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Items: 1 to 50 of 91

1.

A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors.

Romero C, Lambert LJ, Sheffler DJ, De Backer LJS, Raveendra-Panickar D, Celeridad M, Grotegut S, Rodiles S, Holleran J, Sergienko E, Pasquale EB, Cosford NDP, Tautz L.

J Biol Chem. 2020 Feb 28;295(9):2601-2613. doi: 10.1074/jbc.RA119.010838. Epub 2020 Jan 17.

PMID:
31953320
2.

Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2).

Chaikuad A, Koschade SE, Stolz A, Zivkovic K, Pohl C, Shaid S, Ren H, Lambert LJ, Cosford NDP, Brandts CH, Knapp S.

Biochem J. 2019 Mar 12;476(5):875-887. doi: 10.1042/BCJ20190038.

PMID:
30782972
3.

A Combination of Flow and Batch Mode Processes for the Efficient Preparation of mGlu2/3 Receptor Negative Allosteric Modulators (NAMs).

Dhanya RP, Herath A, Sheffler DJ, Cosford NDP.

Tetrahedron. 2018 Jun 21;74(25):3165-3170. doi: 10.1016/j.tet.2018.03.068. Epub 2018 Mar 30.

4.

Autophagy in Cancer: Regulation by Small Molecules.

Limpert AS, Lambert LJ, Bakas NA, Bata N, Brun SN, Shaw RJ, Cosford NDP.

Trends Pharmacol Sci. 2018 Dec;39(12):1021-1032. doi: 10.1016/j.tips.2018.10.004. Review.

5.

Metabotropic Glutamate Receptor 5 as a Target for the Treatment of Depression and Smoking: Robust Preclinical Data but Inconclusive Clinical Efficacy.

Barnes SA, Sheffler DJ, Semenova S, Cosford NDP, Bespalov A.

Biol Psychiatry. 2018 Jun 1;83(11):955-962. doi: 10.1016/j.biopsych.2018.03.001. Epub 2018 Mar 9. Review.

6.

Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.

Pinkerton AB, Sergienko E, Bravo Y, Dahl R, Ma CT, Sun Q, Jackson MR, Cosford NDP, Millán JL.

Bioorg Med Chem Lett. 2018 Jan 1;28(1):31-34. doi: 10.1016/j.bmcl.2017.11.024. Epub 2017 Nov 11.

7.

Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[11C]methoxyphenyl) quinoline-2-carboxamide, for Imaging of Metabotropic Glutamate Receptor 2.

Zhang X, Kumata K, Yamasaki T, Cheng R, Hatori A, Ma L, Zhang Y, Xie L, Wang L, Kang HJ, Sheffler DJ, Cosford NDP, Zhang MR, Liang SH.

ACS Chem Neurosci. 2017 Sep 20;8(9):1937-1948. doi: 10.1021/acschemneuro.7b00098. Epub 2017 Jun 13.

8.

Inducing death in tumor cells: roles of the inhibitor of apoptosis proteins.

Finlay D, Teriete P, Vamos M, Cosford NDP, Vuori K.

F1000Res. 2017 Apr 27;6:587. doi: 10.12688/f1000research.10625.1. eCollection 2017. Review.

9.

An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.

Pagano N, Teriete P, Mattmann ME, Yang L, Snyder BA, Cai Z, Heil ML, Cosford NDP.

Bioorg Med Chem. 2017 Dec 1;25(23):6248-6265. doi: 10.1016/j.bmc.2017.03.061. Epub 2017 Apr 8.

10.

Continuous-flow synthesis of highly functionalized imidazo-oxadiazoles facilitated by microfluidic extraction.

Herath A, Cosford ND.

Beilstein J Org Chem. 2017 Feb 7;13:239-246. doi: 10.3762/bjoc.13.26. eCollection 2017.

11.

Screening for Small Molecule Inhibitors of Statin-Induced APP C-terminal Toxic Fragment Production.

