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Items: 1 to 50 of 55

1.

Impact of the Major Candida glabrata Triazole Resistance Determinants on the Activity of the Novel Investigational Tetrazoles VT-1598 and VT-1161.

Nishimoto AT, Whaley SG, Wiederhold NP, Zhang Q, Yates CM, Hoekstra WJ, Schotzinger RJ, Garvey EP, Rogers PD.

Antimicrob Agents Chemother. 2019 Sep 23;63(10). pii: e01304-19. doi: 10.1128/AAC.01304-19. Print 2019 Oct.

PMID:
31383660
2.

Development of Highly Selective Pyrimidine-Based Aldosterone Synthase (CYP11B2) Inhibitors.

Sparks SM, Danger DP, Hoekstra WJ, Leesnitzer T, Schotzinger RJ, Yates CM, Becherer JD.

ACS Med Chem Lett. 2019 Jun 7;10(7):1056-1060. doi: 10.1021/acsmedchemlett.9b00152. eCollection 2019 Jul 11.

PMID:
31312408
3.

In Vitro Activities of the Novel Investigational Tetrazoles VT-1161 and VT-1598 Compared to the Triazole Antifungals against Azole-Resistant Strains and Clinical Isolates of Candida albicans.

Nishimoto AT, Wiederhold NP, Flowers SA, Zhang Q, Kelly SL, Morschhäuser J, Yates CM, Hoekstra WJ, Schotzinger RJ, Garvey EP, Rogers PD.

Antimicrob Agents Chemother. 2019 May 24;63(6). pii: e00341-19. doi: 10.1128/AAC.00341-19. Print 2019 Jun.

PMID:
30910896
4.

In Vivo Efficacy of VT-1129 against Experimental Cryptococcal Meningitis with the Use of a Loading Dose-Maintenance Dose Administration Strategy.

Wiederhold NP, Xu X, Wang A, Najvar LK, Garvey EP, Ottinger EA, Alimardanov A, Cradock J, Behnke M, Hoekstra WJ, Brand SR, Schotzinger RJ, Jaramillo R, Olivo M, Kirkpatrick WR, Patterson TF.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01315-18. doi: 10.1128/AAC.01315-18. Print 2018 Nov.

5.

The Fungal Cyp51 Inhibitor VT-1129 Is Efficacious in an Experimental Model of Cryptococcal Meningitis.

Wiederhold NP, Najvar LK, Garvey EP, Brand SR, Xu X, Ottinger EA, Alimardanov A, Cradock J, Behnke M, Hoekstra WJ, Schotzinger RJ, Jaramillo R, Olivo M, Kirkpatrick WR, Patterson TF.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e01071-18. doi: 10.1128/AAC.01071-18. Print 2018 Sep.

6.

VT-1161 protects mice against oropharyngeal candidiasis caused by fluconazole-susceptible and -resistant Candida albicans.

Break TJ, Desai JV, Natarajan M, Ferre EMN, Henderson C, Zelazny AM, Siebenlist U, Hoekstra WJ, Schotzinger RJ, Garvey EP, Lionakis MS.

J Antimicrob Chemother. 2018 Jan 1;73(1):151-155. doi: 10.1093/jac/dkx352.

7.

Prophylactic Treatment with VT-1161 Protects Immunosuppressed Mice from Rhizopus arrhizus var. arrhizus Infection.

Gebremariam T, Alkhazraji S, Lin L, Wiederhold NP, Garvey EP, Hoekstra WJ, Schotzinger RJ, Patterson TF, Filler SG, Ibrahim AS.

Antimicrob Agents Chemother. 2017 Aug 24;61(9). pii: e00390-17. doi: 10.1128/AAC.00390-17. Print 2017 Sep.

8.

Design and optimization of highly-selective, broad spectrum fungal CYP51 inhibitors.

Yates CM, Garvey EP, Shaver SR, Schotzinger RJ, Hoekstra WJ.

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3243-3248. doi: 10.1016/j.bmcl.2017.06.037. Epub 2017 Jun 15.

PMID:
28651982
9.

The Tetrazole VT-1161 Is a Potent Inhibitor of Trichophyton rubrum through Its Inhibition of T. rubrum CYP51.

Warrilow AGS, Parker JE, Price CL, Garvey EP, Hoekstra WJ, Schotzinger RJ, Wiederhold NP, Nes WD, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00333-17. doi: 10.1128/AAC.00333-17. Print 2017 Jul.

