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Items: 18

1.

The Next Step Forward in Ubiquitin-Specific Protease 7 Selective Inhibition.

Desroses M, Altun M.

Cell Chem Biol. 2017 Dec 21;24(12):1429-1431. doi: 10.1016/j.chembiol.2017.12.003.

PMID:
29272698
2.

Correction to Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors.

Llona-Minguez S, Höglund A, Ghassemian A, Desroses M, Calderón-Montaño JM, Burgos Morón E, Valerie NCK, Wiita E, Almlöf I, Koolmeister T, Mateus A, Cazares-Körner C, Sanjiv K, Homan E, Loseva O, Baranczewski P, Darabi M, Mehdizadeh A, Fayezi S, Jemth AS, Warpman Berglund U, Sigmundsson K, Lundbäck T, Jenmalm Jensen A, Artursson P, Scobie M, Helleday T.

J Med Chem. 2017 Sep 14;60(17):7614. doi: 10.1021/acs.jmedchem.7b01137. Epub 2017 Sep 1. No abstract available.

PMID:
28862438
3.

Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors.

Llona-Minguez S, Höglund A, Ghassemian A, Desroses M, Calderón-Montaño JM, Burgos Morón E, Valerie NCK, Wiita E, Almlöf I, Koolmeister T, Mateus A, Cazares-Körner C, Sanjiv K, Homan E, Loseva O, Baranczewski P, Darabi M, Mehdizadeh A, Fayezi S, Jemth AS, Warpman Berglund U, Sigmundsson K, Lundbäck T, Jenmalm Jensen A, Artursson P, Scobie M, Helleday T.

J Med Chem. 2017 May 25;60(10):4279-4292. doi: 10.1021/acs.jmedchem.7b00182. Epub 2017 May 16.

PMID:
28508636
4.

Corrigendum: MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool.

Gad H, Koolmeister T, Jemth AS, Eshtad S, Jacques SA, Ström CE, Svensson LM, Schultz N, Lundbäck T, Einarsdottir BO, Saleh A, Göktürk C, Baranczewski P, Svensson R, Berntsson RP, Gustafsson R, Strömberg K, Sanjiv K, Jacques-Cordonnier MC, Desroses M, Gustavsson AL, Olofsson R, Johansson F, Homan EJ, Loseva O, Bräutigam L, Johansson L, Höglund A, Hagenkort A, Pham T, Altun M, Gaugaz FZ, Vikingsson S, Evers B, Henriksson M, Vallin KSA, Wallner OA, Hammarström LGJ, Wiita E, Almlöf I, Kalderén C, Axelsson H, Djureinovic T, Carreras Puigvert J, Häggblad M, Jeppsson F, Martens U, Lundin C, Lundgren B, Granelli I, Jenmalm Jensen A, Artursson P, Nilsson JA, Stenmark P, Scobie M; Ulrika Warpman Berglund &Thomas Helleday.

Nature. 2017 Apr 26;544(7651):508. doi: 10.1038/nature22083. No abstract available.

PMID:
28447629
5.

dUTPase inhibition augments replication defects of 5-Fluorouracil.

Hagenkort A, Paulin CBJ, Desroses M, Sarno A, Wiita E, Mortusewicz O, Koolmeister T, Loseva O, Jemth AS, Almlöf I, Homan E, Lundbäck T, Gustavsson AL, Scobie M, Helleday T.

Oncotarget. 2017 Apr 4;8(14):23713-23726. doi: 10.18632/oncotarget.15785.

6.

Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2.

Wohlkönig A, Remaut H, Moune M, Tanina A, Meyer F, Desroses M, Steyaert J, Willand N, Baulard AR, Wintjens R.

Biochem Biophys Res Commun. 2017 May 27;487(2):403-408. doi: 10.1016/j.bbrc.2017.04.074. Epub 2017 Apr 14.

PMID:
28416386
7.

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420.

Blondiaux N, Moune M, Desroses M, Frita R, Flipo M, Mathys V, Soetaert K, Kiass M, Delorme V, Djaout K, Trebosc V, Kemmer C, Wintjens R, Wohlkönig A, Antoine R, Huot L, Hot D, Coscolla M, Feldmann J, Gagneux S, Locht C, Brodin P, Gitzinger M, Déprez B, Willand N, Baulard AR.

Science. 2017 Mar 17;355(6330):1206-1211. doi: 10.1126/science.aag1006. Epub 2017 Mar 16.

PMID:
28302858
8.

Crystal structure, biochemical and cellular activities demonstrate separate functions of MTH1 and MTH2.

Carter M, Jemth AS, Hagenkort A, Page BD, Gustafsson R, Griese JJ, Gad H, Valerie NC, Desroses M, Boström J, Warpman Berglund U, Helleday T, Stenmark P.

Nat Commun. 2015 Aug 4;6:7871. doi: 10.1038/ncomms8871.

9.

Vinylic MIDA Boronates: New Building Blocks for the Synthesis of Aza-Heterocycles.