Poksay KS, Sheffler DJ, Spilman P, Campagna J, Jagodzinska B, Descamps O, Gorostiza O, Matalis A, Mullenix M, Bredesen DE, Cosford ND, John V.

Front Pharmacol. 2017 Feb 15;8:46. doi: 10.3389/fphar.2017.00046. eCollection 2017.

12.

Characterization of Potent SMAC Mimetics that Sensitize Cancer Cells to TNF Family-Induced Apoptosis.

Welsh K, Milutinovic S, Ardecky RJ, Gonzalez-Lopez M, Ganji SR, Teriete P, Finlay D, Riedl S, Matsuzawa S, Pinilla C, Houghten R, Vuori K, Reed JC, Cosford ND.

PLoS One. 2016 Sep 12;11(9):e0161952. doi: 10.1371/journal.pone.0161952. eCollection 2016.

13.

Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids.

Wang H, Teriete P, Hu A, Raveendra-Panickar D, Pendelton K, Lazo JS, Eiseman J, Holien T, Misund K, Oliynyk G, Arsenian-Henriksson M, Cosford ND, Sundan A, Prochownik EV.

Oncotarget. 2015 Oct 20;6(32):32380-95. doi: 10.18632/oncotarget.6116.

14.

BIRC2/cIAP1 Is a Negative Regulator of HIV-1 Transcription and Can Be Targeted by Smac Mimetics to Promote Reversal of Viral Latency.

Pache L, Dutra MS, Spivak AM, Marlett JM, Murry JP, Hwang Y, Maestre AM, Manganaro L, Vamos M, Teriete P, Martins LJ, König R, Simon V, Bosque A, Fernandez-Sesma A, Cosford ND, Bushman FD, Young JA, Planelles V, Chanda SK.

Cell Host Microbe. 2015 Sep 9;18(3):345-53. doi: 10.1016/j.chom.2015.08.009.

15.

Cell-Based High-Throughput Luciferase Reporter Gene Assays for Identifying and Profiling Chemical Modulators of Endoplasmic Reticulum Signaling Protein, IRE1.

Rong J, Pass I, Diaz PW, Ngo TA, Sauer M, Magnuson G, Zeng FY, Hassig CA, Jackson MR, Cosford ND, Matsuzawa S, Reed JC.

J Biomol Screen. 2015 Dec;20(10):1232-45. doi: 10.1177/1087057115600414. Epub 2015 Aug 11.

PMID:
26265713
16.

Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.

Egan DF, Chun MG, Vamos M, Zou H, Rong J, Miller CJ, Lou HJ, Raveendra-Panickar D, Yang CC, Sheffler DJ, Teriete P, Asara JM, Turk BE, Cosford ND, Shaw RJ.

Mol Cell. 2015 Jul 16;59(2):285-97. doi: 10.1016/j.molcel.2015.05.031. Epub 2015 Jun 25.

17.

Perturbation of the c-Myc-Max protein-protein interaction via synthetic α-helix mimetics.

Jung KY, Wang H, Teriete P, Yap JL, Chen L, Lanning ME, Hu A, Lambert LJ, Holien T, Sundan A, Cosford ND, Prochownik EV, Fletcher S.

J Med Chem. 2015 Apr 9;58(7):3002-24. doi: 10.1021/jm501440q. Epub 2015 Mar 30.

18.

Benzodiazepinone derivatives protect against endoplasmic reticulum stress-mediated cell death in human neuronal cell lines.

Zou H, Limpert AS, Zou J, Dembo A, Lee PS, Grant D, Ardecky R, Pinkerton AB, Magnuson GK, Goldman ME, Rong J, Teriete P, Sheffler DJ, Reed JC, Cosford ND.

ACS Chem Neurosci. 2015 Mar 18;6(3):464-75. doi: 10.1021/cn500297v. Epub 2015 Jan 17.

19.

