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Items: 36

1.

In vitro metabolism, reaction phenotyping, enzyme kinetics, CYP inhibition and induction potential of ataluren.

Kong R, Ma J, Hwang S, Moon YC, Welch EM, Weetall M, Colacino JM, Almstead N, Babiak J, Goodwin E.

Pharmacol Res Perspect. 2020 Apr;8(2):e00576. doi: 10.1002/prp2.576.

2.

Metabolism and Disposition of Ataluren after Oral Administration to Mice, Rats, Dogs, and Humans.

Kong R, Ma J, Hwang S, Goodwin E, Northcutt V, Babiak J, Almstead N, McIntosh J.

Drug Metab Dispos. 2020 Apr;48(4):317-325. doi: 10.1124/dmd.119.089391. Epub 2020 Jan 24.

PMID:
31980502
3.

Ataluren Pharmacokinetics in Healthy Japanese and Caucasian Subjects.

Kong R, Laskin OL, Kaushik D, Jin F, Ma J, McIntosh J, Souza M, Almstead N.

Clin Pharmacol Drug Dev. 2019 Feb;8(2):172-178. doi: 10.1002/cpdd.645. Epub 2019 Jan 10.

4.

Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of Dihydroorotate Dehydrogenase with Favorable Pharmaceutical Properties.

Cao L, Weetall M, Trotta C, Cintron K, Ma J, Kim MJ, Furia B, Romfo C, Graci JD, Li W, Du J, Sheedy J, Hedrick J, Risher N, Yeh S, Qi H, Arasu T, Hwang S, Lennox W, Kong R, Petruska J, Moon YC, Babiak J, Davis TW, Jacobson A, Almstead NG, Branstrom A, Colacino JM, Peltz SW.

Mol Cancer Ther. 2019 Jan;18(1):3-16. doi: 10.1158/1535-7163.MCT-18-0863. Epub 2018 Oct 23.

5.

Correction to Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-Negative Bacteria.

Gerasyuto AI, Arnold MA, Wang J, Chen G, Zhang X, Smith S, Woll MG, Baird J, Zhang N, Almstead NG, Narasimhan J, Peddi S, Dumble M, Sheedy J, Weetall M, Branstrom AA, Prasad JVN, Karp GM.

J Med Chem. 2018 Oct 25;61(20):9394. doi: 10.1021/acs.jmedchem.8b01538. Epub 2018 Oct 16. No abstract available.

6.

Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.

Gerasyuto AI, Arnold MA, Wang J, Chen G, Zhang X, Smith S, Woll MG, Baird J, Zhang N, Almstead NG, Narasimhan J, Peddi S, Dumble M, Sheedy J, Weetall M, Branstrom AA, Prasad JVN, Karp GM.

J Med Chem. 2018 May 24;61(10):4456-4475. doi: 10.1021/acs.jmedchem.8b00114. Epub 2018 May 14. Erratum in: J Med Chem. 2018 Oct 25;61(20):9394.

7.

4-Hydroxy-2-pyridones: Discovery and evaluation of a novel class of antibacterial agents targeting DNA synthesis.

Arnold MA, Gerasyuto AI, Wang J, Du W, Gorske YJK, Arasu T, Baird J, Almstead NG, Narasimhan J, Peddi S, Ginzburg O, Lue SW, Hedrick J, Sheedy J, Lagaud G, Branstrom AA, Weetall M, Prasad JVNV, Karp GM.

Bioorg Med Chem Lett. 2017 Nov 15;27(22):5014-5021. doi: 10.1016/j.bmcl.2017.10.006. Epub 2017 Oct 5.

PMID:
29032026
8.

Discovery of Novel Small Molecule Inhibitors of VEGF Expression in Tumor Cells Using a Cell-Based High Throughput Screening Platform.

Cao L, Weetall M, Bombard J, Qi H, Arasu T, Lennox W, Hedrick J, Sheedy J, Risher N, Brooks PC, Trifillis P, Trotta C, Moon YC, Babiak J, Almstead NG, Colacino JM, Davis TW, Peltz SW.

PLoS One. 2016 Dec 16;11(12):e0168366. doi: 10.1371/journal.pone.0168366. eCollection 2016.

9.

Phase 1 Study of Safety, Tolerability, and Pharmacokinetics of PTC299, an Inhibitor of Stress-Regulated Protein Translation.