10.

Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity.

Hargrove TY, Garvey EP, Hoekstra WJ, Yates CM, Wawrzak Z, Rachakonda G, Villalta F, Lepesheva GI.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00570-17. doi: 10.1128/AAC.00570-17. Print 2017 Jul.

11.

Efficacy of the Investigational Antifungal VT-1161 in Treating Naturally Occurring Coccidioidomycosis in Dogs.

Shubitz LF, Roy ME, Trinh HT, Hoekstra WJ, Schotzinger RJ, Garvey EP.

Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e00111-17. doi: 10.1128/AAC.00111-17. Print 2017 May.

12.

Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis.

Hargrove TY, Friggeri L, Wawrzak Z, Qi A, Hoekstra WJ, Schotzinger RJ, York JD, Guengerich FP, Lepesheva GI.

J Biol Chem. 2017 Apr 21;292(16):6728-6743. doi: 10.1074/jbc.M117.778308. Epub 2017 Mar 3.

13.

Fungal CYP51 Inhibitors VT-1161 and VT-1129 Exhibit Strong In Vitro Activity against Candida glabrata and C. krusei Isolates Clinically Resistant to Azole and Echinocandin Antifungal Compounds.

Schell WA, Jones AM, Garvey EP, Hoekstra WJ, Schotzinger RJ, Alexander BD.

Antimicrob Agents Chemother. 2017 Feb 23;61(3). pii: e01817-16. doi: 10.1128/AAC.01817-16. Print 2017 Mar.

14.

Activity of VT-1129 against Cryptococcus neoformans clinical isolates with high fluconazole MICs.

Nielsen K, Vedula P, Smith KD, Meya DB, Garvey EP, Hoekstra WJ, Schotzinger RJ, Boulware DR.

Med Mycol. 2017 Jun 1;55(4):453-456. doi: 10.1093/mmy/myw089.

PMID:
27664991
15.

The Investigational Drug VT-1129 Is a Highly Potent Inhibitor of Cryptococcus Species CYP51 but Only Weakly Inhibits the Human Enzyme.

Warrilow AG, Parker JE, Price CL, Nes WD, Garvey EP, Hoekstra WJ, Schotzinger RJ, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4530-8. doi: 10.1128/AAC.00349-16. Print 2016 Aug.

16.

The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii.

Lockhart SR, Fothergill AW, Iqbal N, Bolden CB, Grossman NT, Garvey EP, Brand SR, Hoekstra WJ, Schotzinger RJ, Ottinger E, Patterson TF, Wiederhold NP.

Antimicrob Agents Chemother. 2016 Mar 25;60(4):2528-31. doi: 10.1128/AAC.02770-15. Print 2016 Apr.

17.

Clinical Candidate VT-1161's Antiparasitic Effect In Vitro, Activity in a Murine Model of Chagas Disease, and Structural Characterization in Complex with the Target Enzyme CYP51 from Trypanosoma cruzi.

Hoekstra WJ, Hargrove TY, Wawrzak Z, da Gama Jaen Batista D, da Silva CF, Nefertiti AS, Rachakonda G, Schotzinger RJ, Villalta F, Soeiro Mde N, Lepesheva GI.

Antimicrob Agents Chemother. 2015 Dec 7;60(2):1058-66. doi: 10.1128/AAC.02287-15. Print 2016 Feb.

18.

VT-1161 Protects Immunosuppressed Mice from Rhizopus arrhizus var. arrhizus Infection.

Gebremariam T, Wiederhold NP, Fothergill AW, Garvey EP, Hoekstra WJ, Schotzinger RJ, Patterson TF, Filler SG, Ibrahim AS.

Antimicrob Agents Chemother. 2015 Dec;59(12):7815-7. doi: 10.1128/AAC.01437-15. Epub 2015 Sep 14.

19.

Evaluation of VT-1161 for Treatment of Coccidioidomycosis in Murine Infection Models.

Shubitz LF, Trinh HT, Galgiani JN, Lewis ML, Fothergill AW, Wiederhold NP, Barker BM, Lewis ER, Doyle AL, Hoekstra WJ, Schotzinger RJ, Garvey EP.

Antimicrob Agents Chemother. 2015 Dec;59(12):7249-54. doi: 10.1128/AAC.00593-15. Epub 2015 Sep 14.