Triggering necroptosis in cisplatin and IAP antagonist-resistant ovarian carcinoma.

McCabe KE, Bacos K, Lu D, Delaney JR, Axelrod J, Potter MD, Vamos M, Wong V, Cosford ND, Xiang R, Stupack DG.

Cell Death Dis. 2014 Oct 30;5:e1496. doi: 10.1038/cddis.2014.448.

20.

Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.

Bravo Y, Teriete P, Dhanya RP, Dahl R, Lee PS, Kiffer-Moreira T, Ganji SR, Sergienko E, Smith LH, Farquharson C, Millán JL, Cosford ND.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4308-11. doi: 10.1016/j.bmcl.2014.07.013. Epub 2014 Jul 15.

21.

Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.

Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND.

J Med Chem. 2014 May 22;57(10):4154-72. doi: 10.1021/jm5000563. Epub 2014 May 9.

22.

Selective inhibitors of FAS-TE.

Ardecky R, Hedrick MP, Gosalia P, Yamamoto F, Milewski M, Barron N, Sun Q, Zhou J, Ganji S, Mehta A, Sugarman E, Nguyen K, Vasile S, Suyama E, Teriete P, Sheffler D, Lee PS, Mattmann M, De Ingeniis J, Stonich D, Mangravita-Novo A, Salaniwal S, Kung P, Diwan J, Smith LH, Sergienko E, Chung TDY, Pinkerton AB, Cosford NDP, Smith JW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 12 [updated 2014 Jan 13].

23.

Translational enhancers of EAAT2: therapeutic implications for neurodegenerative disease.

Limpert AS, Cosford ND.

J Clin Invest. 2014 Mar;124(3):964-7. doi: 10.1172/JCI74608. Epub 2014 Feb 24.

24.

2-Aminopyridines via reaction of pyridine N-oxides and activated isocyanides.

Vamos M, Cosford ND.

J Org Chem. 2014 Mar 7;79(5):2274-80. doi: 10.1021/jo402693s. Epub 2014 Feb 18.

25.

Small-molecule IAP antagonists sensitize cancer cells to TRAIL-induced apoptosis: roles of XIAP and cIAPs.

Finlay D, Vamos M, González-López M, Ardecky RJ, Ganji SR, Yuan H, Su Y, Cooley TR, Hauser CT, Welsh K, Reed JC, Cosford ND, Vuori K.

Mol Cancer Ther. 2014 Jan;13(1):5-15. doi: 10.1158/1535-7163.MCT-13-0153. Epub 2013 Nov 5.

26.

Amphiphilic suramin dissolves Matrigel, causing an 'inhibition' artefact within in vitro angiogenesis assays.

Prigozhina NL, Heisel AJ, Seldeen JR, Cosford ND, Price JH.

Int J Exp Pathol. 2013 Dec;94(6):412-7. doi: 10.1111/iep.12043. Epub 2013 Sep 2.

27.

Inhibitors of tissue-nonspecific alkaline phosphatase (TNAP): from hits to leads.

Teriete P, Pinkerton AB, Cosford ND.

Methods Mol Biol. 2013;1053:85-101. doi: 10.1007/978-1-62703-562-0_5.

PMID:
23860648
28.

Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS).

Limpert AS, Mattmann ME, Cosford ND.

Beilstein J Org Chem. 2013 Apr 15;9:717-32. doi: 10.3762/bjoc.9.82. Print 2013.

29.

Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.

Ardecky RJ, Welsh K, Finlay D, Lee PS, González-López M, Ganji SR, Ravanan P, Mace PD, Riedl SJ, Vuori K, Reed JC, Cosford ND.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4253-7. doi: 10.1016/j.bmcl.2013.04.096. Epub 2013 May 14.

30.

Expedient synthesis of highly potent antagonists of inhibitor of apoptosis proteins (IAPs) with unique selectivity for ML-IAP.

