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Items: 24

1.

Observing an antisense drug complex in intact human cells by in-cell NMR.

Schlagnitweit J, Friebe Sandoz S, Jaworski A, Guzzetti I, Aussenac F, Carbajo RJ, Chiarparin E, Pell AJ, Petzold K.

Chembiochem. 2019 Jun 17. doi: 10.1002/cbic.201900297. [Epub ahead of print]

PMID:
31206961
2.

Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.

Heightman TD, Callahan JF, Chiarparin E, Coyle JE, Griffiths-Jones C, Lakdawala AS, McMenamin R, Mortenson PN, Norton D, Peakman TM, Rich SJ, Richardson C, Rumsey WL, Sanchez Y, Saxty G, Willems HMG, Wolfe L 3rd, Woolford AJ, Wu Z, Yan H, Kerns JK, Davies TG.

J Med Chem. 2019 May 9;62(9):4683-4702. doi: 10.1021/acs.jmedchem.9b00279. Epub 2019 Apr 25.

PMID:
30973731
3.

Differential uptake, kinetics and mechanisms of intracellular trafficking of next-generation antisense oligonucleotides across human cancer cell lines.

Linnane E, Davey P, Zhang P, Puri S, Edbrooke M, Chiarparin E, Revenko AS, Macleod AR, Norman JC, Ross SJ.

Nucleic Acids Res. 2019 May 21;47(9):4375-4392. doi: 10.1093/nar/gkz214.

4.

A New Straightforward Method for Lipophilicity (logP) Measurement using 19F NMR Spectroscopy.

Wang Z, Jeffries BF, Felstead HR, Wells NJ, Chiarparin E, Linclau B.

J Vis Exp. 2019 Jan 30;(143). doi: 10.3791/58567.

PMID:
30774129
5.

Experimental free ligand conformations: a missing link in structure-based drug discovery.

Chiarparin E, Packer MJ, Wilson DM.

Future Med Chem. 2019 Jan;11(2):79-82. doi: 10.4155/fmc-2018-0339. Epub 2019 Jan 16. No abstract available.

6.

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.

Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD, Gregory GP, Hargreaves D, Hendricks JA, Johannes JW, Johnstone RW, Kazmirski SL, Kettle JG, Lamb ML, Matulis SM, Nooka AK, Packer MJ, Peng B, Rawlins PB, Robbins DW, Schuller AG, Su N, Yang W, Ye Q, Zheng X, Secrist JP, Clark EA, Wilson DM, Fawell SE, Hird AW.

Nat Commun. 2018 Dec 17;9(1):5341. doi: 10.1038/s41467-018-07551-w.

7.

Reducing the Lipophilicity of Perfluoroalkyl Groups by CF2-F/CF2-Me or CF3/CH3 Exchange.

Jeffries B, Wang Z, Graton J, Holland SD, Brind T, Greenwood RDR, Le Questel JY, Scott JS, Chiarparin E, Linclau B.

J Med Chem. 2018 Dec 13;61(23):10602-10618. doi: 10.1021/acs.jmedchem.8b01222. Epub 2018 Nov 28.

PMID:
30411895
8.

Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.

McCoull W, Cheung T, Anderson E, Barton P, Burgess J, Byth K, Cao Q, Castaldi MP, Chen H, Chiarparin E, Carbajo RJ, Code E, Cowan S, Davey PR, Ferguson AD, Fillery S, Fuller NO, Gao N, Hargreaves D, Howard MR, Hu J, Kawatkar A, Kemmitt PD, Leo E, Molina DM, O'Connell N, Petteruti P, Rasmusson T, Raubo P, Rawlins PB, Ricchiuto P, Robb GR, Schenone M, Waring MJ, Zinda M, Fawell S, Wilson DM.

ACS Chem Biol. 2018 Nov 16;13(11):3131-3141. doi: 10.1021/acschembio.8b00698. Epub 2018 Oct 17.

PMID:
30335946
9.

A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).

Johnson CN, Ahn JS, Buck IM, Chiarparin E, Day JEH, Hopkins A, Howard S, Lewis EJ, Martins V, Millemaggi A, Munck JM, Page LW, Peakman T, Reader M, Rich SJ, Saxty G, Smyth T, Thompson NT, Ward GA, Williams PA, Wilsher NE, Chessari G.

J Med Chem. 2018 Aug 23;61(16):7314-7329. doi: 10.1021/acs.jmedchem.8b00900. Epub 2018 Aug 9.

PMID:
30091600
10.

Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).

Tamanini E, Buck IM, Chessari G, Chiarparin E, Day JEH, Frederickson M, Griffiths-Jones CM, Hearn K, Heightman TD, Iqbal A, Johnson CN, Lewis EJ, Martins V, Peakman T, Reader M, Rich SJ, Ward GA, Williams PA, Wilsher NE.

