iSPAAC: isomer‐free generation of a Bcl‐xL‐inhibitor in living cells

C. Lis, S. Rubner, C. Gröst, R. Hoffmann, D. Knappe, T. Berg

Chem. Eur. J., published online. Link to Article


C. Lis, S. Rubner, M. Roatsch, A. Berg, T. Gilcrest, D. Fu, E. Nguyen, A.-M. Schmidt, H. Krautscheid, J. Meiler, T. Berg

Development of Erasin: a chromone-based STAT3 inhibitor which induces apoptosis in Erlotinib-resistant lung cancer cells

Sci. Rep. 2017, 7, 17390. Link to Article (Open Access)

T. Berg

Inhibition of Protein–Protein Interactions: New Options for Developing Drugs against Neglected Tropical Diseases

Angew. Chem. Int. Ed. 2017, 56, 12048–12050. Link to Article


A. Berg, T. Berg

A small-molecule screen identifies the antitrypanosomal agent suramin and analogues NF023 and NF449 as inhibitors of STAT5a/b

Bioorg. Med. Chem. Lett. 2017, 27, 3349-3352. Link to Article

N. Elumalai, K. Natarajan, T. Berg

Halogen-substituted catechol bisphosphates are potent and selective inhibitors of the transcription factor STAT5b

Bioorg. Med. Chem. 2017, 25, 3871–3882. Link to Article


N. Elumalai, A. Berg, S. Rubner, L. Blechschmidt, C. Song, K. Natarajan, J. Matysik, T. Berg

Rational development of Stafib-2: a selective, nanomolar inhibitor of the transcription factor STAT5b.

Sci. Rep. 2017, 7, 819. Link to Article (Open Access)


T. Berg

Protein-Protein-Wechselwirkungen mit organischen Substanzen hemmen.

Nachr. Chem. 2016, 64, 960-964. Link to Article

T. Goldbach, D. Knappe, C. Reinsdorf, T. Berg, R. Hoffmann

Ribosomal binding and antibacterial activity of ethylene glycol-bridged apidaecin Api137 and oncocin Onc112 conjugates.

J. Pept. Sci. 2016, 22, 592-599. Link to Article

A. Scharow, D. Knappe, W. Reindl, R. Hoffmann, T. Berg

Development of bifunctional inhibitors of polo-like kinase 1 with low nanomolar activities against the polo-box domain.

ChemBioChem 2016, 17, 759-767. Link to Article

A. Berg, T. Berg

Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.

ChemBioChem 2016, 17, 650-656. Link to Article

N. Elumalai, A. Berg, S. Rubner, T. Berg

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b

ACS Chem. Biol. 2015, 10, 2884−2890. Link to Article

A. Scharow, M. Raab, K. Saxena, S. Sreeramulu, D. Kudlinzki, S. Gande, C. Dötsch, E. Kurunci-Csacsko, S. Klaeger, B. Kuster, H. Schwalbe, K. Strebhardt, T. Berg

Optimized Plk1 PBD inhibitors based on Poloxin induce mitotic arrest and apoptosis in tumor cells.

ACS Chem. Biol. 2015, 10, 2570-2579. Link to Article


C. Gröst, T. Berg

PYRROC: the first functionalized cycloalkyne that facilitates isomer-free generation of organic molecules by SPAAC

Org. Biomol. Chem. 2015, 13, 3866-3870. DOI: 10.1039/C5OB00212E (Open Access)

Recommended by "Faculty of 1000"


N. Elumalai, A. Berg, K. Natarajan, A. Scharow, T. Berg

Nanomolar Inhibitors of the Transcription Factor STAT5b with High Selectivity over STAT5a

Angew. Chem. Int. Ed. 2015, 54, 4758-4763. DOI: 10.1002/anie.201410672 (Open Access)


D. Cubrilovic, K. Barylyuk, D. Hofmann, M. Walczak, M. Gräber, T. Berg, G. Wider, R. Zenobi

Direct Monitoring of Protein-Protein Inhibition Using Nano Electrospray Ionization Mass Spectrometry

Chem. Sci. 2014, 5, 2794-2803. DOI: 10.1039/C3SC53360C

C. Gröst, M. Gräber, M. Hell, T. Berg

Synthesis and biochemical evaluation of highly enantiomerically pure (R,R)- and (S,S)-alexidine.

Bioorg. Med. Chem. 2013, 21, 7357-7363. DOI: 10.10.1016/j.bmc.2013.09.057


M. Gräber#, M. Hell#, C. Gröst#, A. Friberg, B. Sperl, M. Sattler, T. Berg

Oral disinfectants inhibit protein-protein interactions mediated by the anti-apoptotic protein Bcl-xL and induce apoptosis in human oral tumor cells.

