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Items: 1 to 50 of 61

1.

The target landscape of clinical kinase drugs.

Klaeger S, Heinzlmeir S, Wilhelm M, Polzer H, Vick B, Koenig PA, Reinecke M, Ruprecht B, Petzoldt S, Meng C, Zecha J, Reiter K, Qiao H, Helm D, Koch H, Schoof M, Canevari G, Casale E, Depaolini SR, Feuchtinger A, Wu Z, Schmidt T, Rueckert L, Becker W, Huenges J, Garz AK, Gohlke BO, Zolg DP, Kayser G, Vooder T, Preissner R, Hahne H, Tõnisson N, Kramer K, Götze K, Bassermann F, Schlegl J, Ehrlich HC, Aiche S, Walch A, Greif PA, Schneider S, Felder ER, Ruland J, Médard G, Jeremias I, Spiekermann K, Kuster B.

Science. 2017 Dec 1;358(6367). pii: eaan4368. doi: 10.1126/science.aan4368.

PMID:
29191878
2.

Determination of plasticisers and BPA in Sicilian and Calabrian nectar honeys by selected ion monitoring GC/MS.

Lo Turco V, Di Bella G, Potortì AG, Tropea A, Casale EK, Fede MR, Dugo G.

Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2016 Nov;33(11):1693-1699. Epub 2016 Oct 11.

PMID:
27650776
3.

Characterization and origin of the 'B' and 'C' compounds in the acid/neutral forensic signatures of heroin - products from the acylation of porphyroxine and subsequent hydrolysis.

Casale JF, Casale ES, Toske SG, Hays PA, Panicker S.

Drug Test Anal. 2017 Mar;9(3):462-469. doi: 10.1002/dta.1922. Epub 2015 Nov 23.

PMID:
26593749
4.

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.

Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M, Fasolini M, Forte B, Galvani A, Isacchi A, Khvat A, Krasavin MY, Lupi R, Orsini P, Perego R, Pesenti E, Pezzetta D, Rainoldi S, Riccardi-Sirtori F, Scolaro A, Sola F, Zuccotto F, Felder ER, Donati D, Montagnoli A.

J Med Chem. 2015 Sep 10;58(17):6875-98. doi: 10.1021/acs.jmedchem.5b00680. Epub 2015 Aug 26.

PMID:
26222319
5.

Optimization of diarylthiazole B-raf inhibitors: identification of a compound endowed with high oral antitumor activity, mitigated hERG inhibition, and low paradoxical effect.

Pulici M, Traquandi G, Marchionni C, Modugno M, Lupi R, Amboldi N, Casale E, Colombo N, Corti L, Fasolini M, Gasparri F, Pastori W, Scolaro A, Donati D, Felder E, Galvani A, Isacchi A, Pesenti E, Ciomei M.

ChemMedChem. 2015 Feb;10(2):276-95. doi: 10.1002/cmdc.201402424. Epub 2014 Nov 27.

PMID:
25430902
6.

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.

Casale E, Amboldi N, Brasca MG, Caronni D, Colombo N, Dalvit C, Felder ER, Fogliatto G, Galvani A, Isacchi A, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Casuscelli F.

Bioorg Med Chem. 2014 Aug 1;22(15):4135-50. doi: 10.1016/j.bmc.2014.05.056. Epub 2014 Jun 14.

PMID:
24980703
7.

Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.

Casuscelli F, Ardini E, Avanzi N, Casale E, Cervi G, D'Anello M, Donati D, Faiardi D, Ferguson RD, Fogliatto G, Galvani A, Marsiglio A, Mirizzi DG, Montemartini M, Orrenius C, Papeo G, Piutti C, Salom B, Felder ER.

Bioorg Med Chem. 2013 Dec 1;21(23):7364-80. doi: 10.1016/j.bmc.2013.09.054. Epub 2013 Oct 2.

PMID:
24139169
8.

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).

Brasca MG, Mantegani S, Amboldi N, Bindi S, Caronni D, Casale E, Ceccarelli W, Colombo N, De Ponti A, Donati D, Ermoli A, Fachin G, Felder ER, Ferguson RD, Fiorelli C, Guanci M, Isacchi A, Pesenti E, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Fogliatto G.

