Research Area E - Publications 2016
19-Apr-2017
Chem. Sci.,8, 4644-4653, DOI: 10.1039/c6sc05044a
Chem. Sci., online article
The optical control over biological function with small photoswitchable molecules has gathered significant attention in the last decade. Herein, we describe the design and synthesis of a small library of photoswitchable peptidomimetics based upon human atrial natriuretic peptide (ANP), in which the photochromic amino acid [3-(3-aminomethyl)phenylazo]phenylacetic ...
20-Mar-2017
Am 02.02.2017 durften 22 naturwissenschaftlich besonders interessierte Schüler/innen der Unterstufe des Ernst Mach Gymnasiums zusammen mit ihren Lehrerinnen eine Exkursion zum CIPSM machen.
This is their resume:
„Das Erlebnis startete schon frühmorgens um rechtzeitig am Campus anzukommen. An der Universität wurden wir sehr herzlich empfangen.
Dr. Oliver Baron ...
29-Nov-2016
Molecular & Cellular Oncology, 4:1, e1263713, DOI:10.1080/23723556.2016.1263713
Molecular & Cellular Oncology, online article
Stalling of the DNA replication machinery activates the ATR checkpoint kinase, which coordinates the cellular responses to replication stress. New studies identify a novel ATR activator, ETAA1, which is indispensable for the maintenance of genome integrity. Dysregulation of ETAA1 may contribute to the development of pancreatic cancer.
25-Nov-2016
Chem. Commun., DOI: 10.1039/C6CC07517G
Chem. Commun., online article
A deeper investigation of the chemistry that occurs on the newly discovered epigenetic DNA bases 5-hydroxymethyl-(hmdC), 5-formyl-(fdC), and 5-carboxy-deoxycytidine (cadC) requires chemical tool compounds, which are able to dissect the different potential reaction pathways in cells. Here we report that the 2′-(R)-fluorinated derivatives F-hmdC, F-fdC, and F-cadC, ...
11-Nov-2016
Chem. Commun., 53, 107-110, DOI: 10.1039/C6CC08365J
Chem. Commun., online article
Ramariolides A–D are natural products with antibacterial activity. To exploit their cellular mechanism, we here devise the first total synthesis and prepare a photoprobe for target identification. Antibacterial testing against several pathogenic strains including Mycobacterium tuberculosis revealed the highest potency for ramariolide A. Chemical proteomics ...
07-Nov-2016
Nature Cell Biology, 18, 1357–1366, doi:10.1038/ncb3436
Nature Cell Biology, online article
DNA double-strand breaks (DSBs) are highly cytotoxic DNA lesions, whose accurate repair by non-homologous end-joining (NHEJ) or homologous recombination (HR) is crucial for genome integrity and is strongly influenced by the local chromatin environment1, 2. Here, we identify SCAI (suppressor of cancer cell invasion) as a 53BP1-interacting chromatin-associated ...
30-Oct-2016
J. Proteome Res., 15 (12), pp 4490–4504, DOI: 10.1021/acs.jproteome.6b00621
J. Proteome Res., online article
Although substantial progress has been made regarding the use of molecularly targeted cancer therapies, resistance almost invariably develops and presents a major clinical challenge. The tumor microenvironment can rescue cancer cells from kinase inhibitors by growth-factor-mediated induction of pro-survival pathways. Here we show that epidermal growth factor ...
28-Oct-2016
Mar. Drugs, 14(11), 200; doi:10.3390/md14110200
Mar. Drugs, online article
The glycogen-synthase-kinase 3 (GSK-3) is an important target in drug discovery. This enzyme is involved in the signaling pathways of type 2 diabetes, neurological disorders, cancer, and other diseases. Therefore, inhibitors of GSK-3 are promising drug candidates for the treatment of a broad range of diseases. Here we report pannorin, alternariol, and ...
28-Oct-2016
Chem. Sci., DOI: 10.1039/C6SC03438A
Chem. Sci., online article
Caseinolytic proteases (ClpP) are important for recognition and controlled degradation of damaged proteins. While the majority of bacterial organisms utilize only a single ClpP, Listeria monocytogenes expresses two isoforms (LmClpP1 and LmClpP2). LmClpPs assemble into either a LmClpP2 homocomplex or a LmClpP1/2 heterooligomeric complex. The heterocomplex in ...
