Payne DJ.

Antimicrob Agents Chemother. 2002 Nov;46(11):3343-7.

13.

Discovery of a novel and potent class of FabI-directed antibacterial agents.

Payne DJ, Miller WH, Berry V, Brosky J, Burgess WJ, Chen E, DeWolf WE Jr, Fosberry AP, Greenwood R, Head MS, Heerding DA, Janson CA, Jaworski DD, Keller PM, Manley PJ, Moore TD, Newlander KA, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Slater-Radosti C, Salyers KL, Seefeld MA, Smyth MG, Takata DT, Uzinskas IN, Vaidya K, Wallis NG, Winram SB, Yuan CC, Huffman WF.

Antimicrob Agents Chemother. 2002 Oct;46(10):3118-24.

14.

Structure-based combinatorial library design: discovery of non-peptidic inhibitors of caspases 3 and 8.

Head MS, Ryan MD, Lee D, Feng Y, Janson CA, Concha NO, Keller PM, deWolf WE Jr.

J Comput Aided Mol Des. 2001 Dec;15(12):1105-17.

PMID:
12160093
15.

Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI).

Miller WH, Seefeld MA, Newlander KA, Uzinskas IN, Burgess WJ, Heerding DA, Yuan CC, Head MS, Payne DJ, Rittenhouse SF, Moore TD, Pearson SC, Berry V, DeWolf WE Jr, Keller PM, Polizzi BJ, Qiu X, Janson CA, Huffman WF.

J Med Chem. 2002 Jul 18;45(15):3246-56.

PMID:
12109908
16.

Role of caspases in human renal proximal tubular epithelial cell apoptosis.

Wong VY, Keller PM, Nuttall ME, Kikly K, DeWolf WE Jr, Lee D, Ali SM, Nadeau DP, Grygielko ET, Laping NJ, Brooks DP.

Eur J Pharmacol. 2001 Dec 21;433(2-3):135-40.

PMID:
11755144
17.

Inhibitors of bacterial enoyl acyl carrier protein reductase (FabI): 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as potential antibacterial agents.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, Payne DJ, Rittenhouse SF, Moore TD, DeWolf WE Jr, Keller PM, Qiu X, Janson CA, Vaidya K, Fosberry AP, Smyth MG, Jaworski DD, Slater-Radosti C, Huffman WF.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2241-4.

PMID:
11527706
18.

1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI).

Heerding DA, Chan G, DeWolf WE, Fosberry AP, Janson CA, Jaworski DD, McManus E, Miller WH, Moore TD, Payne DJ, Qiu X, Rittenhouse SF, Slater-Radosti C, Smith W, Takata DT, Vaidya KS, Yuan CC, Huffman WF.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2061-5.

PMID:
11514139
19.

Biochemical and genetic characterization of the action of triclosan on Staphylococcus aureus.

Slater-Radosti C, Van Aller G, Greenwood R, Nicholas R, Keller PM, DeWolf WE Jr, Fan F, Payne DJ, Jaworski DD.

J Antimicrob Chemother. 2001 Jul;48(1):1-6.

PMID:
11418506
20.

Direct cleavage of the human DNA fragmentation factor-45 by granzyme B induces caspase-activated DNase release and DNA fragmentation.

Sharif-Askari E, Alam A, Rhéaume E, Beresford PJ, Scotto C, Sharma K, Lee D, DeWolf WE, Nuttall ME, Lieberman J, Sékaly RP.

EMBO J. 2001 Jun 15;20(12):3101-13.

21.

Potent and selective nonpeptide inhibitors of caspases 3 and 7.

Lee D, Long SA, Murray JH, Adams JL, Nuttall ME, Nadeau DP, Kikly K, Winkler JD, Sung CM, Ryan MD, Levy MA, Keller PM, DeWolf WE Jr.

J Med Chem. 2001 Jun 7;44(12):2015-26.

PMID:
11384246
22.

Inhibition of caspase-3-like activity prevents apoptosis while retaining functionality of human chondrocytes in vitro.

Nuttall ME, Nadeau DP, Fisher PW, Wang F, Keller PM, DeWolf WE Jr, Goldring MB, Badger AM, Lee D, Levy MA, Gowen M, Lark MW.

J Orthop Res. 2000 May;18(3):356-63.

PMID:
10937621
23.

Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality.