Angew. Chem. Int. Ed. 2013, 52, 4487-4491 ("Hot paper"). DOI: 10.1002/anie.201208889


T. Berg

Reply to "Revisiting the specificity of small-molecule inhibitors: the example of Stattic in dendritic cells”.

Chem. Biol. 2012, 19, 1215-1216. DOI: 10.1016/j.chembiol.2012.09.007


T. Itkin, A. Ludin, B. Gradus, S. Gur-Cohen, A. Kalinkovich, A. Schajnovitz, Y. Ovadya, O. Kollet, J. Canaani, E. Shezen, D.J. Coffin, G.N. Enikolopov, T. Berg, W. Piacibello, E. Hornstein, T. Lapidot

FGF-2 Expands Murine Hematopoietic Stem and Progenitor Cells via Proliferation of Stromal Cells, c-Kit Activation and CXCL12 Downregulation

Blood 2012, 120, 1843-1855. DOI: 10.1182/blood-2011-11-394692


F. Liu, J.-E. Park, W-J. Qian, D. Lim, A. Scharow, T. Berg, M.B. Yaffe, K.S Lee, T.R. Burke

Peptoid-Peptide Hybrid Ligands Targeting the Polo Box Domain of Polo-Like Kinase 1

ChemBioChem 2012, 13, 1291-1296. DOI: 10.1002/cbic.201200206


F. Liu, J.-E. Park, W-J. Qian, D. Lim, A. Scharow, T. Berg, M.B. Yaffe, K.S Lee, T.R. Burke

Identification of High Affinity Polo-like Kinase 1 (Plk1) Polo-box Domain Binding Peptides Using Oxime-based Diversification.

ACS Chem. Biol. 2012, 7, 805-810. DOI: 10.1021/cb200469a

M. Sanhaji, N-N. Kreis, B. Zimmer, T. Berg, F. Louwen, J. Yuan

p53 is not directly relevant to the response of Polo-like kinase 1 inhibitors.

Cell Cycle 2012, 11, 543-553. DOI: DOI: 10.4161/cc.11.3.19076

A. Hollis, B. Sperl, M. Gräber, T. Berg

The natural product betulinic acid inhibits C/EBP family transcription factors.

ChemBioChem 2012, 13, 302-307. DOI: 10.1002/cbic.201100652


W. Reindl, K. Strebhardt, T. Berg

A Fluorescence Polarization Assay for the Discovery of Inhibitors of the Polo-Box Domain of Polo-Like Kinase 1.

Meth. Mol. Biol. 2012, 795, 69-81, published online. DOI: 10.1007/978-1-61779-337-0_5


J. Yuan, M. Sanhaji, A. Krämer, W. Reindl, M. Hofmann, N.N. Kreis, B. Zimmer, T. Berg, K. Strebhardt

Polo-Box Domain Inhibitor Poloxin Activates the Spindle Assembly Checkpoint and Inhibits Tumor Growth in Vivo.

Am. J Pathol. 2011 , 179, 2091 - 2099. doi:10.1016/j.ajpath.2011.06.031


M. Gräber, W. Janczyk, B. Sperl, N. Elumalai, C. Kozany, F. Hausch, T.A. Holak, T. Berg

Selective targeting of disease-relevant protein binding domains by O-phosphorylated natural product derivatives.

ACS Chem. Biol. 2011, 6, 1008 - 1014. DOI: 10.1021/cb2001796


F. Liu, J.E. Park, W.J. Qian, D. Lim, M. Gräber, T. Berg, M.B. Yaffe, K.S. Lee, T.R. Burke, Jr.

Serendipitious alkylation of a Plk1 ligand uncovers a new binding channel.

Nat. Chem. Biol. 2011, 7, 595-601. DOI: 10.1038/nchembio.614


S. Richter, I. Neundorf, K. Loebner, M. Gräber, T. Berg, R. Bergmann, J. Steinbach, J. Pietzsch, F. Wuest

Phosphopeptides with improved cellular uptake properties as ligands for the polo-box domain of polo-like kinase 1.

Bioorg. Med. Chem. Lett. 2011, 21, 4686-4689. DOI: 10.1016/j.bmcl.2011.06.103


T. Berg

Small-Molecule Modulators of c-Myc/Max and Max/Max Interactions.

Curr. Top. Microbiol. Immunol. 2011, 348, 139-149. DOI: 10.1007/82_2010_90


S. Wetzel, W. Wilk, S. Chammaa, B. Sperl, A. Roth, A. Yektaoglu, S. Renner, T. Berg, C. Arenz, A. Giannis, T.I. Oprea, D. Rauh, M. Kaiser, H. Waldmann

A Scaffold-Tree-Merging Strategy for Prospective Bioactivity Annotation of gamma-Pyrones.

