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Items: 1 to 50 of 158

1.

The anti-parasitic agent suramin and several of its analogues are inhibitors of the DNA binding protein Mcm10.

Paulson CN, John K, Baxley RM, Kurniawan F, Orellana K, Francis R, Sobeck A, Eichman BF, Chazin WJ, Aihara H, Georg GI, Hawkinson JE, Bielinsky AK.

Open Biol. 2019 Aug 30;9(8):190117. doi: 10.1098/rsob.190117. Epub 2019 Aug 14.

2.

Revisiting microtubule targeting agents: α-Tubulin and the pironetin binding site as unexplored targets for cancer therapeutics.

Coulup SK, Georg GI.

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1865-1873. doi: 10.1016/j.bmcl.2019.05.042. Epub 2019 May 21. Review.

PMID:
31130264
3.

The Future Is Now: Artificial Intelligence in Drug Discovery.

Bajorath J, Kearnes S, Walters WP, Georg GI, Wang S.

J Med Chem. 2019 Jun 13;62(11):5249. doi: 10.1021/acs.jmedchem.9b00805. Epub 2019 May 23. No abstract available.

PMID:
31120741
4.

Drug Metabolism and Toxicology Special Issue Call for Papers.

Guengerich FP, Georg GI, Wang S.

J Med Chem. 2019 Feb 14;62(3):1077. doi: 10.1021/acs.jmedchem.9b00005. Epub 2019 Jan 11. No abstract available.

PMID:
30990043
5.

Women in Medicinal Chemistry Special Issue Call for Papers.

Bolognesi ML, Ganamet KL, Liu H, Poulsen SA, Georg GI, Wang S.

J Med Chem. 2019 Apr 25;62(8):3783. doi: 10.1021/acs.jmedchem.9b00534. Epub 2019 Apr 5. No abstract available.

PMID:
30950604
6.

Intranasal Coadministration of a Diazepam Prodrug with a Converting Enzyme Results in Rapid Absorption of Diazepam in Rats.

Rautiola D, Maglalang PD, Cheryala N, Nelson KM, Georg GI, Fine JM, Svitak AL, Faltesek KA, Hanson LR, Mishra U, Coles LD, Cloyd JC, Siegel RA.

J Pharmacol Exp Ther. 2019 Sep;370(3):796-805. doi: 10.1124/jpet.118.255943. Epub 2019 Mar 5.

PMID:
30837282
7.

A Message from the Editors-in-Chief.

Wang S, Georg GI.

J Med Chem. 2019 Mar 14;62(5):2215-2216. doi: 10.1021/acs.jmedchem.9b00235. Epub 2019 Feb 22. No abstract available.

PMID:
30794406
8.

Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (-)-Pironetin.

Coulup SK, Huang DS, Wong HL, Georg GI.

J Med Chem. 2019 Feb 14;62(3):1684-1689. doi: 10.1021/acs.jmedchem.8b01774. Epub 2019 Jan 29.

PMID:
30693770
9.

Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe.

Paulson CN, Guan X, Ayoub AM, Chan A, Karim RM, Pomerantz WCK, Schönbrunn E, Georg GI, Hawkinson JE.

ACS Med Chem Lett. 2018 Oct 31;9(12):1223-1229. doi: 10.1021/acsmedchemlett.8b00380. eCollection 2018 Dec 13.

PMID:
30613330
10.

Syntheses of PDE3A inhibitor ORG9935 and determination of the absolute stereochemistries of its enantiomers by X-ray crystallography.

Jakkaraj S, Young VG Jr, Georg GI.

Tetrahedron. 2018 May 31;74(22):2769-2774. doi: 10.1016/j.tet.2018.04.045. Epub 2018 Apr 18.

11.

Allosteric Modulators of Drug Targets Special Issue.

Haskell-Luevano C, Georg GI, Wang S, Meanwell N.

J Med Chem. 2018 Feb 22;61(4):1381. doi: 10.1021/acs.jmedchem.8b00171. Epub 2018 Feb 7. No abstract available.

PMID:
29412672
12.

Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception.

Syeda SS, Sánchez G, Hong KH, Hawkinson JE, Georg GI, Blanco G.