Lee D, Long SA, Adams JL, Chan G, Vaidya KS, Francis TA, Kikly K, Winkler JD, Sung CM, Debouck C, Richardson S, Levy MA, DeWolf WE Jr, Keller PM, Tomaszek T, Head MS, Ryan MD, Haltiwanger RC, Liang PH, Janson CA, McDevitt PJ, Johanson K, Concha NO, Chan W, Abdel-Meguid SS, Badger AM, Lark MW, Nadeau DP, Suva LJ, Gowen M, Nuttall ME.

J Biol Chem. 2000 May 26;275(21):16007-14.

24.

Apoptosis in polycystic kidney disease: involvement of caspases.

Ali SM, Wong VY, Kikly K, Fredrickson TA, Keller PM, DeWolf WE Jr, Lee D, Brooks DP.

Am J Physiol Regul Integr Comp Physiol. 2000 Mar;278(3):R763-9.

25.

A substrate combinatorial array for caspases.

Lee D, Adams JL, Brandt M, DeWolf WE Jr, Keller PM, Levy MA.

Bioorg Med Chem Lett. 1999 Jun 21;9(12):1667-72.

PMID:
10397497
26.
27.

Staurosporine-induced apoptosis in cardiomyocytes: A potential role of caspase-3.

Yue TL, Wang C, Romanic AM, Kikly K, Keller P, DeWolf WE Jr, Hart TK, Thomas HC, Storer B, Gu JL, Wang X, Feuerstein GZ.

J Mol Cell Cardiol. 1998 Mar;30(3):495-507.

PMID:
9515027
28.

1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.

Christensen SB, Guider A, Forster CJ, Gleason JG, Bender PE, Karpinski JM, DeWolf WE Jr, Barnette MS, Underwood DC, Griswold DE, Cieslinski LB, Burman M, Bochnowicz S, Osborn RR, Manning CD, Grous M, Hillegas LM, Bartus JO, Ryan MD, Eggleston DS, Haltiwanger RC, Torphy TJ.

J Med Chem. 1998 Mar 12;41(6):821-35.

PMID:
9526558
29.

Role of conserved histidines in catalytic activity and inhibitor binding of human recombinant phosphodiesterase 4A.

Jacobitz S, Ryan MD, McLaughlin MM, Livi GP, DeWolf WE Jr, Torphy TJ.

Mol Pharmacol. 1997 Jun;51(6):999-1006.

30.

Endothelin-converting enzyme: substrate specificity and inhibition by novel analogs of phosphoramidon.

Keller PM, Lee CP, Fenwick AE, Atkinson ST, Elliott JD, DeWolf WE Jr.

Biochem Biophys Res Commun. 1996 Jun 14;223(2):372-8.

PMID:
8670289
31.

Biochemical characteristics and cellular regulation of phosphodiesterase IV.

Torphy TJ, DeWolf WE Jr, Green DW, Livi GP.

Agents Actions Suppl. 1993;43:51-71. Review.

PMID:
8396319
32.

Expression of human preproendothelin-1 cDNA in COS cells results in the production of mature vasoactive endothelin-1.

DiLella AG, Ohlstein E, Elshourbagy N, Bhatnagar PK, Nambi P, DeWolf WE Jr, Caltabiano MM.

Biochem Biophys Res Commun. 1991 Mar 15;175(2):697-705.

PMID:
2018512
33.

Bovine dopamine beta-hydroxylase, primary structure determined by cDNA cloning and amino acid sequencing.

Wang N, Southan C, DeWolf WE Jr, Wells TN, Kruse LI, Leatherbarrow RJ.

Biochemistry. 1990 Jul 10;29(27):6466-74.

PMID:
2207088
34.
35.
36.

Inactivation of dopamine beta-hydroxylase by beta-ethynyltyramine: kinetic characterization and covalent modification of an active site peptide.

DeWolf WE Jr, Chambers PA, Southan C, Saunders D, Kruse LI.

Biochemistry. 1989 May 2;28(9):3833-42.

PMID:
2751998
37.

Inactivation of dopamine beta-hydroxylase by p-cresol: isolation and characterization of covalently modified active site peptides.

DeWolf WE Jr, Carr SA, Varrichio A, Goodhart PJ, Mentzer MA, Roberts GD, Southan C, Dolle RE, Kruse LI.

Biochemistry. 1988 Dec 27;27(26):9093-101.

PMID:
3242615
38.

The copper sites of dopamine beta-hydroxylase: an X-ray absorption spectroscopic study.

Scott RA, Sullivan RJ, DeWolf WE Jr, Dolle RE, Kruse LI.