Angew. Chem. Int. Ed. 2010, 49, 3666-3670. DOI: 10.1002/anie.200906555



D. Castelletti, G. Fiaschetti, V. Di Dato, U. Ziegler, C. Kumps, K. De Preter, M. Zollo, F. Speleman, T. Shalaby, D. De Martino, T. Berg, A. Eggert, A. Arcaro, M.A. Grotzer

The quassinoid derivative NBT-272 targets both the AKT and ERK signaling pathways in embryonal tumors.

Mol. Cancer Ther. 2010, 9, 3145-3157. DOI: 10.1158/1535-7163.MCT-10-0539


T. Berg

Small-molecule inhibitors of protein–protein interactions.

In: Protein-protein complexes: Analysis, Modeling and Drug Design (Editor: Martin Zacharias), Imperial College Press, 2010, 318-339.

A. Riechers, A. Grauer, S. Ritter, B. Sperl, T. Berg, B. König

Binding of phosphorylated peptides and inhibition of their interaction with disease-relevant human proteins by synthetic metal-chelate receptors.

J. Mol. Recognit. 2010, 23, 329-334. DOI:10.1002/jmr.986


W. Reindl, M. Gräber, K. Strebhardt, T. Berg

Development of high-throughput assays based on fluorescence polarization for inhibitors of the polo-box domains of polo-like kinases 2 and 3.

Anal. Biochem. 2009, 395, 189-194. DOI:10.1016/j.ab.2009.08.031


B. Sperl, M.H.J. Seifert, T. Berg

Natural product inhibitors of protein-protein interactions mediated by Src-family SH2 domains.

Bioorg. Med. Chem. Lett. 2009, 19, 3305-3309. DOI: 10.1016/j.bmcl.2009.04.083


W. Reindl, J. Yuan, A. Krämer, K. Strebhardt, T. Berg

A Pan-Specific Inhibitor of the Polo-Box Domains of Polo-like Kinases arrests Cancer Cells in Mitosis.

ChemBioChem 2009, 10, 1145-1148. DOI: 10.1002/cbic.200900059


T. Berg

Allosteric switches: remote controls for proteins.

Angew. Chem. Int. Ed. 2009, 48, 3218-3220. DOI: 10.1002/anie.200806169

T. Berg

Modulation of protein–protein interactions with small molecules.

In: Wiley encyclopedia of chemical biology, volume 4, John Wiley & Sons (Editor: Tadhg P. Begley), 2008, 121-143.


W. Reindl, K. Strebhardt, T. Berg

A high-throughput assay based on fluorescence polarization for inhibitors of the polo-box domain of polo-like kinase 1.

Anal. Biochem. 2008, 383, 205-209. DOI: 10.1016/j.ab.2008.08.014


T. Berg

Small-molecule inhibitors of protein-protein interactions.

Curr. Opin. Drug Discov. Devel. 2008, 11, 666-674. BioMedCentral


T. Berg

Inhibition of transcription factors with small organic molecules.

Curr. Opin. Chem. Biol. 2008, 12, 464-471. DOI: 10.1016/j.cbpa.2008.07.023


T. Berg

Signal Transducers and Activators of Transcription as Targets for Small Organic Molecules.

ChemBioChem 2008, 9, 2039-2044. DOI: 10.1002/cbic.200800274


W. Reindl, J. Yuan, A. Krämer, K. Strebhardt, T. Berg

Inhibition of Polo-like Kinase 1 by Blocking Polo-Box Domain-Dependent Protein-Protein Interactions.

Chem. Biol. 2008,15, 459-466. DOI: 10.1016/j.chembiol.2008.03.013

This article was highlighted by:

1) K.S. Lee, J.R. Idle

Pinning down the polo-box domain

Chem. Biol. 2008,15, 415-416. DOI: 10.1016/j.chembiol.2008.04.009

2) Faculty of 1000 Biology


J. Müller, J. Schust, T. Berg

A high-throughput assay for signal transducer and activator of transcription 5b based on fluorescence polarization.

Anal. Biochem. 2008, 375, 249-254. DOI: 10.1016/j.ab.2008.01.017


J. Müller, B. Sperl, W. Reindl, A. Kiessling, T. Berg

Chromone-based inhibitors of the transcription factor STAT5.

ChemBioChem 2008, 9, 723-727. DOI: 10.1002/cbic.200700701


A. Kiessling, R. Wiesinger, B. Sperl, T. Berg

Selective inhibition of c-Myc/Max dimerization by a pyrazolo[1,5-a]pyrimidine. ChemMedChem 2007, 2, 627-630.

DOI: 10.1002/cmdc.200600294


J. Schust, B. Sperl, A. Hollis, T.U. Mayer, T. Berg

Stattic: a small-molecule inhibitor of STAT3 activation and dimerization.