Bioorg Med Chem. 2013 Nov 15;21(22):7047-63. doi: 10.1016/j.bmc.2013.09.018. Epub 2013 Sep 19. Erratum in: Bioorg Med Chem. 2014 Jan 1;22(1):662.

PMID:
24100158
9.

Structural insight into maternal embryonic leucine zipper kinase (MELK) conformation and inhibition toward structure-based drug design.

Canevari G, Re Depaolini S, Cucchi U, Bertrand JA, Casale E, Perrera C, Forte B, Carpinelli P, Felder ER.

Biochemistry. 2013 Sep 17;52(37):6380-7. doi: 10.1021/bi4005864. Epub 2013 Sep 4.

PMID:
23914841
10.

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death.

Magnaghi P, D'Alessio R, Valsasina B, Avanzi N, Rizzi S, Asa D, Gasparri F, Cozzi L, Cucchi U, Orrenius C, Polucci P, Ballinari D, Perrera C, Leone A, Cervi G, Casale E, Xiao Y, Wong C, Anderson DJ, Galvani A, Donati D, O'Brien T, Jackson PK, Isacchi A.

Nat Chem Biol. 2013 Sep;9(9):548-56. doi: 10.1038/nchembio.1313. Epub 2013 Jul 28.

PMID:
23892893
11.

NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.

Fogliatto G, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder E, Pesenti E, Galvani A, Mantegani S, Isacchi A.

Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14.

12.

PARP inhibitors in cancer therapy: an update.

Papeo G, Casale E, Montagnoli A, Cirla A.

Expert Opin Ther Pat. 2013 Apr;23(4):503-14. doi: 10.1517/13543776.2013.768615. Epub 2013 Feb 5. Review.

PMID:
23379721
13.

Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships.

Polucci P, Magnaghi P, Angiolini M, Asa D, Avanzi N, Badari A, Bertrand J, Casale E, Cauteruccio S, Cirla A, Cozzi L, Galvani A, Jackson PK, Liu Y, Magnuson S, Malgesini B, Nuvoloni S, Orrenius C, Sirtori FR, Riceputi L, Rizzi S, Trucchi B, O'Brien T, Isacchi A, Donati D, D'Alessio R.

J Med Chem. 2013 Jan 24;56(2):437-50. doi: 10.1021/jm3013213. Epub 2013 Jan 4.

PMID:
23245311
14.

Structure-based optimization of potent PDK1 inhibitors.

Angiolini M, Banfi P, Casale E, Casuscelli F, Fiorelli C, Saccardo MB, Silvagni M, Zuccotto F.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4095-9. doi: 10.1016/j.bmcl.2010.05.070. Epub 2010 Jun 8.

PMID:
20621725
15.

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M.

Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25.

PMID:
20153204
16.

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Traquandi G, Ciomei M, Ballinari D, Casale E, Colombo N, Croci V, Fiorentini F, Isacchi A, Longo A, Mercurio C, Panzeri A, Pastori W, Pevarello P, Volpi D, Roussel P, Vulpetti A, Brasca MG.

J Med Chem. 2010 Mar 11;53(5):2171-87. doi: 10.1021/jm901710h.

PMID:
20141146
17.

Through the "gatekeeper door": exploiting the active kinase conformation.

Zuccotto F, Ardini E, Casale E, Angiolini M.

J Med Chem. 2010 Apr 8;53(7):2681-94. doi: 10.1021/jm901443h. Review. No abstract available.

PMID:
20000735
18.

Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.

Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M.

J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559.

PMID:
19603809
19.

Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358.

Modugno M, Casale E, Soncini C, Rosettani P, Colombo R, Lupi R, Rusconi L, Fancelli D, Carpinelli P, Cameron AD, Isacchi A, Moll J.

Cancer Res. 2007 Sep 1;67(17):7987-90.

20.

Stable isotope analyses of heroin seized from the merchant vessel Pong Su.