J Med Chem. 2018 Mar 8;61(5):1800-1820. doi: 10.1021/acs.jmedchem.7b00925. Epub 2018 Jan 19.

13.

Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors.

Chen Y, Zhu JY, Hong KH, Mikles DC, Georg GI, Goldstein AS, Amory JK, Schönbrunn E.

ACS Chem Biol. 2018 Mar 16;13(3):582-590. doi: 10.1021/acschembio.7b00685. Epub 2018 Jan 3.

14.

Synthesis and evaluation of C2 functionalized analogs of the α-tubulin-binding natural product pironetin.

Huang DS, Wong HL, Georg GI.

Bioorg Med Chem Lett. 2018 Sep 1;28(16):2789-2793. doi: 10.1016/j.bmcl.2017.10.057. Epub 2017 Nov 11.

PMID:
29138028
15.

Heme Binding Biguanides Target Cytochrome P450-Dependent Cancer Cell Mitochondria.

Guo Z, Sevrioukova IF, Denisov IG, Zhang X, Chiu TL, Thomas DG, Hanse EA, Cuellar RAD, Grinkova YV, Langenfeld VW, Swedien DS, Stamschror JD, Alvarez J, Luna F, Galván A, Bae YK, Wulfkuhle JD, Gallagher RI, Petricoin EF Rd, Norris B, Flory CM, Schumacher RJ, O'Sullivan MG, Cao Q, Chu H, Lipscomb JD, Atkins WM, Gupta K, Kelekar A, Blair IA, Capdevila JH, Falck JR, Sligar SG, Poulos TL, Georg GI, Ambrose E, Potter DA.

Cell Chem Biol. 2017 Oct 19;24(10):1314. doi: 10.1016/j.chembiol.2017.09.012. No abstract available.

16.

Structure-Activity Studies of N-Butyl-1-deoxynojirimycin (NB-DNJ) Analogues: Discovery of Potent and Selective Aminocyclopentitol Inhibitors of GBA1 and GBA2.

Gu X, Gupta V, Yang Y, Zhu JY, Carlson EJ, Kingsley C, Tash JS, Schönbrunn E, Hawkinson J, Georg GI.

ChemMedChem. 2017 Dec 7;12(23):1977-1984. doi: 10.1002/cmdc.201700558. Epub 2017 Nov 24.

17.

Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2).

Hawkinson JE, Sinville R, Mudaliar D, Shetty J, Ward T, Herr JC, Georg GI.

ChemMedChem. 2017 Nov 22;12(22):1857-1865. doi: 10.1002/cmdc.201700503. Epub 2017 Oct 20.

18.

Heme Binding Biguanides Target Cytochrome P450-Dependent Cancer Cell Mitochondria.

Guo Z, Sevrioukova IF, Denisov IG, Zhang X, Chiu TL, Thomas DG, Hanse EA, Cuellar RAD, Grinkova YV, Langenfeld VW, Swedien DS, Stamschror JD, Alvarez J, Luna F, Galván A, Bae YK, Wulfkuhle JD, Gallagher RI, Petricoin EF Rd, Norris B, Flory CM, Schumacher RJ, O'Sullivan MG, Cao Q, Chu H, Lipscomb JD, Atkins WM, Gupta K, Kelekar A, Blair IA, Capdevila JH, Falck JR, Sligar SG, Poulos TL, Georg GI, Ambrose E, Potter DA.

Cell Chem Biol. 2017 Oct 19;24(10):1259-1275.e6. doi: 10.1016/j.chembiol.2017.08.009. Epub 2017 Sep 14. Erratum in: Cell Chem Biol. 2017 Oct 19;24(10):1314.

19.

Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.

Zhu JY, Cuellar RA, Berndt N, Lee HE, Olesen SH, Martin MP, Jensen JT, Georg GI, Schönbrunn E.

J Med Chem. 2017 Sep 28;60(18):7863-7875. doi: 10.1021/acs.jmedchem.7b00996. Epub 2017 Sep 14.

20.

Correction to BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jul 27;60(14):6458. doi: 10.1021/acs.jmedchem.7b00943. Epub 2017 Jul 11. No abstract available.

PMID:
28696689
21.

BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jun 22;60(12):4805-4817. doi: 10.1021/acs.jmedchem.6b01336. Epub 2017 Jun 7. Erratum in: J Med Chem. 2017 Jul 27;60(14):6458.