Weetall M, Davis T, Elfring G, Northcutt V, Cao L, Moon YC, Riebling P, Dali M, Hirawat S, Babiak J, Colacino J, Almstead N, Spiegel R, Peltz SW.

Clin Pharmacol Drug Dev. 2016 Jul;5(4):296-305. doi: 10.1002/cpdd.240. Epub 2016 Feb 2.

10.

Discovery and Optimization of Small Molecule Splicing Modifiers of Survival Motor Neuron 2 as a Treatment for Spinal Muscular Atrophy.

Woll MG, Qi H, Turpoff A, Zhang N, Zhang X, Chen G, Li C, Huang S, Yang T, Moon YC, Lee CS, Choi S, Almstead NG, Naryshkin NA, Dakka A, Narasimhan J, Gabbeta V, Welch E, Zhao X, Risher N, Sheedy J, Weetall M, Karp GM.

J Med Chem. 2016 Jul 14;59(13):6070-85. doi: 10.1021/acs.jmedchem.6b00460. Epub 2016 Jul 6.

PMID:
27299569
11.

Discovery of 2-(4-sulfonamidophenyl)-indole 3-carboxamides as potent and selective inhibitors with broad hepatitis C virus genotype activity targeting HCV NS4B.

Zhang N, Turpoff A, Zhang X, Huang S, Liu Y, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Pichardo J, Colacino J, Lahser F, Ingravallo P, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):594-601. doi: 10.1016/j.bmcl.2015.11.065. Epub 2015 Nov 19.

PMID:
26652483
12.

6-(Azaindol-2-yl)pyridine-3-sulfonamides as potent and selective inhibitors targeting hepatitis C virus NS4B.

Chen G, Ren H, Zhang N, Lennox W, Turpoff A, Paget S, Li C, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Colacino J, Lahser F, Zhao X, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):781-6. doi: 10.1016/j.bmcl.2014.12.093. Epub 2015 Jan 7.

PMID:
25613678
13.

Motor neuron disease. SMN2 splicing modifiers improve motor function and longevity in mice with spinal muscular atrophy.

Naryshkin NA, Weetall M, Dakka A, Narasimhan J, Zhao X, Feng Z, Ling KK, Karp GM, Qi H, Woll MG, Chen G, Zhang N, Gabbeta V, Vazirani P, Bhattacharyya A, Furia B, Risher N, Sheedy J, Kong R, Ma J, Turpoff A, Lee CS, Zhang X, Moon YC, Trifillis P, Welch EM, Colacino JM, Babiak J, Almstead NG, Peltz SW, Eng LA, Chen KS, Mull JL, Lynes MS, Rubin LL, Fontoura P, Santarelli L, Haehnke D, McCarthy KD, Schmucki R, Ebeling M, Sivaramakrishnan M, Ko CP, Paushkin SV, Ratni H, Gerlach I, Ghosh A, Metzger F.

Science. 2014 Aug 8;345(6197):688-93. doi: 10.1126/science.1250127.

14.

Structure-activity relationship (SAR) optimization of 6-(indol-2-yl)pyridine-3-sulfonamides: identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B.

Zhang N, Zhang X, Zhu J, Turpoff A, Chen G, Morrill C, Huang S, Lennox W, Kakarla R, Liu R, Li C, Ren H, Almstead N, Venkatraman S, Njoroge FG, Gu Z, Clausen V, Graci J, Jung SP, Zheng Y, Colacino JM, Lahser F, Sheedy J, Mollin A, Weetall M, Nomeir A, Karp GM.

J Med Chem. 2014 Mar 13;57(5):2121-35. doi: 10.1021/jm401621g. Epub 2013 Dec 4.

PMID:
24266880
15.

Discovery of novel HCV inhibitors: synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B.

Zhang X, Zhang N, Chen G, Turpoff A, Ren H, Takasugi J, Morrill C, Zhu J, Li C, Lennox W, Paget S, Liu Y, Almstead N, Njoroge FG, Gu Z, Komatsu T, Clausen V, Espiritu C, Graci J, Colacino J, Lahser F, Risher N, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3947-53. doi: 10.1016/j.bmcl.2013.04.049. Epub 2013 Apr 30.

PMID:
23683597
16.

Discovery of N-(4'-(indol-2-yl)phenyl)sulfonamides as novel inhibitors of HCV replication.

