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Items: 1 to 50 of 130

1.

Autoregulation of Class II Alpha PI3K Activity by Its Lipid-Binding PX-C2 Domain Module.

Wang H, Lo WT, Vujičić Žagar A, Gulluni F, Lehmann M, Scapozza L, Haucke V, Vadas O.

Mol Cell. 2018 Jul 19;71(2):343-351.e4. doi: 10.1016/j.molcel.2018.06.042.

PMID:
30029007
2.

Targeting RNA structure in SMN2 reverses spinal muscular atrophy molecular phenotypes.

Garcia-Lopez A, Tessaro F, Jonker HRA, Wacker A, Richter C, Comte A, Berntenis N, Schmucki R, Hatje K, Petermann O, Chiriano G, Perozzo R, Sciarra D, Konieczny P, Faustino I, Fournet G, Orozco M, Artero R, Metzger F, Ebeling M, Goekjian P, Joseph B, Schwalbe H, Scapozza L.

Nat Commun. 2018 May 23;9(1):2032. doi: 10.1038/s41467-018-04110-1.

3.

Repurposing the Selective Oestrogen Receptor Modulator Tamoxifen for the Treatment of Duchenne Muscular Dystrophy.

Gayi E, Neff LA, Ismail HM, Ruegg UT, Scapozza L, Dorchies OM.

Chimia (Aarau). 2018 Apr 25;72(4):238-240. doi: 10.2533/chimia.2018.238.

PMID:
29720316
4.

Modeling and resistant alleles explain the selectivity of antimalarial compound 49c towards apicomplexan aspartyl proteases.

Mukherjee B, Tessaro F, Vahokoski J, Kursula I, Marq JB, Scapozza L, Soldati-Favre D.

EMBO J. 2018 Apr 3;37(7). pii: e98047. doi: 10.15252/embj.201798047. Epub 2018 Mar 8.

PMID:
29519896
5.

Antimycobacterial drug discovery using Mycobacteria-infected amoebae identifies anti-infectives and new molecular targets.

Trofimov V, Kicka S, Mucaria S, Hanna N, Ramon-Olayo F, Del Peral LV, Lelièvre J, Ballell L, Scapozza L, Besra GS, Cox JAG, Soldati T.

Sci Rep. 2018 Mar 2;8(1):3939. doi: 10.1038/s41598-018-22228-6.

6.

A Coincidence Detection Mechanism Controls PX-BAR Domain-Mediated Endocytic Membrane Remodeling via an Allosteric Structural Switch.

Lo WT, Vujičić Žagar A, Gerth F, Lehmann M, Puchkov D, Krylova O, Freund C, Scapozza L, Vadas O, Haucke V.

Dev Cell. 2017 Nov 20;43(4):522-529.e4. doi: 10.1016/j.devcel.2017.10.019.

PMID:
29161595
7.

A high yield optimized method for the production of acylated ACPs enabling the analysis of enzymes involved in P. falciparum fatty acid biosynthesis.

Lauciello L, Lack G, Scapozza L, Perozzo R.

Biochem Biophys Rep. 2016 Oct 6;8:310-317. doi: 10.1016/j.bbrep.2016.09.017. eCollection 2016 Dec.

8.

Inhibitors of Mycobacterium marinum virulence identified in a Dictyostelium discoideum host model.

Ouertatani-Sakouhi H, Kicka S, Chiriano G, Harrison CF, Hilbi H, Scapozza L, Soldati T, Cosson P.

PLoS One. 2017 Jul 20;12(7):e0181121. doi: 10.1371/journal.pone.0181121. eCollection 2017.

9.

Design and purification of active truncated phosphoinositide 3-kinase gamma protein constructs for structural studies.

Vujičić Žagar A, Scapozza L, Vadas O.

Protein Expr Purif. 2017 Jul;135:1-7. doi: 10.1016/j.pep.2017.04.011. Epub 2017 Apr 22.

PMID:
28442430
10.

Mammalian RAD52 Functions in Break-Induced Replication Repair of Collapsed DNA Replication Forks.

Sotiriou SK, Kamileri I, Lugli N, Evangelou K, Da-Ré C, Huber F, Padayachy L, Tardy S, Nicati NL, Barriot S, Ochs F, Lukas C, Lukas J, Gorgoulis VG, Scapozza L, Halazonetis TD.