26-Oct-2016
Angew. Chem. Int. Ed., 55, 1 – 7, DOI: 10.1002/anie.201607338
Angew. Chem. Int. Ed., online article
Gram-negative bacteria represent a challenging task for antibacterial drug discovery owing to their impermeable cell membrane and restricted uptake of small molecules. We herein describe the synthesis of natural-product-derived epoxycyclohexenones and explore their antibiotic activity against several pathogenic bacteria. A compound with activity against ...
22-Oct-2016
PROTEINS, Pages 65-71, Volume85, Issue1, Pages 65-71, https://doi.org/10.1002/prot.25193
PROTEINS, online article
The analysis and comparison of large numbers of immunoglobulin (Ig) sequences that arise during an antibody selection campaign can be time‐consuming and tedious. Typically, the identification and annotation of framework as well as complementarity‐determining regions (CDRs) is based on multiple sequence alignments using standardized numbering schemes, which allow ...
21-Oct-2016
ACS Chem. Biol., 11 (12), pp 3400–3411, DOI: 10.1021/acschembio.6b00709
ACS Chem. Biol., online article
The receptor tyrosine kinase EPHA2 (Ephrin type-A receptor 2) plays important roles in oncogenesis, metastasis, and treatment resistance, yet therapeutic targeting, drug discovery, or investigation of EPHA2 biology is hampered by the lack of appropriate inhibitors and structural information. Here, we used chemical proteomics to survey 235 clinical kinase ...
17-Oct-2016
Nature Microbiology, 2, Article number: 16189, doi:10.1038/nmicrobiol.2016.189
Nature Microbiology, online article
Helicobacter pylori specifically colonizes the human gastric epithelium and is the major causative agent for ulcer disease and gastric cancer development. Here, we identify members of the carcinoembryonic antigen-related cell adhesion molecule (CEACAM) family as receptors of H. pylori and show that HopQ is the surface-exposed adhesin that specifically binds human ...
10-Oct-2016
Chem. Eur. J.,22, 16433 – 16436, DOI: 10.1002/chem.201604237
Chem. Eur. J., online article
The first example of a bis-hemithioindigo (bis-HTI)-based molecular receptor was realized. Its folding and selective binding affinity for aromatic guest molecules can be precisely controlled by visible light and heat. The thermodynamically stable state of the bis-HTI is the s-shaped planar Z,Z-configuration. After irradiation with 420 nm light only the ...
10-Oct-2016
Nature Cell Biology, 18, 1196–1207, doi:10.1038/ncb3422
Nature Cell Biology, online article
Activation of the ATR kinase following perturbations to DNA replication relies on a complex mechanism involving ATR recruitment to RPA-coated single-stranded DNA via its binding partner ATRIP and stimulation of ATR kinase activity by TopBP1. Here, we discovered an independent ATR activation pathway in vertebrates, mediated by the uncharacterized protein ETAA1 ...
29-Sep-2016
ChemBioChem, DOI: 10.1002/cbic.201600483
ChemBioChem, online article
The receptor tyrosine kinase EPHA2 is overexpressed in several cancer entities (breast, head and neck, non-small cell lung cancer). Small molecule-based inhibition of the activity of the EPHA2 kinase domain (KD) has been seen as an important strategy for achieving therapeutic intervention. However, obtaining structural information by protein crystallography or by ...
28-Sep-2016
Eur. J. Inorg. Chem., DOI: 10.1002/ejic.201600811
Eur. J. Inorg. Chem., online article
Self-assembled coordination cages are interesting as drug-delivery systems. Therefore, the synthesis of new M2L4 (M = Pd, Pt) molecular cages derived from highly fluorescent, rigid polyaromatic ligands is reported herein, and the first Pt2L4 cage with a ligand consisting of three pyridine moieties is described. The photophysical properties were examined, and they ...
27-Sep-2016
Cell Press, Volume 45, Issue 4, p761–773, http://dx.doi.org/10.1016/j.immuni.2016.08.010
Cell Press, online article
Imiquimod is a small-molecule ligand of Toll-like receptor-7 (TLR7) that is licensed for the treatment of viral infections and cancers of the skin. Imiquimod has TLR7-independent activities that are mechanistically unexplained, including NLRP3 inflammasome activation in myeloid cells and apoptosis induction in cancer cells. We investigated the mechanism ...
