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Items: 23

1.

Computationally Empowered Workflow Identifies Novel Covalent Allosteric Binders for KRASG12C.

Mortier J, Friberg A, Badock V, Moosmayer D, Schroeder J, Steigemann P, Siegel F, Gradl S, Bauser M, Hillig RC, Briem H, Eis K, Bader B, Nguyen D, Christ CD.

ChemMedChem. 2020 Apr 1. doi: 10.1002/cmdc.201900727. [Epub ahead of print]

PMID:
32237114
2.

The novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies.

Christian S, Merz C, Evans L, Gradl S, Seidel H, Friberg A, Eheim A, Lejeune P, Brzezinka K, Zimmermann K, Ferrara S, Meyer H, Lesche R, Stoeckigt D, Bauser M, Haegebarth A, Sykes DB, Scadden DT, Losman JA, Janzer A.

Leukemia. 2019 Oct;33(10):2403-2415. doi: 10.1038/s41375-019-0461-5. Epub 2019 Apr 2.

PMID:
30940908
3.

Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.

Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C, Prechtl S, Suelzle D, Siegel F, Prinz F, Lesche R, Nicke B, Nowak-Reppel K, Himmel H, Mumberg D, von Nussbaum F, Nising CF, Bauser M, Haegebarth A.

J Med Chem. 2019 Jan 24;62(2):928-940. doi: 10.1021/acs.jmedchem.8b01606. Epub 2019 Jan 9.

PMID:
30563338
4.

Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance.

Quanz M, Bender E, Kopitz C, Grünewald S, Schlicker A, Schwede W, Eheim A, Toschi L, Neuhaus R, Richter C, Toedling J, Merz C, Lesche R, Kamburov A, Siebeneicher H, Bauser M, Hägebarth A.

Mol Cancer Ther. 2018 Nov;17(11):2285-2296. doi: 10.1158/1535-7163.MCT-17-1253. Epub 2018 Aug 16.

5.

Donated chemical probes for open science.

Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A.

Elife. 2018 Apr 20;7. pii: e34311. doi: 10.7554/eLife.34311.

6.

Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design.

Rahm F, Viklund J, Trésaugues L, Ellermann M, Giese A, Ericsson U, Forsblom R, Ginman T, Günther J, Hallberg K, Lindström J, Persson LB, Silvander C, Talagas A, Díaz-Sáez L, Fedorov O, Huber KVM, Panagakou I, Siejka P, Gorjánácz M, Bauser M, Andersson M.

J Med Chem. 2018 Mar 22;61(6):2533-2551. doi: 10.1021/acs.jmedchem.7b01884. Epub 2018 Mar 7.

PMID:
29485874
7.

Novel Class of Potent and Cellularly Active Inhibitors Devalidates MTH1 as Broad-Spectrum Cancer Target.

Ellermann M, Eheim A, Rahm F, Viklund J, Guenther J, Andersson M, Ericsson U, Forsblom R, Ginman T, Lindström J, Silvander C, Trésaugues L, Giese A, Bunse S, Neuhaus R, Weiske J, Quanz M, Glasauer A, Nowak-Reppel K, Bader B, Irlbacher H, Meyer H, Queisser N, Bauser M, Haegebarth A, Gorjánácz M.

ACS Chem Biol. 2017 Aug 18;12(8):1986-1992. doi: 10.1021/acschembio.7b00370. Epub 2017 Jul 12.

8.

Hafnium-Based Contrast Agents for X-ray Computed Tomography.

Berger M, Bauser M, Frenzel T, Hilger CS, Jost G, Lauria S, Morgenstern B, Neis C, Pietsch H, Sülzle D, Hegetschweiler K.

Inorg Chem. 2017 May 15;56(10):5757-5761. doi: 10.1021/acs.inorgchem.7b00359. Epub 2017 Apr 21.

PMID:
28430423
9.

18F-GP1, a Novel PET Tracer Designed for High-Sensitivity, Low-Background Detection of Thrombi.

Lohrke J, Siebeneicher H, Berger M, Reinhardt M, Berndt M, Mueller A, Zerna M, Koglin N, Oden F, Bauser M, Friebe M, Dinkelborg LM, Huetter J, Stephens AW.

J Nucl Med. 2017 Jul;58(7):1094-1099. doi: 10.2967/jnumed.116.188896. Epub 2017 Mar 16.

10.

Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo.

Chaturvedi A, Herbst L, Pusch S, Klett L, Goparaju R, Stichel D, Kaulfuss S, Panknin O, Zimmermann K, Toschi L, Neuhaus R, Haegebarth A, Rehwinkel H, Hess-Stumpp H, Bauser M, Bochtler T, Struys EA, Sharma A, Bakkali A, Geffers R, Araujo-Cruz MM, Thol F, Gabdoulline R, Ganser A, Ho AD, von Deimling A, Rippe K, Heuser M, Krämer A.

Leukemia. 2017 Oct;31(10):2020-2028. doi: 10.1038/leu.2017.46. Epub 2017 Jan 31.

11.

Pan-mutant IDH1 inhibitor BAY 1436032 for effective treatment of IDH1 mutant astrocytoma in vivo.