22.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Med Chem Lett. 2017 Feb 28;8(4):379-382. doi: 10.1021/acsmedchemlett.7b00056. eCollection 2017 Apr 13. No abstract available.

23.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Cent Sci. 2017 Mar 22;3(3):143-147. doi: 10.1021/acscentsci.7b00069. Epub 2017 Feb 28. No abstract available.

24.

Current Medicinal Chemistry Research in India: Progress and Opportunities.

Georg GI, Wang S.

J Med Chem. 2017 Mar 9;60(5):1619. doi: 10.1021/acs.jmedchem.7b00317. No abstract available.

PMID:
28274124
25.

Synthesis and Cytotoxicity Evaluation of C4- and C5-Modified Analogues of the α,β-Unsaturated Lactone of Pironetin.

Huang DS, Wong HL, Georg GI.

ChemMedChem. 2017 Apr 6;12(7):520-528. doi: 10.1002/cmdc.201700084. Epub 2017 Mar 22.

26.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

J Med Chem. 2017 Mar 23;60(6):2165-2168. doi: 10.1021/acs.jmedchem.7b00229. Epub 2017 Feb 28. No abstract available.

PMID:
28244745
27.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

J Chem Inf Model. 2017 Mar 27;57(3):387-390. doi: 10.1021/acs.jcim.7b00105. Epub 2017 Feb 28. No abstract available.

PMID:
28244743
28.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

Biochemistry. 2017 Mar 14;56(10):1363-1366. doi: 10.1021/acs.biochem.7b00110. Epub 2017 Feb 28. No abstract available.

PMID:
28244742
29.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Chem Neurosci. 2017 Mar 15;8(3):420-423. doi: 10.1021/acschemneuro.7b00064. Epub 2017 Feb 28. No abstract available.

PMID:
28244737
30.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Chem Biol. 2017 Mar 17;12(3):575-578. doi: 10.1021/acschembio.7b00119. Epub 2017 Feb 28. No abstract available.

PMID:
28244728
31.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Infect Dis. 2017 Apr 14;3(4):259-262. doi: 10.1021/acsinfecdis.7b00023. Epub 2017 Feb 28. No abstract available.

PMID:
28244723
32.

Synthesis of Arylazide- and Diazirine-Containing CrAsH-EDT2 Photoaffinity Probes: Unfortunately, in the article.

Syeda SS, Rice D, Hook DJ, Heckert LL, Georg GI.

Arch Pharm (Weinheim). 2016 Jul;349(7):572. doi: 10.1002/ardp.201670022. No abstract available.

PMID:
27373873
33.

Chirally Pure Prodrugs and Their Converting Enzymes Lead to High Supersaturation and Rapid Transcellular Permeation of Benzodiazepines.

Kapoor M, Cheryala N, Rautiola D, Georg GI, Cloyd JC, Siegel RA.

J Pharm Sci. 2016 Aug;105(8):2365-71. doi: 10.1016/j.xphs.2016.05.011. Epub 2016 Jun 22.

PMID:
27342435
34.

Enantiospecific Synthesis and Cytotoxicity Evaluation of Oximidine II Analogues.

Schneider CM, Li W, Khownium K, Lushington GH, Georg GI.

ChemMedChem. 2016 Aug 5;11(15):1600-16. doi: 10.1002/cmdc.201600024. Epub 2016 May 31.

35.

Characterizing the Epothilone Binding Site on β-Tubulin by Photoaffinity Labeling: Identification of β-Tubulin Peptides TARGSQQY and TSRGSQQY as Targets of an Epothilone Photoprobe for Polymerized Tubulin.

Ranade AR, Higgins L, Markowski TW, Glaser N, Kashin D, Bai R, Hong KH, Hamel E, Höfle G, Georg GI.

J Med Chem. 2016 Apr 14;59(7):3499-514. doi: 10.1021/acs.jmedchem.6b00188. Epub 2016 Mar 17.

36.

Synthesis of Arylazide- and Diazirine-Containing CrAsH-EDT2 Photoaffinity Probes.

Syeda SS, Rice D, Hook DJ, Heckert LL, Georg GI.