Casale J, Casale E, Collins M, Morello D, Cathapermal S, Panicker S.

J Forensic Sci. 2006 May;51(3):603-6.

PMID:
16696708
21.

Chemical profiling of heroin recovered from the North Korean merchant vessel Pong Su.

Collins M, Casale E, Hibbert DB, Panicker S, Robertson J, Vujic S.

J Forensic Sci. 2006 May;51(3):597-602.

PMID:
16696707
22.

Neutral heroin impurities from tetrahydrobenzylisoquinoline alkaloids.

Toske SG, Cooper SD, Morello DR, Hays PA, Casale JF, Casale E.

J Forensic Sci. 2006 Mar;51(2):308-20.

PMID:
16566764
23.

Structure-based drug design to the discovery of new 2-aminothiazole CDK2 inhibitors.

Vulpetti A, Casale E, Roletto F, Amici R, Villa M, Pevarello P.

J Mol Graph Model. 2006 Mar;24(5):341-8. Epub 2005 Nov 2.

PMID:
16260160
24.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.

Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA.

J Med Chem. 2004 Jun 17;47(13):3367-80.

PMID:
15189033
25.

Dimer formation through domain swapping in the crystal structure of the Grb2-SH2-Ac-pYVNV complex.

Schiering N, Casale E, Caccia P, Giordano P, Battistini C.

Biochemistry. 2000 Nov 7;39(44):13376-82.

PMID:
11063574
26.

A placebo-controlled trial of lamotrigine add-on therapy for partial seizures in children. Lamictal Pediatric Partial Seizure Study Group.

Duchowny M, Pellock JM, Graf WD, Billard C, Gilman J, Casale E, Womble G, Risner M, Manasco P.

Neurology. 1999 Nov 10;53(8):1724-31.

PMID:
10563619
27.

Lamictal (lamotrigine) monotherapy for typical absence seizures in children.

Frank LM, Enlow T, Holmes GL, Manasco P, Concannon S, Chen C, Womble G, Casale EJ.

Epilepsia. 1999 Jul;40(7):973-9.

28.

Pharmacokinetics of lamotrigine in children in the absence of other antiepileptic drugs.

Chen C, Casale EJ, Duncan B, Culverhouse EH, Gilman J.

Pharmacotherapy. 1999 Apr;19(4):437-41.

PMID:
10212015
29.

Human alpha-thrombin inhibition by the active site titrant N alpha-(N,N-dimethylcarbamoyl)-alpha-azalysine p-nitrophenyl ester: a comparative kinetic and X-ray crystallographic study.

Nardini M, Pesce A, Rizzi M, Casale E, Ferraccioli R, Balliano G, Milla P, Ascenzi P, Bolognesi M.

J Mol Biol. 1996 May 24;258(5):851-9. Erratum in: J Mol Biol 1996 Oct 18;263(1):99.

PMID:
8637015
30.

[Primary intestinal lymphangiectasia in children. Report of 3 cases].

Diaz N, Khoury A, Taboada M, Isava I, Calderon A, Lopez C, Casale E, Romer H.

G E N. 1995 Oct-Dec;49(4):307-9. Spanish.

PMID:
8762662
31.

Comparison of the infusion requirements and recovery profiles of vecuronium and cisatracurium 51W89 in intensive care unit patients.

Prielipp RC, Coursin DB, Scuderi PE, Bowton DL, Ford SR, Cardenas VJ Jr, Vender J, Howard D, Casale EJ, Murray MJ.

Anesth Analg. 1995 Jul;81(1):3-12.

PMID:
7598277
32.
33.

Structural studies on the loggerhead sea turtle (Caretta caretta) myoglobin.

Petruzzelli R, Aureli G, Casale E, Nardini M, Rizzi M, Ascenzi P, Coletta M, De Sanctis G, Desideri A, Galtieri A, et al.

Biochem Mol Biol Int. 1993 Sep;31(1):19-24.

PMID:
8260943
34.

Physiological and morphological characteristics of spinal neurons projecting to the parabrachial region of the cat.

Light AR, Sedivec MJ, Casale EJ, Jones SL.

