A Kramer
Andreas Krämer

Principal Investigator

Frankfurt
kraemer@pharmchem.uni-frankfurt.de
+49 (0)69  798 29875

Andreas Krämer graduated with a diploma in Chemistry from the University of Freiburg in 2012. During his PhD thesis at the University of Darmstadt (2013-2017), he focused on structural studies of bacterial members of the histone deacetylase superfamily (HDAC). After completing his PhD, he joined the group led byStefan Knapp at the SGC Frankfurt as a postdoc, where he was funded by the Wellcome Trust, working on the structure-based development of selective and potent CaMK1D kinase inhibitors for the treatment of highly aggressive subtypes of breast cancer. Afterwards he worked at the Frankfurt Cancer Institute (FCI) as a staff scientist where, among other things, he was responsible for developing a comprehensive screening platform for kinases. In the beginning of 2022, Andreas became aprincipal investigato rand is responsible for running the X-ray crystallography facility unit. His current research interests focus primarily on the structural biology of kinases and E3 ligases.

Publications AKramer

Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.
Krämer A, Kurz CG, Berger BT, Celik IE, Tjaden A, Greco FA, Knapp S, Hanke T
Eur J Med Chem. 2020 208:112770. doi: 10.1016/j.ejmech.2020.112770
PMID: 32883634

Discovery of first in vivo active inhibitors of soluble epoxide hydrolase (sEH) phosphatase domain.
Kramer JS, Woltersdorf S, Duflot T, Hiesinger K, Lillich FF, Knöll F, Wittmann SK, Klingler FM, Brunst S, Chaikuad A, Morisseau C, Hammock BD, Buccellati C, Sala A, Rovati GE, Leuillier M, Fraineau S, Rondeaux J, Hernandez Olmos V, Heering J, Merk D, Pogoryelov D, Steinhilber D, Knapp S, Bellien J, Proschak E
J. Med. Chem.. 2019 . doi: 10.1021/acs.jmedchem.9b00445
PMID: 31436984

2023

Deep Annotation of Donated Chemical Probes (DCP) in Organotypic Human Liver Cultures and Patient-Derived Organoids from Tumor and Normal Colorectum.
Tredup C, Ndreshkjana B, Schneider NS, Tjaden A, Kemas AM, Youhanna S, Lauschke VM, Berger BT, Krämer A, Berger LM, Röhm S, Knapp S, Farin HF, Müller S
ACS Chem Biol. 21.03.2023 . doi: 10.1021/acschembio.2c00877
PMID: 36944371

Chemistry-led investigations into the mode of action of NAMPT activators, resulting in the discovery of non-pyridyl class NAMPT activators.
Tang S, Garzon Sanz M, Smith O, Krämer A, Egbase D, Caton PW, Knapp S, Butterworth S
Acta Pharm Sin B. 07.03.2023 13(2):709-721. doi: 10.1016/j.apsb.2022.07.016
PMID: 36873168

2022

Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH
Eur J Med Chem. 30.12.2022 249:115043. doi: 10.1016/j.ejmech.2022.115043
PMID: 36736152

MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core.
Schröder M, Leiendecker M, Grädler U, Braun J, Blum A, Wanior M, Berger BT, Krämer A, Müller S, Esdar C, Knapp S, Heinrich T
J Med Chem. 14.12.2022 . doi: 10.1021/acs.jmedchem.2c01705
PMID: 36516476

Discovery of 3-Amino-1H-pyrazole-Based Kinase Inhibitors to Illuminate the Understudied PCTAIRE Family.
Amrhein JA, Berger LM, Tjaden A, Krämer A, Elson L, Tolvanen T, Martinez-Molina D, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T
Int J Mol Sci. 27.11.2022 23(23):. doi: 10.3390/ijms232314834
PMID: 36499165

Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Amrhein JA, Beyett TS, Feng WW, Krämer A, Weckesser J, Schaeffner IK, Rana JK, Jänne PA, Eck MJ, Knapp S, Hanke T
J Med Chem. 16.11.2022 . doi: 10.1021/acs.jmedchem.2c01041
PMID: 36384036

Compilation and evaluation of a fatty acid mimetics screening library.
Ehrler JHM, Brunst S, Tjaden A, Kilu W, Heering J, Hernandez-Olmos V, Krommes A, Kramer JS, Steinhilber D, Schubert-Zsilavecz M, Müller S, Merk D, Proschak E
Biochem Pharmacol. 27.07.2022 204:115191. doi: 10.1016/j.bcp.2022.115191
PMID: 35907497

Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-a]pyrimidine-Based Macrocycles.
Kurz CG, Preuss F, Tjaden A, Cusack M, Amrhein JA, Chatterjee D, Mathea S, Berger LM, Berger BT, Krämer A, Weller M, Weiss T, Müller S, Knapp S, Hanke T
J Med Chem. 24.05.2022 . doi: 10.1021/acs.jmedchem.2c00173
PMID: 35608370

Cascade Synthesis of Kinase-Privileged 3-Aminoindazoles via Intramolecular N-N Bond Formation.
Zhu WF, Krämer A, Knapp S, Proschak E, Hernandez-Olmos V
J Org Chem. 18.02.2022 . doi: 10.1021/acs.joc.1c03057
PMID: 35179025

Aurora Kinase A Is Involved in Controlling the Localization of Aquaporin-2 in Renal Principal Cells.
Baltzer S, Bulatov T, Schmied C, Krämer A, Berger BT, Oder A, Walker-Gray R, Kuschke C, Zühlke K, Eichhorst J, Lehmann M, Knapp S, Weston J, von Kries JP, Süssmuth RD, Klussmann E
Int J Mol Sci. 11.01.2022 23(2):. doi: 10.3390/ijms23020763
PMID: 35054947

2021

Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.
Lillich FF, Willems S, Ni X, Kilu W, Borkowsky C, Brodsky M, Kramer JS, Brunst S, Hernandez-Olmos V, Heering J, Schierle S, Kestner RI, Mayser FM, Helmstädter M, Göbel T, Weizel L, Namgaladze D, Kaiser A, Steinhilber D, Pfeilschifter W, Kahnt AS, Proschak A, Chaikuad A, Knapp S, Merk D, Proschak E
J Med Chem. 24.11.2021 . doi: 10.1021/acs.jmedchem.1c01331
PMID: 34818007

Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.
Dölle A, Adhikari B, Krämer A, Weckesser J, Berner N, Berger LM, Diebold M, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Gebel J, Löhr F, Dötsch V, Eilers M, Heinzlmeir S, Kuster B, Sotriffer C, Wolf E, Knapp S
J Med Chem. 13.05.2021 . doi: 10.1021/acs.jmedchem.1c00146
PMID: 33980013

Exploiting vulnerabilities of SWI/SNF chromatin remodelling complexes for cancer therapy.
Wanior M, Krämer A, Knapp S, Joerger AC
Oncogene. 03.05.2021 . doi: 10.1038/s41388-021-01781-x
PMID: 33941852

Development of a potent and selective chemical probe for the pleiotropic kinase CK2.
Wells CI, Drewry DH, Pickett JE, Tjaden A, Krämer A, Müller S, Gyenis L, Menyhart D, Litchfield DW, Knapp S, Axtman AD
Cell Chem Biol. 11.01.2021 . doi: 10.1016/j.chembiol.2020.12.013
PMID: 33484635

2020

Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis.
Wanior M, Preuss F, Ni X, Krämer A, Mathea S, Göbel T, Heidenreich D, Simonyi S, Kahnt AS, Joerger AC, Knapp S
J Med Chem. 10.12.2020 63(23):14680-14699. doi: 10.1021/acs.jmedchem.0c01242
PMID: 33216538

Large eQTL meta-analysis reveals differing patterns between cerebral cortical and cerebellar brain regions
Sieberts SK, Perumal TM, Carrasquillo MM, Allen M, Reddy JS, Hoffman GE, Dang KK, Calley J, Ebert PJ, Eddy J, Wang X, Greenwood AK, Mostafavi S, Akbarian S, Bendl J, Breen MS, Brennand K, Brown L, Browne A, Buxbaum JD, Charney A, Chess A, Couto L, Crawford G, Devillers O, Devlin B, Dobbyn A, Domenici E, Filosi M, Flatow E, Francoeur N, Fullard J, Gil SE, Girdhar K, Gulyás-Kovács A, Gur R, Hahn CG, Haroutunian V, Hauberg ME, Huckins L, Jacobov R, Jiang Y, Johnson JS, Kassim B, Kim Y, Klei L, Kramer R, Lauria M, Lehner T, Lewis DA, Lipska BK, Montgomery K, Park R, Rosenbluh C, Roussos P, Ruderfer DM, Senthil G, Shah HR, Sloofman L, Song L, Stahl E, Sullivan P, Visintainer R, Wang J, Wang YC, Wiseman J, Xia E, Zhang W, Zharovsky E, Addis L, Addo SN, Airey DC, Arnold M, Bennett DA, Bi Y, Biber K, Blach C, Bradhsaw E, Brennan P, Canet-Aviles R, Cao S, Cavalla A, Chae Y, Chen WW, Cheng J, Collier DA, Dage JL, Dammer EB, Davis JW, Davis J, Drake D, Duong D, Eastwood BJ, Ehrlich M, Ellingson B, Engelmann BW, Esmaeelinieh S, Felsky D, Funk C, Gaiteri C
Scientific Data. 01.12.2020 7:-. doi: 10.1038/s41597-020-00642-8
PMID: 33046718