Chem. Biol. 2006, 13, 1235-1242. DOI: 10.1016/j.chembiol.2006.09.018

This article was highlighted by:

1) J.S. McMurray

A New Small-Molecule Stat3 Inhibitor

Chem. Biol. 2006, 13, 1123-1124. doi:10.1016/j.chembiol.2006.11.001

2) Faculty of 1000 Biology

A. Kiessling, B. Sperl, A. Hollis, D. Eick, T. Berg

Selective inhibition of c-Myc/Max dimerization and DNA binding by small molecules.

Chem. Biol. 2006, 13, 745-751. DOI: 10.1016/j.chembiol.2006.05.011


T. Berg

Inhibition of TNF-a signaling: divide and conquer.

ChemMedChem 2006,1, 687-688. DOI: 10.1002/cmdc.200600050


T. Berg, T.U. Mayer, R. Frank

Trendbericht „Chemische Biologie“ im Gebiet „Biochemie und Molekularbiologie“ 2005.

Nachr. Chem. 2006, 54, 265-270.


S.K. Knauer, S. Moodt, T. Berg, U. Liebel, R. Pepperkok, R.H. Stauber

Translocation biosensors to study signal-specific nucleo-cytoplasmic transport, protease activity and protein-protein interactions.

Traffic 2005, 6, 594-606. DOI: 10.1111/j.1600-0854.2005.00298.x


T. Berg

Cellular profiling of small-molecule bioactivities: an alternative tool for chemical biology.

Angew. Chem. Int. Ed. 2005, 44, 5008-5011.

DOI: 10.1002/anie.200500721


T. Berg

Protein-Protein Interactions: Methods and Applications.

ChemBioChem 2005, 6, 446-447 (book review).


J. Schust, T. Berg

A high-throughput fluorescence polarization assay for STAT3.

Anal. Biochem. 2004, 330, 114-118. DOI: 10.1016/j.ab.2004.03.024


T. Berg

Use of “tethering” for the identification of a small molecule which binds to a dynamic hot spot on the interleukin-2 surface.

ChemBioChem 2004, 5, 1051-1053. DOI: 10.1002/cbic.200400054


T. Berg

When chemistry met biology.

Angew. Chem. Int. Ed. 2004, 43, 3750-3751 (Meeting report).

DOI: 10.1002/anie.200460998


J.S. Iacovoni, S.B. Cohen, T. Berg, P.K. Vogt

v-Jun targets showing an expression pattern that correlates with the transformed cellular phenotype.

Oncogene 2004, 23, 5703-5706.

DOI: 10.1038/sj.onc.1207737


T. Berg

Modulation of protein-protein interactions with small organic molecules.

Angew. Chem. Int. Ed. 2003, 42, 2462-2481.

DOI: 10.1002/anie.200200558


T. Berg, S.B. Cohen, J. Desharnais, C. Sonderegger, D.J. Maslyar, J. Goldberg, D.L. Boger, P.K. Vogt

Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts.

Proc. Natl. Acad. Sci. USA 2002, 99, 3830-3835. DOI: 10.1073/pnas.062036999

This article was highlighted by Faculty of 1000 Biology


E. Vogel, N. Jux, J. Dörr, T. Pelster, T. Berg, H.-S. Böhm, F. Behrens, J. Lex, D. Bremm, G. Hohlneicher

Furan-Based Porphyrins: Tetraoxa[4n+2]porphyrin dications with 18 p-, 22 p-, or 26 p-electron systems.

Angew. Chem. Int. Ed. 2000, 39, 1101-1104.

DOI: 10.1002/(SICI)1521-3773(20000317)39:63.0.CO;2-F


T. Berg, A. Simeonov, K.D. Janda

A combined parallel synthesis and screening of macrocyclic lanthanide complexes for the cleavage of phospho di- and triesters and double-stranded DNA.

J. Comb. Chem. 1999, 1, 96-100. DOI: 10.1021/cc9800125


T. Berg, A. Vandersteen, K.D. Janda

High-throughput synthesis and screening for the discovery of hydrolytic metal complexes.

Bioorg. Med. Chem. Lett. 1998, 8, 1221-1224.



D. Enders, T. Berg, G. Raabe, J. Runsink

Enantioselective synthesis of a-phosphanyl ketones and 2-phosphanyl alcohols.

Liebigs. Ann. 1997, 345-361. 10.1002/jlac.199719970212


D. Enders, T. Berg

Enantioselective synthesis of 2-phosphino alcohols via phosphinylation of metalated chiral aldehyde hydrazones.

Synlett 1996, 796-798. DOI: 10.1055/s-1996-5519


D. Enders, T. Berg, G. Raabe, J. Runsink

Enantioselektive Synthese von a‑Phosphino­ketonen.

Helv. Chim. Acta 1996, 79, 118 - 122. DOI: 10.1002/hlca.19960790112