Chen G, Ren H, Turpoff A, Arefolov A, Wilde R, Takasugi J, Khan A, Almstead N, Gu Z, Komatsu T, Freund C, Breslin J, Colacino J, Hedrick J, Weetall M, Karp GM.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3942-6. doi: 10.1016/j.bmcl.2013.04.050. Epub 2013 Apr 30.

PMID:
23683596
17.

Identification of PTC725, an orally bioavailable small molecule that selectively targets the hepatitis C Virus NS4B protein.

Gu Z, Graci JD, Lahser FC, Breslin JJ, Jung SP, Crona JH, McMonagle P, Xia E, Liu S, Karp G, Zhu J, Huang S, Nomeir A, Weetall M, Almstead NG, Peltz SW, Tong X, Ralston R, Colacino JM.

Antimicrob Agents Chemother. 2013 Jul;57(7):3250-61. doi: 10.1128/AAC.00527-13. Epub 2013 Apr 29.

18.

Selective synthesis of 1-substituted 4-chloropyrazolo[3,4-d]pyrimidines.

Babu S, Morrill C, Almstead NG, Moon YC.

Org Lett. 2013 Apr 19;15(8):1882-5. doi: 10.1021/ol4005382. Epub 2013 Apr 10.

PMID:
23574146
19.
20.

PTC124 targets genetic disorders caused by nonsense mutations.

Welch EM, Barton ER, Zhuo J, Tomizawa Y, Friesen WJ, Trifillis P, Paushkin S, Patel M, Trotta CR, Hwang S, Wilde RG, Karp G, Takasugi J, Chen G, Jones S, Ren H, Moon YC, Corson D, Turpoff AA, Campbell JA, Conn MM, Khan A, Almstead NG, Hedrick J, Mollin A, Risher N, Weetall M, Yeh S, Branstrom AA, Colacino JM, Babiak J, Ju WD, Hirawat S, Northcutt VJ, Miller LL, Spatrick P, He F, Kawana M, Feng H, Jacobson A, Peltz SW, Sweeney HL.

Nature. 2007 May 3;447(7140):87-91. Epub 2007 Apr 22.

PMID:
17450125
21.

Safety, tolerability, and pharmacokinetics of PTC124, a nonaminoglycoside nonsense mutation suppressor, following single- and multiple-dose administration to healthy male and female adult volunteers.

Hirawat S, Welch EM, Elfring GL, Northcutt VJ, Paushkin S, Hwang S, Leonard EM, Almstead NG, Ju W, Peltz SW, Miller LL.

J Clin Pharmacol. 2007 Apr;47(4):430-44.

PMID:
17389552
22.

Comparison of the pharmacology of hydroxamate- and carboxylate-based matrix metalloproteinase inhibitors (MMPIs) for the treatment of osteoarthritis.

Janusz MJ, Hookfin EB, Brown KK, Hsieh LC, Heitmeyer SA, Taiwo YO, Natchus MG, Pikul S, Almstead NG, De B, Peng SX, Baker TR, Patel V.

Inflamm Res. 2006 Feb;55(2):60-5.

PMID:
16612565
23.

Moderation of iodoacetate-induced experimental osteoarthritis in rats by matrix metalloproteinase inhibitors.

Janusz MJ, Hookfin EB, Heitmeyer SA, Woessner JF, Freemont AJ, Hoyland JA, Brown KK, Hsieh LC, Almstead NG, De B, Natchus MG, Pikul S, Taiwo YO.

Osteoarthritis Cartilage. 2001 Nov;9(8):751-60.

24.

Potent and selective carboxylic acid-based inhibitors of matrix metalloproteinases.

Pikul S, Ohler NE, Ciszewski G, Laufersweiler MC, Almstead NG, De B, Natchus MG, Hsieh LC, Janusz MJ, Peng SX, Branch TM, King SL, Taiwo YO, Mieling GE.

J Med Chem. 2001 Aug 2;44(16):2499-502. No abstract available.

PMID:
11472202
25.

The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold.

Tullis JS, Laufersweiler MJ, VanRens JC, Natchus MG, Bookland RG, Almstead NG, Pikul S, De B, Hsieh LC, Janusz MJ, Branch TM, Peng SX, Jin YY, Hudlicky T, Oppong K.

Bioorg Med Chem Lett. 2001 Aug 6;11(15):1975-9.