Mol Cell. 2016 Dec 15;64(6):1127-1134. doi: 10.1016/j.molcel.2016.10.038.

11.

RET kinase inhibitors: a review of recent patents (2012-2015).

Mologni L, Gambacorti-Passerini C, Goekjian P, Scapozza L.

Expert Opin Ther Pat. 2017 Jan;27(1):91-99. Epub 2016 Sep 26. Review.

PMID:
27646564
12.

In Silico Driven Design and Synthesis of Rhodanine Derivatives as Novel Antibacterials Targeting the Enoyl Reductase InhA.

Slepikas L, Chiriano G, Perozzo R, Tardy S, Kranjc A, Patthey-Vuadens O, Ouertatani-Sakouhi H, Kicka S, Harrison CF, Scrignari T, Perron K, Hilbi H, Soldati T, Cosson P, Tarasevicius E, Scapozza L.

J Med Chem. 2016 Dec 22;59(24):10917-10928. doi: 10.1021/acs.jmedchem.5b01620. Epub 2016 Dec 9.

PMID:
26730986
13.

Caloric restriction induces energy-sparing alterations in skeletal muscle contraction, fiber composition and local thyroid hormone metabolism that persist during catch-up fat upon refeeding.

De Andrade PB, Neff LA, Strosova MK, Arsenijevic D, Patthey-Vuadens O, Scapozza L, Montani JP, Ruegg UT, Dulloo AG, Dorchies OM.

Front Physiol. 2015 Sep 16;6:254. doi: 10.3389/fphys.2015.00254. eCollection 2015.

14.

Efficacy study of two novel hyaluronic acid-based formulations for viscosupplementation therapy in an early osteoarthrosic rabbit model.

Kaderli S, Viguier E, Watrelot-Virieux D, Roger T, Gurny R, Scapozza L, Möller M, Boulocher C, Jordan O.

Eur J Pharm Biopharm. 2015 Oct;96:388-95. doi: 10.1016/j.ejpb.2015.09.005. Epub 2015 Sep 11.

PMID:
26369477
15.

Amoebae-Based Screening Reveals a Novel Family of Compounds Restricting Intracellular Legionella pneumophila.

Harrison CF, Chiriano G, Finsel I, Manske C, Hoffmann C, Steiner B, Kranjc A, Patthey-Vuadens O, Kicka S, Trofimov V, Ouertatani-Sakouhi H, Soldati T, Scapozza L, Hilbi H.

ACS Infect Dis. 2015 Jul 10;1(7):327-38. doi: 10.1021/acsinfecdis.5b00002. Epub 2015 May 16.

PMID:
27622823
16.

A subset of N-substituted phenothiazines inhibits NADPH oxidases.

Seredenina T, Chiriano G, Filippova A, Nayernia Z, Mahiout Z, Fioraso-Cartier L, Plastre O, Scapozza L, Krause KH, Jaquet V.

Free Radic Biol Med. 2015 Sep;86:239-49. doi: 10.1016/j.freeradbiomed.2015.05.023. Epub 2015 May 23.

PMID:
26013584
17.

A Bioorthogonal Chemical Reporter of Viral Infection.

Neef AB, Pernot L, Schreier VN, Scapozza L, Luedtke NW.

Angew Chem Int Ed Engl. 2015 Jun 26;54(27):7911-4. doi: 10.1002/anie.201500250. Epub 2015 May 14.

PMID:
25974835
18.

Adrenergic antagonists restrict replication of Legionella.

Harrison CF, Kicka S, Kranjc A, Finsel I, Chiriano G, Ouertatani-Sakouhi H, Soldati T, Scapozza L, Hilbi H.

Microbiology. 2015 Jul;161(7):1392-406. doi: 10.1099/mic.0.000094. Epub 2015 Apr 14.

PMID:
25873585
19.

NPM/ALK mutants resistant to ASP3026 display variable sensitivity to alternative ALK inhibitors but succumb to the novel compound PF-06463922.

Mologni L, Ceccon M, Pirola A, Chiriano G, Piazza R, Scapozza L, Gambacorti-Passerini C.

Oncotarget. 2015 Mar 20;6(8):5720-34.