20.

Efficacy of the clinical agent VT-1161 against fluconazole-sensitive and -resistant Candida albicans in a murine model of vaginal candidiasis.

Garvey EP, Hoekstra WJ, Schotzinger RJ, Sobel JD, Lilly EA, Fidel PL Jr.

Antimicrob Agents Chemother. 2015 Sep;59(9):5567-73. doi: 10.1128/AAC.00185-15. Epub 2015 Jun 29.

21.

VT-1161 dosed once daily or once weekly exhibits potent efficacy in treatment of dermatophytosis in a guinea pig model.

Garvey EP, Hoekstra WJ, Moore WR, Schotzinger RJ, Long L, Ghannoum MA.

Antimicrob Agents Chemother. 2015 Apr;59(4):1992-7. doi: 10.1128/AAC.04902-14. Epub 2015 Jan 20.

22.

The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme.

Warrilow AG, Hull CM, Parker JE, Garvey EP, Hoekstra WJ, Moore WR, Schotzinger RJ, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2014 Dec;58(12):7121-7. doi: 10.1128/AAC.03707-14. Epub 2014 Sep 15.

23.

Design and optimization of highly-selective fungal CYP51 inhibitors.

Hoekstra WJ, Garvey EP, Moore WR, Rafferty SW, Yates CM, Schotzinger RJ.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3455-8. doi: 10.1016/j.bmcl.2014.05.068. Epub 2014 Jun 9.

PMID:
24948565
24.

Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors.

Rafferty SW, Eisner JR, Moore WR, Schotzinger RJ, Hoekstra WJ.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2444-7. doi: 10.1016/j.bmcl.2014.04.024. Epub 2014 Apr 16.

PMID:
24775307
25.

Tribute to a living legend.

Hoekstra WJ, Pirotte B.

Curr Med Chem. 2012;19(25):4207. No abstract available.

PMID:
23251926
26.

A tribute to a living legend.

Hoekstra WJ, Hilgeroth A, Chou KC, Toth I, McCluskey A, Zhang MR, Cos P.

Med Chem. 2012 Sep;8(5):i. No abstract available.

PMID:
22894697
27.

Co-crystal structure guided array synthesis of PPARgamma inverse agonists.

Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. Epub 2007 May 18.

PMID:
17533125
28.

Design and synthesis of an array of selective androgen receptor modulators.

Trump RP, Blanc JB, Stewart EL, Brown PJ, Caivano M, Gray DW, Hoekstra WJ, Willson TM, Han B, Turnbull P.

J Comb Chem. 2007 Jan-Feb;9(1):107-14.

PMID:
17206838
29.

Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.

Wiethe RW, Stewart EL, Drewry DH, Gray DW, Mehbob A, Hoekstra WJ.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3777-9. Epub 2006 May 5.

PMID:
16678409
30.

Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.

Jones DG, Liang X, Stewart EL, Noe RA, Kallander LS, Madauss KP, Williams SP, Thompson SK, Gray DW, Hoekstra WJ.

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3203-6.

PMID:
15925510
31.

Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.

Hoekstra WJ, Patel HS, Liang X, Blanc JB, Heyer DO, Willson TM, Iannone MA, Kadwell SH, Miller LA, Pearce KH, Simmons CA, Shearin J.

J Med Chem. 2005 Mar 24;48(6):2243-7.

PMID:
15771467
32.

Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.

De Corte BL, Kinney WA, Liu L, Ghosh S, Brunner L, Hoekstra WJ, Santulli RJ, Tuman RW, Baker J, Burns C, Proost JC, Tounge BA, Damiano BP, Maryanoff BE, Johnson DL, Galemmo RA Jr.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.

PMID:
15380233
33.

Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.

Matthews JM, Hoekstra WJ, Dyatkin AB, Hecker LR, Hlasta DJ, Poulter BL, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Reynolds CH, Maryanoff BE.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2747-52.

PMID:
15125926
34.

Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.

Dyatkin AB, Hoekstra WJ, Kinney WA, Kontoyianni M, Santulli RJ, Kimball ES, Fisher MC, Prouty SM, Abraham WM, de Garavilla L, Andrade-Gordon P, Hlasta DJ, He W, Hornby PJ, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):591-6. Erratum in: Bioorg Med Chem Lett. 2004 May 3;14(9):2371.

PMID:
14741249
35.

Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.