23-Sep-2016
Nature Communications, 7, Article number: 12852, doi:10.1038/ncomms12852
Nature Communications, online article
Dissecting cellular signalling requires the analysis of large number of proteins. The DigiWest approach we describe here transfers the western blot to a bead-based microarray platform. By combining gel-based protein separation with immobilization on microspheres, hundreds of replicas of the initial blot are created, thus enabling the comprehensive analysis of ...
16-Sep-2016
Biological Chemistry, ISSN (Online) 1437-4315, ISSN (Print) 1431-6730, DOI: 10.1515/hsz-2016-0198
Biological Chemistry, online article
Helicobacter pylori infects the stomach of 50% of the population worldwide, thus causing chronic gastritis. Although this infection can be cured by antibiotic treatment, therapeutic options are increasingly limited due to the development of resistances. The γ-glutamyltranspeptidase (gGT) of Helicobacter pylori (HpgGT) is a virulence factor important for ...
08-Sep-2016
Chem. Eur. J., 22, 1 – 11, DOI: 10.1002/chem.201602784
Chem. Eur. J., online article
Structural features and internal dynamics of inosine-containing RNAs are poorly understood. NMR studies of such RNAs require 13C,15N-labeling, which cannot be achieved using in vitro transcription as inosine and guanosine are not distinguished by RNA polymerase. Herein, we report the synthesis of an inosine phosphoramidite with selective 13C8 and 15N7-isotope ...
08-Sep-2016
Chem. Eur. J., Volume 22, Issue 43, Pages 15350–15359, DOI: 10.1002/chem.201602784
Chem. Eur. J., online article
Structural features and internal dynamics of inosine-containing RNAs are poorly understood. NMR studies of such RNAs require 13C,15N-labeling, which cannot be achieved using in vitro transcription as inosine and guanosine are not distinguished by RNA polymerase. Herein, we report the synthesis of an inosine phosphoramidite with selective 13C8 and 15N7-isotope ...
06-Sep-2016
Bioconjugate Chem., 27 (10), pp 2359–2371, DOI: 10.1021/acs.bioconjchem.6b00369
Bioconjugate Chem., online article
The Ornithodoros moubata Complement Inhibitor (OmCI) binds complement component 5 (C5) with high affinity and, thus, selectively prevents proteolytic activation of the terminal lytic complement pathway. A recombinant version of OmCI (also known as Coversin and rEV576) has proven efficacious in several animal models of complement-mediated diseases and successfully ...
31-Aug-2016
Chem. Commun., 52, 11971-11974, DOI: 10.1039/C6CC05807H
Chem. Commun., online article
N-Acylhomoserine lactones are autoinducers of quorum sensing (QS) in Gram-negative bacteria. We exploit here the role of structurally related β-lactones in the inhibition of Vibrio harveyi bioluminescence and identify a derivative with nanomolar potency. Surprisingly, QS was not affected and combined proteomic/biochemical studies revealed insights into the ...
29-Aug-2016
J. Am. Chem. Soc., 138 (37), pp 12219–12227, DOI: 10.1021/jacs.6b05981
J. Am. Chem. Soc., online article
Controlling the internal motions of molecules by outside stimuli is a decisive task for the generation of responsive and complex molecular behavior and functionality. Light-induced structural changes of photoswitches are of special high interest due to the ease of signal application and high repeatability. Typically photoswitches use one reaction coordinate in ...
29-Aug-2016
Protein Engineering, Design & Selection, vol. 29 no. 12, pp. 557–562, doi: 10.1093/protein/gzw039
Protein Engineering, Design & Selection, online article
To facilitate biocatalytic conversion of the biotechnologically accessible dicyclic dialcohol isosorbide into its industrially relevant diamines, we have designed a fusion protein between two homo-oligomeric enzymes: the levodione reductase (LR) from Leifsonia aquatica and the variant L417M of the ω-aminotransferase from Paracoccus denitrificans (PDωAT(L417M)), ...
25-Aug-2016
Angew. Chem. Int. Ed., Volume 55, Issue 39, Pages 11797–11800, DOI: 10.1002/anie.201605994
Angew. Chem. Int. Ed, online article
5-Formyl-2′-deoxycytosine (fdC) is a recently discovered epigenetic base in the genome of stem cells, with yet unknown functions. Sequencing data show that the base is enriched in CpG islands of promoters and hence likely involved in the regulation of transcription during cellular differentiation. fdC is known to be recognized and excised by the enzyme ...