Pusch S, Krausert S, Fischer V, Balss J, Ott M, Schrimpf D, Capper D, Sahm F, Eisel J, Beck AC, Jugold M, Eichwald V, Kaulfuss S, Panknin O, Rehwinkel H, Zimmermann K, Hillig RC, Guenther J, Toschi L, Neuhaus R, Haegebart A, Hess-Stumpp H, Bauser M, Wick W, Unterberg A, Herold-Mende C, Platten M, von Deimling A.

Acta Neuropathol. 2017 Apr;133(4):629-644. doi: 10.1007/s00401-017-1677-y. Epub 2017 Jan 25.

PMID:
28124097
12.

Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876.

Siebeneicher H, Cleve A, Rehwinkel H, Neuhaus R, Heisler I, Müller T, Bauser M, Buchmann B.

ChemMedChem. 2016 Oct 19;11(20):2261-2271. doi: 10.1002/cmdc.201600276. Epub 2016 Aug 23.

13.

Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments.

Haftchenary S, Nelson SD Jr, Furst L, Dandapani S, Ferrara SJ, Bošković ŽV, Figueroa Lazú S, Guerrero AM, Serrano JC, Crews DK, Brackeen C, Mowat J, Brumby T, Bauser M, Schreiber SL, Phillips AJ.

ACS Comb Sci. 2016 Sep 12;18(9):569-74. doi: 10.1021/acscombsci.6b00050. Epub 2016 Aug 12.

14.

Characterization of a Novel Hafnium-Based X-ray Contrast Agent.

Frenzel T, Bauser M, Berger M, Hilger CS, Hegele-Hartung C, Jost G, Neis C, Hegetschweiler K, Riefke B, Suelzle D, Pietsch H.

Invest Radiol. 2016 Dec;51(12):776-785.

PMID:
27299578
15.

Identification of novel GLUT inhibitors.

Siebeneicher H, Bauser M, Buchmann B, Heisler I, Müller T, Neuhaus R, Rehwinkel H, Telser J, Zorn L.

Bioorg Med Chem Lett. 2016 Apr 1;26(7):1732-7. doi: 10.1016/j.bmcl.2016.02.050. Epub 2016 Feb 19.

PMID:
26949183
16.

Gene expression levels of matrix metalloproteinases in human atherosclerotic plaques and evaluation of radiolabeled inhibitors as imaging agents for plaque vulnerability.

Müller A, Krämer SD, Meletta R, Beck K, Selivanova SV, Rancic Z, Kaufmann PA, Vos B, Meding J, Stellfeld T, Heinrich TK, Bauser M, Hütter J, Dinkelborg LM, Schibli R, Ametamey SM.

Nucl Med Biol. 2014 Aug;41(7):562-9. doi: 10.1016/j.nucmedbio.2014.04.085. Epub 2014 Apr 21.

PMID:
24853402
17.

Design, synthesis, and initial evaluation of a high affinity positron emission tomography probe for imaging matrix metalloproteinases 2 and 9.

Selivanova SV, Stellfeld T, Heinrich TK, Müller A, Krämer SD, Schubiger PA, Schibli R, Ametamey SM, Vos B, Meding J, Bauser M, Hütter J, Dinkelborg LM.

J Med Chem. 2013 Jun 27;56(12):4912-20. doi: 10.1021/jm400156p. Epub 2013 Jun 7.

PMID:
23688254
18.

Discovery and optimization of 2-aryl oxazolo-pyrimidines as adenosine kinase inhibitors using liquid phase parallel synthesis.

Bauser M, Delapierre G, Hauswald M, Flessner T, D'Urso D, Hermann A, Beyreuther B, De Vry J, Spreyer P, Reissmüller E, Meier H.

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1997-2000.

PMID:
15050645
19.

New class of bacterial phenylalanyl-tRNA synthetase inhibitors with high potency and broad-spectrum activity.

Beyer D, Kroll HP, Endermann R, Schiffer G, Siegel S, Bauser M, Pohlmann J, Brands M, Ziegelbauer K, Haebich D, Eymann C, Brötz-Oesterhelt H.

Antimicrob Agents Chemother. 2004 Feb;48(2):525-32.

21.

Identification of a potent analogue of Nazumamide A through iteration of combinatorial tetrapeptide libraries.

Kundu B, Bauser M, Betschinger J, Kraas W, Jung G.

Bioorg Med Chem Lett. 1998 Jul 7;8(13):1669-72.

PMID:
9873411
22.

Investigation of the Molecular Recognition of Amino Acids by Cyclopeptides with Reflectometric Interference Spectroscopy.

Leipert D, Nopper D, Bauser M, Gauglitz G, Jung G.

Angew Chem Int Ed Engl. 1998 Dec 17;37(23):3308-3311. doi: 10.1002/(SICI)1521-3773(19981217)37:23<3308::AID-ANIE3308>3.0.CO;2-#.

PMID:
29711422
23.

Synthesis of hydantoins via N,N'-ureas derived from polymer-bound amino acids.

Bauser M, Winter M, Valenti CA, Wiesmüller KH, Jung G.

Mol Divers. 1997-1998;3(4):257-60.

PMID:
9850523

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