Matthews JM, Greco MN, Hecker LR, Hoekstra WJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Maryanoff BE.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):753-6.

PMID:
12639574
36.

Recent advances in peroxisome proliferator-activated receptor science.

Shearer BG, Hoekstra WJ.

Curr Med Chem. 2003 Feb;10(4):267-80. Review.

PMID:
12570700
37.

Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.

Dyatkin AB, Hoekstra WJ, Hlasta DJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Gunnet JW, Hageman W, Look R, Maryanoff BE.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3081-4. Erratum in: Bioorg Med Chem Lett. 2004 Jun 21;14(12):3363.

PMID:
12372506
38.

Antiplatelet and antithrombotic activity of RWJ-53308, a novel orally active glycoprotein IIb/IIIa antagonist.

Damiano BP, Mitchell JA, Giardino E, Corcoran T, Haertlein BJ, de Garavilla L, Kauffman JA, Hoekstra WJ, Maryanoff BE, Andrade-Gordon P.

Thromb Res. 2001 Oct 15;104(2):113-26.

PMID:
11672755
39.

1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists.

Lawson EC, Hoekstra WJ, Addo MF, Andrade-Gordon P, Damiano BP, Kauffman JA, Mitchell JA, Maryanoff BE.

Bioorg Med Chem Lett. 2001 Oct 8;11(19):2619-22.

PMID:
11551763
40.

Tritiated photoactivatable analogs of the native human thrombin receptor (PAR-1) agonist peptide, SFLLRN-NH2.

Elliott JT, Hoekstra WJ, Derian CK, Addo MF, Maryanoff BE, Ahern DG, Prestwich GD.

J Pept Res. 2001 Jun;57(6):494-506.

PMID:
11437953
41.

Protease-activated receptor-2 (PAR-2): structure-function study of receptor activation by diverse peptides related to tethered-ligand epitopes.

Maryanoff BE, Santulli RJ, McComsey DF, Hoekstra WJ, Hoey K, Smith CE, Addo M, Darrow AL, Andrade-Gordon P.

Arch Biochem Biophys. 2001 Feb 15;386(2):195-204.

PMID:
11368342
42.

Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.

Zhang HC, Derian CK, Andrade-Gordon P, Hoekstra WJ, McComsey DF, White KB, Poulter BL, Addo MF, Cheung WM, Damiano BP, Oksenberg D, Reynolds EE, Pandey A, Scarborough RM, Maryanoff BE.

J Med Chem. 2001 Mar 29;44(7):1021-4. No abstract available.

PMID:
11297447
43.

The 2-chlorotrityl resin: a worthy addition to the medicinal chemist's toolbox.

Hoekstra WJ.

Curr Med Chem. 2001 May;8(6):715-9. Review.

PMID:
11281850
44.

Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.

Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF, Mitchell JA, Scott L, Shah RD, Yabut SC.

J Med Chem. 1999 Dec 16;42(25):5254-65.

PMID:
10602710
45.

Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor.

Andrade-Gordon P, Maryanoff BE, Derian CK, Zhang HC, Addo MF, Darrow AL, Eckardt AJ, Hoekstra WJ, McComsey DF, Oksenberg D, Reynolds EE, Santulli RJ, Scarborough RM, Smith CE, White KB.

Proc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62.

46.

Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1).

Elliott JT, Hoekstra WJ, Maryanoff BE, Prestwich GD.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):279-84.

PMID:
10021945
47.

Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif.

Hoekstra WJ, Hulshizer BL, McComsey DF, Andrade-Gordon P, Kauffman JA, Addo MF, Oksenberg D, Scarborough RM, Maryanoff BE.

Bioorg Med Chem Lett. 1998 Jul 7;8(13):1649-54.

PMID:
9873407
48.

Combinatorial chemistry techniques applied to nonpeptide integrin antagonists.

Hoekstra WJ, Poulter BL.

Curr Med Chem. 1998 Jun;5(3):195-204. Review.

PMID:
9562602
49.

NOE-derived conformation of GRGDSP cell adhesion recognition site in the presence of SDS micelles and integrin receptor GPIIB/IIIA.

Mayo KH, Fan F, Beavers MP, Eckardt A, Keane P, Hoekstra WJ, Andrade-Gordon P.

Biochim Biophys Acta. 1996 Aug 15;1296(1):95-102.

PMID:
8765234
50.

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