Selective targeting of the αC and DFG-out pocket in p38 MAPK.
Röhm S, Schröder M, Dwyer JE, Widdowson CS, Chaikuad A, Berger BT, Joerger AC, Krämer A, Harbig J, Dauch D, Kudolo M, Laufer S, Bagley MC, Knapp S
Eur J Med Chem. 20.08.2020 208:112721. doi: 10.1016/j.ejmech.2020.112721
PMID: 33035818

Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.
Krämer A, Kurz CG, Berger BT, Celik IE, Tjaden A, Greco FA, Knapp S, Hanke T
Eur J Med Chem. 23.08.2020 208:112770. doi: 10.1016/j.ejmech.2020.112770
PMID: 32883634

Discovery of highly selective inhibitors of calmodulin-dependent kinases that restore insulin sensitivity in the diet-induced obese in vivo mouse model.
Fromont C, Atzori A, Kaur D, Hashmi L, Greco G, Cabanillas A, Nguyen HV, Jones DH, Garzón M, Varela A, Stevenson B, Iacobini G, Lenoir M, Rajesh S, Box C, Kumar J, Grant P, Novitskaia V, Morgan J, Sorrell F, Redondo C, Kramer A, Harris CJ, Leighton B, Vickers S, Cheetham S, Kenyon C, Grabowska AM, Overduin M, Berditchevski F, Weston CJ, Knapp S, Fischer PM, Butterworth S
J. Med. Chem.. 20.05.2020 . doi: 10.1021/acs.jmedchem.9b01803
PMID: 32433887

Targeting Cavity-Creating p53 Cancer Mutations with Small-Molecule Stabilizers: the Y220X Paradigm.
Bauer MR, Krämer A, Settanni G, Jones RN, Ni X, Khan Tareque R, Fersht AR, Spencer J, Joerger AC
ACS Chem Biol. 20.03.2020 15(3):657-668. doi: 10.1021/acschembio.9b00748
PMID: 31990523

2019

Aspartate/asparagine-β-hydroxylase crystal structures reveal an unexpected epidermal growth factor-like domain substrate disulfide pattern.
Pfeffer I, Brewitz L, Krojer T, Jensen SA, Kochan GT, Kershaw NJ, Hewitson KS, McNeill LA, Kramer H, Münzel M, Hopkinson RJ, Oppermann U, Handford PA, McDonough MA, Schofield CJ
Nat Commun. 28.10.2019 10(1):4910. doi: 10.1038/s41467-019-12711-7
PMID: 31659163

Discovery of first in vivo active inhibitors of soluble epoxide hydrolase (sEH) phosphatase domain.
Kramer JS, Woltersdorf S, Duflot T, Hiesinger K, Lillich FF, Knöll F, Wittmann SK, Klingler FM, Brunst S, Chaikuad A, Morisseau C, Hammock BD, Buccellati C, Sala A, Rovati GE, Leuillier M, Fraineau S, Rondeaux J, Hernandez Olmos V, Heering J, Merk D, Pogoryelov D, Steinhilber D, Knapp S, Bellien J, Proschak E
J. Med. Chem.. 22.08.2019 . doi: 10.1021/acs.jmedchem.9b00445
PMID: 31436984

A chemical toolbox for the study of bromodomains and epigenetic signaling.
Wu Q, Heidenreich D, Zhou S, Ackloo S, Krämer A, Nakka K, Lima-Fernandes E, Deblois G, Duan S, Vellanki RN, Li F, Vedadi M, Dilworth J, Lupien M, Brennan PE, Arrowsmith CH, Müller S, Fedorov O, Filippakopoulos P, Knapp S
Nat Commun. 23.04.2019 10(1):1915. doi: 10.1038/s41467-019-09672-2
PMID: 31015424

2009

Structural basis and specificity of human otubain 1-mediated deubiquitination.
Edelmann MJ, Iphöfer A, Akutsu M, Altun M, di Gleria K, Kramer HB, Fiebiger E, Dhe-Paganon S, Kessler BM
Biochem. J.. 1.3.2009 418(2):379-90. doi: 10.1042/BJ20081318
PMID: 18954305

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