20.

Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.

Seebacher W, Wolkinger V, Faist J, Kaiser M, Brun R, Saf R, Bucar F, Gröblacher B, Brantner A, Merino V, Kalia Y, Scapozza L, Perozzo R, Weis R.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1390-3. doi: 10.1016/j.bmcl.2015.02.044. Epub 2015 Feb 28.

PMID:
25746816
21.

A novel biocompatible hyaluronic acid-chitosan hybrid hydrogel for osteoarthrosis therapy.

Kaderli S, Boulocher C, Pillet E, Watrelot-Virieux D, Rougemont AL, Roger T, Viguier E, Gurny R, Scapozza L, Jordan O.

Int J Pharm. 2015 Apr 10;483(1-2):158-68. doi: 10.1016/j.ijpharm.2015.01.052. Epub 2015 Feb 7.

PMID:
25666331
22.

A novel oxido-viscosifying Hyaluronic Acid-antioxidant conjugate for osteoarthritis therapy: biocompatibility assessments.

Kaderli S, Boulocher C, Pillet E, Watrelot-Virieux D, Roger T, Viguier E, Gurny R, Scapozza L, Möller M.

Eur J Pharm Biopharm. 2015 Feb;90:70-9. doi: 10.1016/j.ejpb.2014.10.016. Epub 2014 Nov 11.

PMID:
25445302
23.

RNA interference screening identifies a novel role for PCTK1/CDK16 in medulloblastoma with c-Myc amplification.

Ćwiek P, Leni Z, Salm F, Dimitrova V, Styp-Rekowska B, Chiriano G, Carroll M, Höland K, Djonov V, Scapozza L, Guiry P, Arcaro A.

Oncotarget. 2015 Jan 1;6(1):116-29.

24.

Diapocynin, a dimer of the NADPH oxidase inhibitor apocynin, reduces ROS production and prevents force loss in eccentrically contracting dystrophic muscle.

Ismail HM, Scapozza L, Ruegg UT, Dorchies OM.

PLoS One. 2014 Oct 17;9(10):e110708. doi: 10.1371/journal.pone.0110708. eCollection 2014.

25.

Targeted cutaneous delivery of ciclosporin A using micellar nanocarriers and the possible role of inter-cluster regions as molecular transport pathways.

Lapteva M, Santer V, Mondon K, Patmanidis I, Chiriano G, Scapozza L, Gurny R, Möller M, Kalia YN.

J Control Release. 2014 Dec 28;196:9-18. doi: 10.1016/j.jconrel.2014.09.021. Epub 2014 Sep 30.

PMID:
25278258
26.

Virtual screening: an in silico tool for interlacing the chemical universe with the proteome.

Westermaier Y, Barril X, Scapozza L.

Methods. 2015 Jan;71:44-57. doi: 10.1016/j.ymeth.2014.08.001. Epub 2014 Sep 2.

PMID:
25193260
27.

Purine metabolite and energy charge analysis of Trypanosoma brucei cells in different growth phases using an optimized ion-pair RP-HPLC/UV for the quantification of adenine and guanine pools.

Graven P, Tambalo M, Scapozza L, Perozzo R.

Exp Parasitol. 2014 Jun;141:28-38. doi: 10.1016/j.exppara.2014.03.006. Epub 2014 Mar 19.

PMID:
24657574
28.

Synthesis of a non-peptidic PET tracer designed for α5β1 integrin receptor.

Monaco A, Michelin O, Prior J, Rüegg C, Scapozza L, Seimbille Y.

J Labelled Comp Radiopharm. 2014 May 15;57(5):365-70. doi: 10.1002/jlcr.3190. Epub 2014 Mar 14.

PMID:
24634266
29.

Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors.

Wang T, Bisson WH, Mäser P, Scapozza L, Picard D.

J Med Chem. 2014 Mar 27;57(6):2524-35. doi: 10.1021/jm401801t. Epub 2014 Mar 3.

PMID:
24580531
30.

Establishment and validation of whole-cell based fluorescence assays to identify anti-mycobacterial compounds using the Acanthamoeba castellanii-Mycobacterium marinum host-pathogen system.