Vamos M, Welsh K, Finlay D, Lee PS, Mace PD, Snipas SJ, Gonzalez ML, Ganji SR, Ardecky RJ, Riedl SJ, Salvesen GS, Vuori K, Reed JC, Cosford ND.

ACS Chem Biol. 2013 Apr 19;8(4):725-32. doi: 10.1021/cb3005512. Epub 2013 Feb 5.

31.

Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.

Sidique S, Dhanya RP, Sheffler DJ, Nickols HH, Yang L, Dahl R, Mangravita-Novo A, Smith LH, D'Souza MS, Semenova S, Conn PJ, Markou A, Cosford ND.

J Med Chem. 2012 Nov 26;55(22):9434-45. doi: 10.1021/jm3005306. Epub 2012 Oct 23.

32.

Pharmacological inhibition of PHOSPHO1 suppresses vascular smooth muscle cell calcification.

Kiffer-Moreira T, Yadav MC, Zhu D, Narisawa S, Sheen C, Stec B, Cosford ND, Dahl R, Farquharson C, Hoylaerts MF, Macrae VE, Millán JL.

J Bone Miner Res. 2013 Jan;28(1):81-91. doi: 10.1002/jbmr.1733.

33.

Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

Sheffler DJ, Pinkerton AB, Dahl R, Markou A, Cosford ND.

ACS Chem Neurosci. 2011 Aug 17;2(8):382-93. doi: 10.1021/cn200008d. Epub 2011 Apr 12. Review.

34.

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.

Sheffler DJ, Wenthur CJ, Bruner JA, Carrington SJ, Vinson PN, Gogi KK, Blobaum AL, Morrison RD, Vamos M, Cosford ND, Stauffer SR, Daniels JS, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3921-5. doi: 10.1016/j.bmcl.2012.04.112. Epub 2012 Apr 30.

35.

Automated Multistep Continuous Flow Synthesis of 2-(1H-Indol-3-yl)thiazole Derivatives.

Pagano N, Heil ML, Cosford ND.

Synthesis (Stuttg). 2012;44(16):2537-2546.

36.

Inhibition of hematopoietic protein tyrosine phosphatase augments and prolongs ERK1/2 and p38 activation.

Sergienko E, Xu J, Liu WH, Dahl R, Critton DA, Su Y, Brown BT, Chan X, Yang L, Bobkova EV, Vasile S, Yuan H, Rascon J, Colayco S, Sidique S, Cosford ND, Chung TD, Mustelin T, Page R, Lombroso PJ, Tautz L.

ACS Chem Biol. 2012 Feb 17;7(2):367-77. doi: 10.1021/cb2004274. Epub 2011 Nov 17.

37.

Phosphomannose isomerase inhibitors improve N-glycosylation in selected phosphomannomutase-deficient fibroblasts.

Sharma V, Ichikawa M, He P, Scott DA, Bravo Y, Dahl R, Ng BG, Cosford ND, Freeze HH.

J Biol Chem. 2011 Nov 11;286(45):39431-8. doi: 10.1074/jbc.M111.285502. Epub 2011 Sep 26. Erratum in: J Biol Chem. 2011 Dec 16;286(50):43588. Scott, David A [added].

39.

A disalicylic acid-furanyl derivative inhibits ephrin binding to a subset of Eph receptors.

Noberini R, De SK, Zhang Z, Wu B, Raveendra-Panickar D, Chen V, Vazquez J, Qin H, Song J, Cosford ND, Pellecchia M, Pasquale EB.

Chem Biol Drug Des. 2011 Oct;78(4):667-78. doi: 10.1111/j.1747-0285.2011.01199.x. Epub 2011 Sep 6.

40.

Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

González-López M, Welsh K, Finlay D, Ardecky RJ, Ganji SR, Su Y, Yuan H, Teriete P, Mace PD, Riedl SJ, Vuori K, Reed JC, Cosford ND.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4332-6. doi: 10.1016/j.bmcl.2011.05.049. Epub 2011 May 24.