PMID:
11454461
26.

Heterocycle-based MMP inhibitors with P2' substituents.

Pikul S, Dunham KM, Almstead NG, De B, Natchus MG, Taiwo YO, Williams LE, Hynd BA, Hsieh LC, Janusz MJ, Gu F, Mieling GE.

Bioorg Med Chem Lett. 2001 Apr 23;11(8):1009-13.

PMID:
11327577
27.

Development of new carboxylic acid-based MMP inhibitors derived from functionalized propargylglycines.

Natchus MG, Bookland RG, Laufersweiler MJ, Pikul S, Almstead NG, De B, Janusz MJ, Hsieh LC, Gu F, Pokross ME, Patel VS, Garver SM, Peng SX, Branch TM, King SL, Baker TR, Foltz DJ, Mieling GE.

J Med Chem. 2001 Mar 29;44(7):1060-71.

PMID:
11297453
28.

Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.

Natchus MG, Bookland RG, De B, Almstead NG, Pikul S, Janusz MJ, Heitmeyer SA, Hookfin EB, Hsieh LC, Dowty ME, Dietsch CR, Patel VS, Garver SM, Gu F, Pokross ME, Mieling GE, Baker TR, Foltz DJ, Peng SX, Bornes DM, Strojnowski MJ, Taiwo YO.

J Med Chem. 2000 Dec 28;43(26):4948-63.

PMID:
11150165
29.

Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.

Cheng M, De B, Pikul S, Almstead NG, Natchus MG, Anastasio MV, McPhail SJ, Snider CE, Taiwo YO, Chen L, Dunaway CM, Gu F, Dowty ME, Mieling GE, Janusz MJ, Wang-Weigand S.

J Med Chem. 2000 Feb 10;43(3):369-80.

PMID:
10669564
30.

Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.

Cheng M, De B, Almstead NG, Pikul S, Dowty ME, Dietsch CR, Dunaway CM, Gu F, Hsieh LC, Janusz MJ, Taiwo YO, Natchus MG, Hudlicky T, Mandel M.

J Med Chem. 1999 Dec 30;42(26):5426-36.

PMID:
10639284
31.

Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.

Almstead NG, Bradley RS, Pikul S, De B, Natchus MG, Taiwo YO, Gu F, Williams LE, Hynd BA, Janusz MJ, Dunaway CM, Mieling GE.

J Med Chem. 1999 Nov 4;42(22):4547-62.

PMID:
10579818
32.

The next generation of MMP inhibitors. Design and synthesis.

De B, Natchus MG, Cheng M, Pikul S, Almstead NG, Taiwo YO, Snider CE, Chen L, Barnett B, Gu F, Dowty M.

Ann N Y Acad Sci. 1999 Jun 30;878:40-60. Review.

PMID:
10415719
33.

Gas chromatographic-mass spectrometric analysis of hydroxylamine for monitoring the metabolic hydrolysis of metalloprotease inhibitors in rat and human liver microsomes.

Peng SX, Strojnowski MJ, Hu JK, Smith BJ, Eichhold TH, Wehmeyer KR, Pikul S, Almstead NG.

J Chromatogr B Biomed Sci Appl. 1999 Mar 5;724(1):181-7.

PMID:
10202971
34.

Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.

Pikul S, McDow Dunham KL, Almstead NG, De B, Natchus MG, Anastasio MV, McPhail SJ, Snider CE, Taiwo YO, Chen L, Dunaway CM, Gu F, Mieling GE.

J Med Chem. 1999 Jan 14;42(1):87-94.

PMID:
9888835
35.

Design and synthesis of conformationally-constrained MMP inhibitors.

Natchus MG, Cheng M, Wahl CT, Pikul S, Almstead NG, Bradley RS, Taiwo YO, Mieling GE, Dunaway CM, Snider CE, McIver JM, Barnett BL, McPhail SJ, Anastasio MB, De B.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2077-80.

PMID:
9873489
36.

Discovery of potent, achiral matrix metalloproteinase inhibitors.

Pikul S, McDow Dunham KL, Almstead NG, De B, Natchus MG, Anastasio MV, McPhail SJ, Snider CE, Taiwo YO, Rydel T, Dunaway CM, Gu F, Mieling GE.

J Med Chem. 1998 Sep 10;41(19):3568-71. No abstract available.

PMID:
9733482

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