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Items: 22

1.

Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.

Heightman TD, Berdini V, Braithwaite H, Buck IM, Cassidy M, Castro J, Courtin A, Day JEH, East C, Fazal L, Graham B, Griffiths-Jones CM, Lyons JF, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Reader M, Rees DC, Rich SJ, Richardson C, Saini H, Thompson NT, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW.

J Med Chem. 2018 Jun 14;61(11):4978-4992. doi: 10.1021/acs.jmedchem.8b00421. Epub 2018 May 31.

PMID:
29775310
2.

Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).

Woolford AJ, Day PJ, Bénéton V, Berdini V, Coyle JE, Dudit Y, Grondin P, Huet P, Lee LY, Manas ES, McMenamin RL, Murray CW, Page LW, Patel VK, Potvain F, Rich SJ, Sang Y, Somers DO, Trottet L, Wan Z, Zhang X.

J Med Chem. 2016 Dec 8;59(23):10738-10749. Epub 2016 Nov 18.

PMID:
27933945
3.

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
4.

Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X-ray Fragment Screening.

Woolford AJ, Pero JE, Aravapalli S, Berdini V, Coyle JE, Day PJ, Dodson AM, Grondin P, Holding FP, Lee LY, Li P, Manas ES, Marino J Jr, Martin AC, McCleland BW, McMenamin RL, Murray CW, Neipp CE, Page LW, Patel VK, Potvain F, Rich S, Rivero RA, Smith K, Somers DO, Trottet L, Velagaleti R, Williams G, Xie R.

J Med Chem. 2016 Jun 9;59(11):5356-67. doi: 10.1021/acs.jmedchem.6b00212. Epub 2016 May 20.

PMID:
27167608
5.

Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.

Murray CW, Berdini V, Buck IM, Carr ME, Cleasby A, Coyle JE, Curry JE, Day JE, Day PJ, Hearn K, Iqbal A, Lee LY, Martins V, Mortenson PN, Munck JM, Page LW, Patel S, Roomans S, Smith K, Tamanini E, Saxty G.

ACS Med Chem Lett. 2015 Jun 4;6(7):798-803. doi: 10.1021/acsmedchemlett.5b00143. eCollection 2015 Jul 9.

6.

Perspective on computational and structural aspects of kinase discovery from IPK2014.

Martin E, Knapp S, Engh RA, Moebitz H, Varin T, Roux B, Meiler J, Berdini V, Baumann A, Vieth M.

Biochim Biophys Acta. 2015 Oct;1854(10 Pt B):1595-604. doi: 10.1016/j.bbapap.2015.03.014. Epub 2015 Apr 7. Review.

7.

Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.

Johnson CN, Adelinet C, Berdini V, Beke L, Bonnet P, Brehmer D, Calo F, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, Mevellec L, McMenamin R, Pasquier E, Patel S, Rees DC, Linders JT.

ACS Med Chem Lett. 2014 May 23;6(1):31-6. doi: 10.1021/ml5001273. eCollection 2015 Jan 8.

8.

Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.

Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, McMenamin R, Patel S, Rees DC, Sharff A, Sommen F, Wu T, Linders JT.

ACS Med Chem Lett. 2014 May 23;6(1):25-30. doi: 10.1021/ml5001245. eCollection 2015 Jan 8.

9.

Fragment-based approaches to the discovery of kinase inhibitors.

Mortenson PN, Berdini V, O'Reilly M.

Methods Enzymol. 2014;548:69-92. doi: 10.1016/B978-0-12-397918-6.00003-3. Review.

PMID:
25399642
10.

Crystal structure of human soluble adenylate cyclase reveals a distinct, highly flexible allosteric bicarbonate binding pocket.

Saalau-Bethell SM, Berdini V, Cleasby A, Congreve M, Coyle JE, Lock V, Murray CW, O'Brien MA, Rich SJ, Sambrook T, Vinkovic M, Yon JR, Jhoti H.

ChemMedChem. 2014 Apr;9(4):823-32. doi: 10.1002/cmdc.201300480. Epub 2014 Feb 24.

11.

Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.