Arch Pharm (Weinheim). 2016 Apr;349(4):233-41. doi: 10.1002/ardp.201500440. Epub 2016 Mar 7. Erratum in: Arch Pharm (Weinheim). 2016 Jul;349(7):572.

37.

Recombinant production of enzymatically active male contraceptive drug target hTSSK2 - Localization of the TSKS domain phosphorylated by TSSK2.

Shetty J, Sinville R, Shumilin IA, Minor W, Zhang J, Hawkinson JE, Georg GI, Flickinger CJ, Herr JC.

Protein Expr Purif. 2016 May;121:88-96. doi: 10.1016/j.pep.2016.01.009. Epub 2016 Jan 14.

38.

Human Adenine Nucleotide Translocase (ANT) Modulators Identified by High-Throughput Screening of Transgenic Yeast.

Zhang Y, Tian D, Matsuyama H, Hamazaki T, Shiratsuchi T, Terada N, Hook DJ, Walters MA, Georg GI, Hawkinson JE.

J Biomol Screen. 2016 Apr;21(4):381-90. doi: 10.1177/1087057115624637. Epub 2016 Jan 8.

39.

The Fungal Sexual Pheromone Sirenin Activates the Human CatSper Channel Complex.

Syeda SS, Carlson EJ, Miller MR, Francis R, Clapham DE, Lishko PV, Hawkinson JE, Hook D, Georg GI.

ACS Chem Biol. 2016 Feb 19;11(2):452-9. doi: 10.1021/acschembio.5b00748. Epub 2015 Dec 16.

41.

Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.

Patil S, Lis LG, Schumacher RJ, Norris BJ, Morgan ML, Cuellar RA, Blazar BR, Suryanarayanan R, Gurvich VJ, Georg GI.

J Med Chem. 2015 Dec 10;58(23):9334-44. doi: 10.1021/acs.jmedchem.5b01329. Epub 2015 Nov 24.

42.

Synthesis of Strained 1,3-Diene Macrocycles via Copper-Mediated Castro-Stephens Coupling/Alkyne Reduction Tandem Reactions.

Li W, Schneider CM, Georg GI.

Org Lett. 2015 Aug 7;17(15):3902-5. doi: 10.1021/acs.orglett.5b01892. Epub 2015 Jul 15.

PMID:
26176267
43.

Water-soluble benzodiazepine prodrug/enzyme combinations for intranasal rescue therapies.

Siegel RA, Kapoor M, Cheryala N, Georg GI, Cloyd JC.

Epilepsy Behav. 2015 Aug;49:347-50. doi: 10.1016/j.yebeh.2015.05.004. Epub 2015 Jun 24.

PMID:
26115606
44.

Reformulating Tylocrebrine in Epidermal Growth Factor Receptor Targeted Polymeric Nanoparticles Improves Its Therapeutic Index.

Kirtane AR, Wong HL, Guru BR, Lis LG, Georg GI, Gurvich VJ, Panyam J.

Mol Pharm. 2015 Aug 3;12(8):2912-23. doi: 10.1021/acs.molpharmaceut.5b00173. Epub 2015 Jul 3.

45.

Scalable syntheses of the BET bromodomain inhibitor JQ1.

Syeda SS, Jakkaraj S, Georg GI.

Tetrahedron Lett. 2015 Jun 3;56(23):3354-3457.

46.

A concise formal total synthesis of lactimidomycin.

Li W, Georg GI.

Chem Commun (Camb). 2015 May 21;51(41):8634-6. doi: 10.1039/c5cc02571k.

PMID:
25900419
47.

Stability of the human Hsp90-p50Cdc37 chaperone complex against nucleotides and Hsp90 inhibitors, and the influence of phosphorylation by casein kinase 2.

Olesen SH, Ingles DJ, Zhu JY, Martin MP, Betzi S, Georg GI, Tash JS, Schönbrunn E.

Molecules. 2015 Jan 19;20(1):1643-60. doi: 10.3390/molecules20011643.

48.
49.

Absolute quantitative (1)h NMR spectroscopy for compound purity determination.

Cushman M, Georg GI, Holzgrabe U, Wang S.

J Med Chem. 2014 Nov 26;57(22):9219. doi: 10.1021/jm501683w. Epub 2014 Nov 7. No abstract available.

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