Kicka S, Trofimov V, Harrison C, Ouertatani-Sakouhi H, McKinney J, Scapozza L, Hilbi H, Cosson P, Soldati T.

PLoS One. 2014 Jan 31;9(1):e87834. doi: 10.1371/journal.pone.0087834. eCollection 2014.

31.

Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors.

Tardy S, Orsato A, Mologni L, Bisson WH, Donadoni C, Gambacorti-Passerini C, Scapozza L, Gueyrard D, Goekjian PG.

Bioorg Med Chem. 2014 Feb 15;22(4):1303-12. doi: 10.1016/j.bmc.2014.01.007. Epub 2014 Jan 10.

PMID:
24468632
32.

Synthesis and in vitro evaluation of a novel radioligand for αvβ3 integrin receptor imaging: [18F]FPPA-c(RGDfK).

Monaco A, Zoete V, Alghisi GC, Rüegg C, Michelin O, Prior J, Scapozza L, Seimbille Y.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6068-72. doi: 10.1016/j.bmcl.2013.09.031. Epub 2013 Sep 19.

PMID:
24095096
33.

Design, synthesis, and biological and crystallographic evaluation of novel inhibitors of Plasmodium falciparum enoyl-ACP-reductase (PfFabI).

Belluti F, Perozzo R, Lauciello L, Colizzi F, Kostrewa D, Bisi A, Gobbi S, Rampa A, Bolognesi ML, Recanatini M, Brun R, Scapozza L, Cavalli A.

J Med Chem. 2013 Oct 10;56(19):7516-26. doi: 10.1021/jm400637m. Epub 2013 Sep 25.

PMID:
24063369
34.

Inhibition of iPLA2 β and of stretch-activated channels by doxorubicin alters dystrophic muscle function.

Ismail HM, Dorchies OM, Perozzo R, Strosova MK, Scapozza L, Ruegg UT.

Br J Pharmacol. 2013 Aug;169(7):1537-50. doi: 10.1111/bph.12188.

35.

Expression, purification and biochemical characterization of recombinant Ca-dependent protein kinase 2 of the malaria parasite Plasmodium falciparum.

Lauciello L, Kappes B, Scapozza L, Perozzo R.

Protein Expr Purif. 2013 Aug;90(2):170-7. doi: 10.1016/j.pep.2013.06.006. Epub 2013 Jun 18.

PMID:
23792132
36.

Identification of aggregation breakers for bevacizumab (Avastin®) self-association through similarity searching and interaction studies.

Westermaier Y, Veurink M, Riis-Johannessen T, Guinchard S, Gurny R, Scapozza L.

Eur J Pharm Biopharm. 2013 Nov;85(3 Pt A):773-80. doi: 10.1016/j.ejpb.2013.04.012. Epub 2013 May 9.

PMID:
23665445
37.

C-5 hydroxyethyl and hydroxypropyl acyclonucleosides as substrates for thymidine kinase of herpes simplex virus type 1 (HSV-1 TK): syntheses and biological evaluation.

Meščić A, Krištafor S, Novaković I, Osmanović A, Müller U, Završnik D, Ametamey SM, Scapozza L, Raić-Malić S.

Molecules. 2013 May 2;18(5):5104-24. doi: 10.3390/molecules18055104.

38.

RNA pentaloop structures as effective targets of regulators belonging to the RsmA/CsrA protein family.

Lapouge K, Perozzo R, Iwaszkiewicz J, Bertelli C, Zoete V, Michielin O, Scapozza L, Haas D.

RNA Biol. 2013 Jun;10(6):1031-41. doi: 10.4161/rna.24771. Epub 2013 Apr 23.

39.

Breaking the aggregation of the monoclonal antibody bevacizumab (avastin®) by dexamethasone phosphate: insights from molecular modelling and asymmetrical flow field-flow fractionation.

Veurink M, Westermaier Y, Gurny R, Scapozza L.

Pharm Res. 2013 Apr;30(4):1176-87. doi: 10.1007/s11095-012-0955-6. Epub 2013 Feb 15.

PMID:
23412914
40.

Naphthoquinone derivatives exert their antitrypanosomal activity via a multi-target mechanism.