41.

Antagonists of IAP-family anti-apoptotic proteins - Probe 2.

Lopez M, Welsh K, Yuan H, Stonich D, Su Y, Garcia X, Cuddy M, Houghten R, Sergienko E, Reed JC, Ardecky R, Reddy S, Finlay D, Vuori K, Dad S, Chung TDY, Cosford NDP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Sep 1 [updated 2011 Feb 10].

42.

Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.

Dahl R, Bravo Y, Sharma V, Ichikawa M, Dhanya RP, Hedrick M, Brown B, Rascon J, Vicchiarelli M, Mangravita-Novo A, Yang L, Stonich D, Su Y, Smith LH, Sergienko E, Freeze HH, Cosford ND.

J Med Chem. 2011 May 26;54(10):3661-8. doi: 10.1021/jm101401a. Epub 2011 May 3.

43.

A Cell Based Assay for the Identification of Lead Compounds with Anti-Viral Activity Against West Nile Virus.

Chung DH, Ardecky R, Ganji SR, Cosford NDP, Jonsson CB, Moore BP, Jia F, Maddox C, McKellip SN, White EL, Ananthan S, Feng S, Rasmussen L, Su Y, Chung TDY, Dad S, Tower NA, Heil M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 27 [updated 2010 Oct 4].

44.

The Role of PHOSPHO1 in the Initiation of Skeletal Calcification.

Stonich D, Su Y, Dad S, Reddy S, Mostofi Y, Russell D, Chung TDY, Hedrick NM, Rascon J, Garcia X, Sergienko E, Millán JL, Stonich D, Cosford N.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Apr 18 [updated 2010 Sep 2].

45.

Therapeutic Inhibitors of Phosphomannose Isomerase - Probe 2.

Hedrick M, Brown B, Rascon J, Sergienko E, Sharma V, Ng B, Ichikawa M, Freeze H, Stonich D, Su Y, Dad S, Chung TDY, Dahl R, Cosford N.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 May 17 [updated 2010 Sep 2].

46.

Therapeutic Inhibitors of Phosphomannose Isomerase - Probe 1.

Hedrick M, Brown B, Rascon J, Sergienko E, Sharma V, Ng B, Ichikawa M, Freeze H, Stonich D, Su Y, Chung TDY, Dahl R, Cosford N.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Apr 21 [updated 2010 Sep 2].

47.

Placental Alkaline Phosphatase (PLAP) Luminescent HTS assay - Probe 1.

Sergienko E, Garcia X, Brown B, Rascon J, Narisawa S, Simao AM, Millán JL, Stonich D, Su Y, Khan P, Roth G, Smith L, Dad S, Chung TDY, Cosford NDP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Apr 18 [updated 2010 Sep 2].

48.

Antagonists of IAP-family anti-apoptotic proteins - Probe 1.

Welsh K, Yuan H, Stonich D, Su Y, Garcia X, Cuddy M, Houghten R, Sergienko E, Reed JC, Ardecky R, Ganji SR, Lopez M, Dad S, Chung TDY, Cosford N.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 May 18 [updated 2010 Sep 2].

49.

HTS identification of compounds activating TNAP at an intermediate concentration of phosphate acceptor detected in luminescent assay.

Chan X, Brown B, Hedrick M, Rascon J, Millán JL, Sergienko E, Roth G, Reddy S, Dad S, Chung TDY, Cosford N, Stonich D, Su Y.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Apr 21 [updated 2010 Sep 2].

50.

Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.

Dhanya RP, Sidique S, Sheffler DJ, Nickols HH, Herath A, Yang L, Dahl R, Ardecky R, Semenova S, Markou A, Conn PJ, Cosford ND.

J Med Chem. 2011 Jan 13;54(1):342-53. doi: 10.1021/jm1012165. Epub 2010 Dec 14.

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