J Med Chem. 2017 Jun 8;60(11):4611-4625. doi: 10.1021/acs.jmedchem.6b01877. Epub 2017 May 24.

PMID:
28492317
11.

Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.

Tisi D, Chiarparin E, Tamanini E, Pathuri P, Coyle JE, Hold A, Holding FP, Amin N, Martin AC, Rich SJ, Berdini V, Yon J, Acklam P, Burke R, Drouin L, Harmer JE, Jeganathan F, van Montfort RL, Newbatt Y, Tortorici M, Westlake M, Wood A, Hoelder S, Heightman TD.

ACS Chem Biol. 2016 Nov 18;11(11):3093-3105. Epub 2016 Sep 27.

PMID:
27571355
12.

NMR backbone resonance assignment and solution secondary structure determination of human NSD1 and NSD2.

Amin N, Nietlispach D, Qamar S, Coyle J, Chiarparin E, Williams G.

Biomol NMR Assign. 2016 Oct;10(2):315-20. doi: 10.1007/s12104-016-9691-x. Epub 2016 Jun 29.

PMID:
27356987
13.

1H, 15N and 13C backbone assignments of GDP-bound human H-Ras mutant G12V.

Amin N, Chiarparin E, Coyle J, Nietlispach D, Williams G.

Biomol NMR Assign. 2016 Apr;10(1):121-3. doi: 10.1007/s12104-015-9649-4. Epub 2015 Sep 15.

PMID:
26373425
14.

Exploring weak ligand-protein interactions by long-lived NMR states: improved contrast in fragment-based drug screening.

Buratto R, Mammoli D, Chiarparin E, Williams G, Bodenhausen G.

Angew Chem Int Ed Engl. 2014 Oct 13;53(42):11376-80. doi: 10.1002/anie.201404921. Epub 2014 Sep 4.

15.

Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.

Howard S, Amin N, Benowitz AB, Chiarparin E, Cui H, Deng X, Heightman TD, Holmes DJ, Hopkins A, Huang J, Jin Q, Kreatsoulas C, Martin AC, Massey F, McCloskey L, Mortenson PN, Pathuri P, Tisi D, Williams PA.

ACS Med Chem Lett. 2013 Oct 18;4(12):1208-12. doi: 10.1021/ml4003277. eCollection 2013 Dec 12.

16.

In vitro measurement of drug efficiency index to aid early lead optimization.

Valko K, Chiarparin E, Nunhuck S, Montanari D.

J Pharm Sci. 2012 Nov;101(11):4155-69. doi: 10.1002/jps.23305. Epub 2012 Aug 28.

PMID:
22930396
17.

Application of drug efficiency index in drug discovery: a strategy towards low therapeutic dose.

Montanari D, Chiarparin E, Gleeson MP, Braggio S, Longhi R, Valko K, Rossi T.

Expert Opin Drug Discov. 2011 Sep;6(9):913-20. doi: 10.1517/17460441.2011.602968. Epub 2011 Jul 22.

PMID:
22646214
18.

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.

Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30.

PMID:
21831639
19.

Measurement of long-range cross-correlation rates using a combination of single- and multiple-quantum NMR spectroscopy in one experiment.

Fruh D, Chiarparin E, Pelupessy P, Bodenhausen G.

J Am Chem Soc. 2002 Apr 17;124(15):4050-7.

PMID:
11942843
20.

Hydrogen bonds in RNA base pairs investigated by cross-correlated relaxation of multiple-quantum coherence in NMR.

Chiarparin E, RĂ¼disser S, Bodenhausen G.

Chemphyschem. 2001 Jan 19;2(1):41-5. doi: 10.1002/1439-7641(20010119)2:1<41::AID-CPHC41>3.0.CO;2-H. No abstract available.

PMID:
23696380
21.

Measurement of relaxation rates of N(H) and H(alpha) backbone protons in proteins with tailored initial conditions.

Millet O, Chiarparin E, Pelupessy P, Pons M, Bodenhausen G.

J Magn Reson. 1999 Aug;139(2):434-8.

PMID:
10423382
22.

Efficient determination of angles subtended by C(alpha)-H(alpha) and N-H(N) vectors in proteins via dipole-dipole cross-correlation.

Pelupessy P, Chiarparin E, Ghose R, Bodenhausen G.

J Biomol NMR. 1999 Apr;13(4):375-80.

PMID:
10383199
23.

Excitation of selected proton signals in NMR of isotopically labeled macromolecules

Pelupessy P, Chiarparin E, Bodenhausen G.

J Magn Reson. 1999 May;138(1):178-81.

PMID:
10329243
24.

Normalized one-dimensional NOE measurements in isotopically labeled macromolecules using two-way cross-polarization.

Chiarparin E, Pelupessy P, Cutting B, Eykyn TR, Bodenhausen G.

J Biomol NMR. 1999 Jan;13(1):61-5. doi: 10.1023/A:1008307012647.

PMID:
21080263

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