19-Aug-2016
Org. Lett., DOI: 10.1021/acs.orglett.6b02110
Org. Lett., online article
Investigation of the function of the new epigenetic bases requires the development of stabilized analogues that are stable during base excision repair (BER). Here we report the synthesis of 2′-(R)-fluorinated versions of the phosphoramidites of 5-methylcytosine (mC), 5-hydroxymethylcytosine (hmC), 5-formylcytosine (fC), and 5-carboxycytosine (caC). For ...
17-Aug-2016
Nature, doi:10.1038/nature19081
Nature, online article
Hypermethylation of the promoters of tumour suppressor genes represses transcription of these genes, conferring growth advantages to cancer cells. How these changes arise is poorly understood. Here we show that the activity of oxygen-dependent ten-eleven translocation (TET) enzymes is reduced by tumour hypoxia in human and mouse cells. TET enzymes catalyse DNA ...
12-Aug-2016
PNAS; vol. 113; no.35; E5192-E5201 www.pnas.org/cgi/doi/10.1073/pnas.1603435113
PNAS, online article
Highly pathogenic severe acute respiratory syndrome coronavirus (SARS-CoV) has developed strategies to inhibit host immune recognition. We identify cellular E3 ubiquitin ligase ring-finger and CHY zinc-finger domain-containing 1 (RCHY1) as an interacting partner of the viral SARS-unique domain (SUD) and papain-like protease (PLpro), and, as a consequence, the ...
04-Aug-2016
Nature Communications, 7, Article number: 12418, doi:10.1038/ncomms12418
Nature Communications, online article
Methylation at 5-cytosine (5-mC) is a fundamental epigenetic DNA modification associated recently with cardiac disease. In contrast, the role of 5-hydroxymethylcytosine (5-hmC)—5-mC’s oxidation product—in cardiac biology and disease is unknown. Here we assess the hydroxymethylome in embryonic, neonatal, adult and hypertrophic mouse cardiomyocytes, showing that ...
26-Jul-2016
Biological Chemistry, Band 398, Heft 1, Seiten 39–55, ISSN (Online) 1437-4315, ISSN (Print) 1431-6730, DOI: https://doi.org/10.1515/hsz-2016-0195
Biological Chemistry, online article
Members of the vascular endothelial growth factor receptor (VEGFR) family play a central role in angiogenesis as well as lymphangiogenesis and are crucial for tumor growth and metastasis. In particular, VEGFR-3 expression is induced in endothelial cells during tumor angiogenesis. We report the design of anticalins that specifically recognize the ligand-binding ...
25-Jul-2016
Chem. Eur. J., Volume 22, Issue 31, Pages 10782–10785, DOI : 10.1002/chem.201602438
Chem. Eur. J., online article
Heterocyclic aromatic amines react with purine bases and result in bulky DNA adducts that cause mutations. Such structurally diverse lesions are substrates for the nucleotide excision repair (NER). It is thought that the NER machinery recognises and verifies distorted DNA conformations, also involving the xeroderma pigmentosum group A and C proteins (XPA, XPC) ...
14-Jul-2016
J Nucl Med 2016; 57:1971–1977, DOI: 10.2967/jnumed.116.176784
J Nucl Med, online article
Antibodies have become an established treatment modality in cancer therapy during the last decade. However, these treatments often suffer from insufficient and heterogeneous response despite validated antigen or target receptor expression in the tumor. In fact, therapeutic success depends both on the presence and accessibility of the tumor antigen by the ...
13-Jul-2016
Proteins, Volume 84, Issue 10, Pages 1390–1407, DOI: 10.1002/prot.25084
Proteins, online article
Substrate binding to Hsp70 chaperones is involved in many biological processes, and the identification of potential substrates is important for a comprehensive understanding of these events. We present a multi-scale pipeline for an accurate, yet efficient prediction of peptides binding to the Hsp70 chaperone BiP by combining sequence-based prediction with ...
30-Jun-2016
Org. Lett., 18 (14), pp 3474–3477, DOI: 10.1021/acs.orglett.6b01672
Org. Lett., online article
An operationally simple one-pot reaction for the preparation of a novel class of racemic trifluoromethylated 2,3-dihydro-1H-imidazoles derived from electron-poor N,O-acetals and aryl Grignard reagents is described. In addition, access to highly functionalized 2-trifluoromethyl-2,3-dihydro-1H-imidazoles was accomplished by reaction of N-aryl hemiaminal ethers and ...
