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Fast NMR Methods for Measuring in the Direct and/or Competition Mode the Dissociation Constants of Chemical Fragments Interacting with a Receptor.

Dalvit C, Parent A, Vallée F, Mathieu M, Rak A.

ChemMedChem. 2019 Jun 5;14(11):1115-1127. doi: 10.1002/cmdc.201900152. Epub 2019 May 14.


Estimation of Drug-Target Residence Times by τ-Random Acceleration Molecular Dynamics Simulations.

Kokh DB, Amaral M, Bomke J, Grädler U, Musil D, Buchstaller HP, Dreyer MK, Frech M, Lowinski M, Vallee F, Bianciotto M, Rak A, Wade RC.

J Chem Theory Comput. 2018 Jul 10;14(7):3859-3869. doi: 10.1021/acs.jctc.8b00230. Epub 2018 Jun 4.


Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844).

Ugolini A, Kenigsberg M, Rak A, Vallée F, Houtmann J, Lowinski M, Capdevila C, Khider J, Albert E, Martinet N, Nemecek C, Grapinet S, Bacqué E, Roesner M, Delaisi C, Calvet L, Bonche F, Semiond D, Egile C, Goulaouic H, Schio L.

J Med Chem. 2016 Aug 11;59(15):7066-74. doi: 10.1021/acs.jmedchem.6b00280. Epub 2016 Jul 13.


CODV-Ig, a universal bispecific tetravalent and multifunctional immunoglobulin format for medical applications.

Steinmetz A, Vallée F, Beil C, Lange C, Baurin N, Beninga J, Capdevila C, Corvey C, Dupuy A, Ferrari P, Rak A, Wonerow P, Kruip J, Mikol V, Rao E.

MAbs. 2016 Jul;8(5):867-78. doi: 10.1080/19420862.2016.1162932. Epub 2016 Mar 16.


An Automated Microscale Thermophoresis Screening Approach for Fragment-Based Lead Discovery.

Linke P, Amaning K, Maschberger M, Vallee F, Steier V, Baaske P, Duhr S, Breitsprecher D, Rak A.

J Biomol Screen. 2016 Apr;21(4):414-21. doi: 10.1177/1087057115618347. Epub 2015 Dec 2.


Selective blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs learning and memory performance while producing antinociceptive activity in rodents.

Griebel G, Pichat P, Beeské S, Leroy T, Redon N, Jacquet A, Françon D, Bert L, Even L, Lopez-Grancha M, Tolstykh T, Sun F, Yu Q, Brittain S, Arlt H, He T, Zhang B, Wiederschain D, Bertrand T, Houtmann J, Rak A, Vallée F, Michot N, Augé F, Menet V, Bergis OE, George P, Avenet P, Mikol V, Didier M, Escoubet J.

Sci Rep. 2015 Jan 6;5:7642. doi: 10.1038/srep07642.


Selective inhibition of mutant isocitrate dehydrogenase 1 (IDH1) via disruption of a metal binding network by an allosteric small molecule.

Deng G, Shen J, Yin M, McManus J, Mathieu M, Gee P, He T, Shi C, Bedel O, McLean LR, Le-Strat F, Zhang Y, Marquette JP, Gao Q, Zhang B, Rak A, Hoffmann D, Rooney E, Vassort A, Englaro W, Li Y, Patel V, Adrian F, Gross S, Wiederschain D, Cheng H, Licht S.

J Biol Chem. 2015 Jan 9;290(2):762-74. doi: 10.1074/jbc.M114.608497. Epub 2014 Nov 12.


Structures of a pan-specific antagonist antibody complexed to different isoforms of TGFβ reveal structural plasticity of antibody-antigen interactions.

Moulin A, Mathieu M, Lawrence C, Bigelow R, Levine M, Hamel C, Marquette JP, Le Parc J, Loux C, Ferrari P, Capdevila C, Dumas J, Dumas B, Rak A, Bird J, Qiu H, Pan CQ, Edmunds T, Wei RR.

Protein Sci. 2014 Dec;23(12):1698-707. doi: 10.1002/pro.2548. Epub 2014 Sep 26.


Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.

Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L.

J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15.


The use of virtual screening and differential scanning fluorimetry for the rapid identification of fragments active against MEK1.

Amaning K, Lowinski M, Vallee F, Steier V, Marcireau C, Ugolini A, Delorme C, Foucalt F, McCort G, Derimay N, Andouche C, Vougier S, Llopart S, Halland N, Rak A.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3620-6. doi: 10.1016/j.bmcl.2013.04.003. Epub 2013 Apr 10.


Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.

Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Abecassis PY, Lejeune P, Vincent L, Bonnevaux H, Nicolas JP, Bertrand T, Marquette JP, Michot N, Benard T, Below P, Vade I, Chatreaux F, Lebourg G, Pilorge F, Angouillant-Boniface O, Louboutin A, Lengauer C, Schio L.

J Med Chem. 2012 May 24;55(10):4788-805. doi: 10.1021/jm300241b. Epub 2012 May 2.


Armus is a Rac1 effector that inactivates Rab7 and regulates E-cadherin degradation.

Frasa MA, Maximiano FC, Smolarczyk K, Francis RE, Betson ME, Lozano E, Goldenring J, Seabra MC, Rak A, Ahmadian MR, Braga VM.

Curr Biol. 2010 Feb 9;20(3):198-208. doi: 10.1016/j.cub.2009.12.053. Epub 2010 Jan 28.


The human formin FHOD1 contains a bipartite structure of FH3 and GTPase-binding domains required for activation.

Schulte A, Stolp B, Schönichen A, Pylypenko O, Rak A, Fackler OT, Geyer M.

Structure. 2008 Sep 10;16(9):1313-23. doi: 10.1016/j.str.2008.06.008.


Flow cytometry for real-time measurement of guanine nucleotide binding and exchange by Ras-like GTPases.

Schwartz SL, Tessema M, Buranda T, Pylypenko O, Rak A, Simons PC, Surviladze Z, Sklar LA, Wandinger-Ness A.

Anal Biochem. 2008 Oct 15;381(2):258-66. doi: 10.1016/j.ab.2008.06.039. Epub 2008 Jul 8.


Extreme temperature tolerance of a hyperthermophilic protein coupled to residual structure in the unfolded state.

Wallgren M, Adén J, Pylypenko O, Mikaelsson T, Johansson LB, Rak A, Wolf-Watz M.

J Mol Biol. 2008 Jun 13;379(4):845-58. doi: 10.1016/j.jmb.2008.04.007. Epub 2008 Apr 8.


A structural model of the GDP dissociation inhibitor rab membrane extraction mechanism.

Ignatev A, Kravchenko S, Rak A, Goody RS, Pylypenko O.

J Biol Chem. 2008 Jun 27;283(26):18377-84. doi: 10.1074/jbc.M709718200. Epub 2008 Apr 20.


Farnesylation of the SNARE protein Ykt6 increases its stability and helical folding.

Pylypenko O, Schönichen A, Ludwig D, Ungermann C, Goody RS, Rak A, Geyer M.

J Mol Biol. 2008 Apr 11;377(5):1334-45. doi: 10.1016/j.jmb.2008.01.099. Epub 2008 Feb 13.


A combinatorial approach to crystallization of PX-BAR unit of the human Sorting Nexin 9.

Pylypenko O, Ignatev A, Lundmark R, Rasmuson E, Carlsson SR, Rak A.

J Struct Biol. 2008 May;162(2):356-60. Epub 2007 Nov 1.


Rab GTPases at a glance.

Schwartz SL, Cao C, Pylypenko O, Rak A, Wandinger-Ness A.

J Cell Sci. 2007 Nov 15;120(Pt 22):3905-10. No abstract available. Erratum in: J Cell Sci. 2008 Jan 15;121(Pt 2):246.


The PX-BAR membrane-remodeling unit of sorting nexin 9.

Pylypenko O, Lundmark R, Rasmuson E, Carlsson SR, Rak A.

EMBO J. 2007 Nov 14;26(22):4788-800. Epub 2007 Oct 18.

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