Llona-Minguez S, Desroses M, Ghassemian A, Jacques SA, Eriksson L, Isacksson R, Koolmeister T, Stenmark P, Scobie M, Helleday T.

Chemistry. 2015 May 11;21(20):7394-8. doi: 10.1002/chem.201406549. Epub 2015 Mar 25.

PMID:
25809883
10.

MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool.

Gad H, Koolmeister T, Jemth AS, Eshtad S, Jacques SA, Ström CE, Svensson LM, Schultz N, Lundbäck T, Einarsdottir BO, Saleh A, Göktürk C, Baranczewski P, Svensson R, Berntsson RP, Gustafsson R, Strömberg K, Sanjiv K, Jacques-Cordonnier MC, Desroses M, Gustavsson AL, Olofsson R, Johansson F, Homan EJ, Loseva O, Bräutigam L, Johansson L, Höglund A, Hagenkort A, Pham T, Altun M, Gaugaz FZ, Vikingsson S, Evers B, Henriksson M, Vallin KS, Wallner OA, Hammarström LG, Wiita E, Almlöf I, Kalderén C, Axelsson H, Djureinovic T, Puigvert JC, Häggblad M, Jeppsson F, Martens U, Lundin C, Lundgren B, Granelli I, Jensen AJ, Artursson P, Nilsson JA, Stenmark P, Scobie M, Berglund UW, Helleday T.

Nature. 2014 Apr 10;508(7495):215-21. doi: 10.1038/nature13181. Epub 2014 Apr 2. Erratum in: Nature. 2017 Apr 26;544(7651):508.

PMID:
24695224
11.

DXR inhibition by potent mono- and disubstituted fosmidomycin analogues.

Jansson AM, Więckowska A, Björkelid C, Yahiaoui S, Sooriyaarachchi S, Lindh M, Bergfors T, Dharavath S, Desroses M, Suresh S, Andaloussi M, Nikhil R, Sreevalli S, Srinivasa BR, Larhed M, Jones TA, Karlén A, Mowbray SL.

J Med Chem. 2013 Aug 8;56(15):6190-9. doi: 10.1021/jm4006498. Epub 2013 Jul 17.

PMID:
23819803
12.

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis.

Flipo M, Willand N, Lecat-Guillet N, Hounsou C, Desroses M, Leroux F, Lens Z, Villeret V, Wohlkönig A, Wintjens R, Christophe T, Kyoung Jeon H, Locht C, Brodin P, Baulard AR, Déprez B.

J Med Chem. 2012 Jul 26;55(14):6391-402. doi: 10.1021/jm300377g. Epub 2012 Jul 17.

PMID:
22738293
13.

Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors.

Flipo M, Desroses M, Lecat-Guillet N, Villemagne B, Blondiaux N, Leroux F, Piveteau C, Mathys V, Flament MP, Siepmann J, Villeret V, Wohlkönig A, Wintjens R, Soror SH, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N.

J Med Chem. 2012 Jan 12;55(1):68-83. doi: 10.1021/jm200825u. Epub 2011 Dec 6.

PMID:
22098589
14.

Crystal structure of human MTH1 and the 8-oxo-dGMP product complex.

Svensson LM, Jemth AS, Desroses M, Loseva O, Helleday T, Högbom M, Stenmark P.

FEBS Lett. 2011 Aug 19;585(16):2617-21. doi: 10.1016/j.febslet.2011.07.017. Epub 2011 Jul 23.

15.

Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors.

Flipo M, Desroses M, Lecat-Guillet N, Dirié B, Carette X, Leroux F, Piveteau C, Demirkaya F, Lens Z, Rucktooa P, Villeret V, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N.

J Med Chem. 2011 Apr 28;54(8):2994-3010. doi: 10.1021/jm200076a. Epub 2011 Apr 1.

PMID:
21417236
16.

Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator.

Willand N, Desroses M, Toto P, Dirié B, Lens Z, Villeret V, Rucktooa P, Locht C, Baulard A, Deprez B.

ACS Chem Biol. 2010 Nov 19;5(11):1007-13. doi: 10.1021/cb100177g.

PMID:
20704273
17.

Synthetic EthR inhibitors boost antituberculous activity of ethionamide.

Willand N, Dirié B, Carette X, Bifani P, Singhal A, Desroses M, Leroux F, Willery E, Mathys V, Déprez-Poulain R, Delcroix G, Frénois F, Aumercier M, Locht C, Villeret V, Déprez B, Baulard AR.

Nat Med. 2009 May;15(5):537-44. doi: 10.1038/nm.1950. Epub 2009 May 3.

PMID:
19412174
18.

Derivatives of Iressa, a specific epidermal growth factor receptor inhibitor, are powerful apoptosis inducers in PC3 prostatic cancer cells.

Telliez A, Desroses M, Pommery N, Briand O, Farce A, Laconde G, Lemoine A, Depreux P, Hénichart JP.

ChemMedChem. 2007 Mar;2(3):318-32.

PMID:
17206733

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