Somatosens Mot Res. 1993;10(3):309-25.

PMID:
8237218
35.

Serine proteinase inhibition by the cyclic thiolic compound YS3025: a crystallographic study.

Rizzi M, Casale E, Coda A, La Rosa C, Ascenzi P, Luisetti M, Bolognesi M.

Biochem Int. 1992 Nov;28(3):385-92.

PMID:
1482382
36.

Purification and Characterization of a Keratinase from a Feather-Degrading Bacillus licheniformis Strain.

Lin X, Lee CG, Casale ES, Shih JC.

Appl Environ Microbiol. 1992 Oct;58(10):3271-5.

37.

Structural study and preliminary crystallographic data for the hemoglobin from reindeer (Rangifer tarandus tarandus)

Conti E, Casale E, Ascenzi P, Coletta M, Condo SG, Merli A, Giardina B, Bordo D, Bolognesi M.

Biochem Biophys Res Commun. 1992 Sep 16;187(2):1063-70. Erratum in: Biochem Biophys Res Commun 1992 Dec 15;189(2):1253.

PMID:
1530603
38.

Structure of a human monoclonal antibody Fab fragment against gp41 of human immunodeficiency virus type 1.

He XM, Rüker F, Casale E, Carter DC.

Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):7154-8.

39.

Anti-IgG immobilized controlled-pore glass. Thionyl chloride-activated succinamidopropyl-glass as a covalent immobilization matrix.

Stabel TJ, Casale ES, Swaisgood HE, Horton HR.

Appl Biochem Biotechnol. 1992 Aug;36(2):87-96.

PMID:
1359836
40.

Immunocytochemical and scanning electron microscopic studies of atherosclerosis in Japanese quail.

Casale ES, Qureshi MA, Shih JC.

Poult Sci. 1992 Jan;71(1):141-50.

PMID:
1539014
41.

Crystallization and preliminary data for the ferric form of Lucina pectinata hemoglobin I.

Casale E, Lionetti C, Coda A, Merli A, Ascenzi P, Wittenberg JB, Bolognesi M.

J Mol Biol. 1991 Dec 5;222(3):447-9.

PMID:
1748987
43.

Crystallization of the Fab from a human monoclonal antibody against gp 41 of human immunodeficiency virus type I.

Casale E, Wenisch E, He XM, Righetti PG, Snyder RS, Jungbauer A, Tauer C, Ruker F, Carter DC.

J Mol Biol. 1990 Dec 5;216(3):511-2.

PMID:
2258926
44.

HydroLink gel electrophoresis (HLGE). I. Matrix characterization.

Righetti PG, Chiari M, Casale E, Chiesa C, Jain T, Shorr R.

J Biochem Biophys Methods. 1989 Jul;19(1):37-49.

PMID:
2809066
45.

Synthesis of buffers for generating immobilized pH gradients. I: Acidic acrylamido buffers.

Chiari M, Casale E, Santaniello E, Righetti PG.

Appl Theor Electrophor. 1989;1(2):99-102.

PMID:
2488594
46.

Oxidation of alkaline immobiline buffers for isoelectric focusing in immobilized pH gradients.

Righetti PG, Chiari M, Casale E, Chiesa C.

Appl Theor Electrophor. 1989;1(2):115-21.

PMID:
2488590
47.

Synthesis of buffers for generating immobilized pH gradients. II: Basic acrylamido buffers.

Chiari M, Casale E, Santaniello E, Righetti PG.

Appl Theor Electrophor. 1989;1(2):103-7.

PMID:
2488588
48.

Direct projection of the corticospinal tract to the superficial laminae of the spinal cord in the rat.

Casale EJ, Light AR, Rustioni A.

J Comp Neurol. 1988 Dec 8;278(2):275-86.

PMID:
3230165
49.

Parasitosis and mycosis of the central nervous system: 20 years of experience.

Krivoy A, Casale E, Valdivia RD, Silva V, Gonzalez A.

Childs Nerv Syst. 1988 Apr;4(2):76-8. No abstract available.

PMID:
3401874
50.

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