Biochemistry. 1988 Jul 26;27(15):5411-7.

PMID:
3179263
39.

Effects of the novel dopamine beta-hydroxylase inhibitor SK&F 102698 on catecholamines and blood pressure in spontaneously hypertensive rats.

Berkowitz BA, Arleth AJ, Sung CP, Kruse LI, DeWolf WE Jr, Ohlstein EH.

J Pharmacol Exp Ther. 1988 Jun;245(3):850-7.

PMID:
3385645
40.

Beta-substituted phenethylamines as high-affinity mechanism-based inhibitors of dopamine beta-hydroxylase.

Kruse LI, Kaiser C, DeWolf WE Jr, Chambers PA, Goodhart PJ, Ezekiel M, Ohlstein EH.

J Med Chem. 1988 Apr;31(4):704-6. No abstract available.

PMID:
3351845
41.

Immuno cross-reactivity suggests that catecholamine biosynthesis enzymes and beta-adrenergic receptors may be related.

Shorr RG, Minnich MD, Varrichio A, Strohsacker MW, Gotlib L, Kruse LI, DeWolf WE Jr, Crooke ST.

Mol Pharmacol. 1987 Aug;32(1):195-200.

PMID:
3039336
42.

Mechanism-based inactivation of dopamine beta-hydroxylase by p-cresol and related alkylphenols.

Goodhart PJ, DeWolf WE Jr, Kruse LI.

Biochemistry. 1987 May 5;26(9):2576-83.

PMID:
3607034
43.

Cardiovascular effects of a new potent dopamine beta-hydroxylase inhibitor in spontaneously hypertensive rats.

Ohlstein EH, Kruse LI, Ezekiel M, Sherman SS, Erickson R, DeWolf WE Jr, Berkowitz BA.

J Pharmacol Exp Ther. 1987 May;241(2):554-9.

PMID:
3572812
44.

Multisubstrate inhibitors of dopamine beta-hydroxylase. 2. Structure-activity relationships at the phenethylamine binding site.

Kruse LI, Kaiser C, DeWolf WE Jr, Frazee JS, Ross ST, Wawro J, Wise M, Flaim KE, Sawyer JL, Erickson RW, et al.

J Med Chem. 1987 Mar;30(3):486-94.

PMID:
3820219
45.

Multisubstrate inhibitors of dopamine beta-hydroxylase. 1. Some 1-phenyl and 1-phenyl-bridged derivatives of imidazole-2-thione.

Kruse LI, Kaiser C, DeWolf WE Jr, Frazee JS, Garvey E, Hilbert EL, Faulkner WA, Flaim KE, Sawyer JL, Berkowitz BA.

J Med Chem. 1986 Dec;29(12):2465-72.

PMID:
3783606
46.

Design and kinetic characterization of multisubstrate inhibitors of dopamine beta-hydroxylase.

Kruse LI, DeWolf WE Jr, Chambers PA, Goodhart PJ.

Biochemistry. 1986 Nov 18;25(23):7271-8.

PMID:
3801416
47.

AMP nucleosidase: kinetic mechanism and thermodynamics.

DeWolf WE Jr, Emig FA, Schramm VL.

Biochemistry. 1986 Jul 15;25(14):4132-40.

PMID:
3741845
48.

Substituted 1-benzylimidazole-2-thiols as potent and orally active inhibitors of dopamine beta-hydroxylase.

Kruse LI, Kaiser C, DeWolf WE Jr, Frazee JS, Erickson RW, Ezekiel M, Ohlstein EH, Ruffolo RR Jr, Berkowitz BA.

J Med Chem. 1986 Jun;29(6):887-9. No abstract available.

PMID:
3712378
49.

Studies on the active site of succinyl-CoA:tetrahydrodipicolinate N-succinyltransferase. Characterization using analogs of tetrahydrodipicolinate.

Berges DA, DeWolf WE Jr, Dunn GL, Newman DJ, Schmidt SJ, Taggart JJ, Gilvarg C.

J Biol Chem. 1986 May 15;261(14):6160-7.

50.

Peptides of 2-aminopimelic acid: antibacterial agents that inhibit diaminopimelic acid biosynthesis.

Berges DA, DeWolf WE Jr, Dunn GL, Grappel SF, Newman DJ, Taggart JJ, Gilvarg C.

J Med Chem. 1986 Jan;29(1):89-95.

PMID:
3079832

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