Squires M, Ward G, Saxty G, Berdini V, Cleasby A, King P, Angibaud P, Perera T, Fazal L, Ross D, Jones CG, Madin A, Benning RK, Vickerstaffe E, O'Brien A, Frederickson M, Reader M, Hamlett C, Batey MA, Rich S, Carr M, Miller D, Feltell R, Thiru A, Bethell S, Devine LA, Graham BL, Pike A, Cosme J, Lewis EJ, Freyne E, Lyons J, Irving J, Murray C, Newell DR, Thompson NT.

Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15.

12.

Crystal structure of Schistosoma purine nucleoside phosphorylase complexed with a novel monocyclic inhibitor.

Pereira HM, Berdini V, Ferri MR, Cleasby A, Garratt RC.

Acta Trop. 2010 May;114(2):97-102. doi: 10.1016/j.actatropica.2010.01.010. Epub 2010 Feb 1.

PMID:
20122887
13.

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.

Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL, Heathcote M, Maman S, Matthews JE, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Rees DC, Reule M, Tisi D, Williams G, Vinković M, Wyatt PG.

J Med Chem. 2009 Jan 22;52(2):379-88. doi: 10.1021/jm800984v.

PMID:
19143567
14.

Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.

Wyatt PG, Woodhead AJ, Berdini V, Boulstridge JA, Carr MG, Cross DM, Davis DJ, Devine LA, Early TR, Feltell RE, Lewis EJ, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Reule M, Saxty G, Seavers LC, Smith DM, Squires MS, Trewartha G, Walker MT, Woolford AJ.

J Med Chem. 2008 Aug 28;51(16):4986-99. doi: 10.1021/jm800382h. Epub 2008 Jul 26.

PMID:
18656911
15.

Crystal structure of calf spleen purine nucleoside phosphorylase complexed to a novel purine analogue.

Pereira HM, Berdini V, Cleasby A, Garratt RC.

FEBS Lett. 2007 Oct 30;581(26):5082-6. Epub 2007 Oct 2.

16.

Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.

Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I.

J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24.

PMID:
17451235
17.

Identification of inhibitors of protein kinase B using fragment-based lead discovery.

Saxty G, Woodhead SJ, Berdini V, Davies TG, Verdonk ML, Wyatt PG, Boyle RG, Barford D, Downham R, Garrett MD, Carr RA.

J Med Chem. 2007 May 17;50(10):2293-6. Epub 2007 Apr 24.

PMID:
17451234
18.

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.

Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, Workman P, McDonald E.

Bioorg Med Chem. 2006 Feb 15;14(4):1255-73. Epub 2005 Oct 24.

PMID:
16249095
19.

2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.

Allegretti M, Bertini R, Cesta MC, Bizzarri C, Di Bitondo R, Di Cioccio V, Galliera E, Berdini V, Topai A, Zampella G, Russo V, Di Bello N, Nano G, Nicolini L, Locati M, Fantucci P, Florio S, Colotta F.

J Med Chem. 2005 Jun 30;48(13):4312-31.

PMID:
15974585
20.

Virtual screening using protein-ligand docking: avoiding artificial enrichment.

Verdonk ML, Berdini V, Hartshorn MJ, Mooij WT, Murray CW, Taylor RD, Watson P.

J Chem Inf Comput Sci. 2004 May-Jun;44(3):793-806.

PMID:
15154744
21.

Carbocysteine lysine salt monohydrate (SCMC-LYS) is a selective scavenger of reactive oxygen intermediates (ROIs).

Brandolini L, Allegretti M, Berdini V, Cervellera MN, Mascagni P, Rinaldi M, Melillo G, Ghezzi P, Mengozzi M, Bertini R.

Eur Cytokine Netw. 2003 Jan-Mar;14(1):20-6.

22.

Canalicular cholestasis due to amiodarone toxicity. A definite diagnosis obtained by electron microscopy.

Macarri G, Feliciangeli G, Berdini V, Jezequel AM, Benedetti A.

Ital J Gastroenterol. 1995 Oct-Nov;27(8):436-8. Review.

PMID:
8775470

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