Pieretti S, Haanstra JR, Mazet M, Perozzo R, Bergamini C, Prati F, Fato R, Lenaz G, Capranico G, Brun R, Bakker BM, Michels PA, Scapozza L, Bolognesi ML, Cavalli A.

PLoS Negl Trop Dis. 2013;7(1):e2012. doi: 10.1371/journal.pntd.0002012. Epub 2013 Jan 17.

41.

Synthesis and preclinical evaluation of a new C-6 alkylated pyrimidine derivative as a PET imaging agent for HSV1-tk gene expression.

Müller U, Ross TL, Ranadheera C, Slavik R, Müller A, Born M, Trauffer E, Sephton SM, Scapozza L, Krämer SD, Ametamey SM.

Am J Nucl Med Mol Imaging. 2013;3(1):71-84. Epub 2013 Jan 5.

42.

Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors.

Ceccon M, Mologni L, Bisson W, Scapozza L, Gambacorti-Passerini C.

Mol Cancer Res. 2013 Feb;11(2):122-32. doi: 10.1158/1541-7786.MCR-12-0569. Epub 2012 Dec 13.

43.

TTAS a new stilbene derivative that induces apoptosis in Leishmania infantum.

Tolomeo M, Roberti M, Scapozza L, Tarantelli C, Giacomini E, Titone L, Saporito L, Di Carlo P, Colomba C.

Exp Parasitol. 2013 Jan;133(1):37-43. doi: 10.1016/j.exppara.2012.10.006. Epub 2012 Oct 26.

PMID:
23103597
44.

The pharmaceutical biochemistry group: where pharmaceutical chemistry meets biology and drug delivery.

Kalia YN, Perozzo R, Scapozza L.

Chimia (Aarau). 2012;66(5):313-9. doi: 10.2533/chimia.2012.313. Review.

PMID:
22867543
45.

Validation of a novel molecular dynamics simulation approach for lipophilic drug incorporation into polymer micelles.

Kasimova AO, Pavan GM, Danani A, Mondon K, Cristiani A, Scapozza L, Gurny R, Möller M.

J Phys Chem B. 2012 Apr 12;116(14):4338-45. doi: 10.1021/jp2104819. Epub 2012 Apr 2.

PMID:
22435641
46.

The different flexibility of c-Src and c-Abl kinases regulates the accessibility of a druggable inactive conformation.

Lovera S, Sutto L, Boubeva R, Scapozza L, Dölker N, Gervasio FL.

J Am Chem Soc. 2012 Feb 8;134(5):2496-9. doi: 10.1021/ja210751t. Epub 2012 Jan 30.

PMID:
22280319
47.

A new N-methyl thymine derivative comprising a dihydroxyisobutenyl unit as ligand for thymidine kinase of herpes simplex virus type 1 (HSV-1 TK).

Krištafor S, Novaković I, Gazivoda Kraljević T, Kraljević Pavelić S, Lučin P, Westermaier Y, Pernot L, Scapozza L, Ametamey SM, Raić-Malić S.

Bioorg Med Chem Lett. 2011 Oct 15;21(20):6161-5. doi: 10.1016/j.bmcl.2011.07.115. Epub 2011 Aug 6.

PMID:
21911293
48.

Design, synthesis, and biological activity of urea derivatives as anaplastic lymphoma kinase inhibitors.

af Gennäs GB, Mologni L, Ahmed S, Rajaratnam M, Marin O, Lindholm N, Viltadi M, Gambacorti-Passerini C, Scapozza L, Yli-Kauhaluoma J.

ChemMedChem. 2011 Sep 5;6(9):1680-92. doi: 10.1002/cmdc.201100168. Epub 2011 Jun 30.

PMID:
21721129
49.

ClickMD: an intuitive web-oriented molecular dynamics platform.

Cristiani A, Brisotto N, Cedrati FC, Floris M, Scapozza L, Moro S.

Future Med Chem. 2011 Jun;3(8):923-31. doi: 10.4155/fmc.11.59.

PMID:
21707396
50.

Noninvasive transdermal iontophoretic delivery of biologically active human basic fibroblast growth factor.

Dubey S, Perozzo R, Scapozza L, Kalia YN.

Mol Pharm. 2011 Aug 1;8(4):1322-31. doi: 10.1021/mp200125j. Epub 2011 Jul 5.

PMID:
21696184

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