27-Jun-2016
Eur. J. Org. Chem., Volume 2016, Issue 22, Pages 3709–3720, DOI: 10.1002/ejoc.201600523
Eur. J. Org. Chem., online article
The decoding of the mechanisms underlying glycan-mediated recognition in disease and health requires access to structurally well-defined oligosaccharides as molecular probes. Owing to their often favourable properties, deoxyfluorosugars have emerged as a promising class of selectively modified carbohydrates for biological and immunological studies. In particular ...
13-Jun-2016
Nature Medicine, 22, 735–743, doi:10.1038/nm.4128
Nature Medicine, online article
Immunomodulatory drugs (IMiDs), such as thalidomide and its derivatives lenalidomide and pomalidomide, are key treatment modalities for hematologic malignancies, particularly multiple myeloma (MM) and del(5q) myelodysplastic syndrome (MDS). Cereblon (CRBN), a substrate receptor of the CRL4 ubiquitin ligase complex, is the primary target by which IMiDs mediate ...
07-Jun-2016
Diabetologia, Volume 59, Issue 9, pp 2005–2012, DOI: 10.1007/s00125-016-4004-6
Diabetologia, online article
Aims/hypothesis
Recombinant leptin offers a viable treatment for lipodystrophy (LD) syndromes. However, due to its short plasma half-life, leptin replacement therapy requires at least daily subcutaneous (s.c.) injections. Here, we optimised this treatment strategy in LD mice by using a novel leptin version with extended plasma half-life using PASylation ...
30-May-2016
Protein Engineering, Design & Selection, vol. 29 no. 7, pp. 263–270, doi: 10.1093/protein/gzw016
Protein Engineering, Design & Selection, online article
ANTICALIgN is an interactive software developed to simultaneously visualize, analyze and modify alignments of DNA and/or protein sequences that arise during combinatorial protein engineering, design and selection. ANTICALIgN combines powerful functions known from currently available sequence analysis tools with unique features for protein engineering, in ...
13-May-2016
Science, Vol. 352, Issue 6287, pp. 833-836, DOI: 10.1126/science.aad2808
The origin of life is believed to have started with prebiotic molecules reacting along unidentified pathways to produce key molecules such as nucleosides. To date, a single prebiotic pathway to purine nucleosides had been proposed. It is considered to be inefficient due to missing regioselectivity and low yields. We report that the condensation of ...
02-May-2016
Proteomics, Volume 16, Issue 10, Pages 1447–1456, DOI 10.1002/pmic.201500523
Proteomics, online article
Phosphorylation is a reversible posttranslational protein modification which plays a pivotal role in intracellular signaling. Despite extensive efforts, phosphorylation site mapping of proteomes is still incomplete motivating the exploration of alternative methods that complement existing workflows. In this study, we compared tandem mass spectrometry (MS/MS) on ...
30-Mar-2016
Biochemical Journal, 473, 1563–1578, doi:10.1042/BCJ20160114
Biochemical Journal, online article
Amyloid beta (Aβ) peptides, in particular Aβ42 and Aβ40, exert neurotoxic effects and their overproduction leads to amyloid deposits in the brain, thus constituting an important biomolecular target for treatments ofAlzheimer’s disease (AD).We describe the engineering of cognate Anticalins as a novel type of neutralizing protein reagent based on the human ...
09-Mar-2016
PROTEINS, Volume 84, Issue 6, Pages 855–858, DOI: 10.1002/prot.25010
PROTEINS, online article
Spirochaeta thermophila secretes seven glycoside hydrolases for plant biomass degradation that carry a carbohydrate-binding module 64 (CBM64) appended at the C-terminus. CBM64 adsorbs to various β1-4-linked pyranose substrates and shows high affinity for cellulose. We present the first crystal structure of a CBM64 at 1.2 Å resolution, which reveals a ...
29-Feb-2016
Nature Genetics, doi:10.1038/ng.3522
The vertebrate body plan and organs are shaped during a conserved embryonic phase called the phylotypic stage. However, the mechanisms that guide the epigenome through this transition and their evolutionary conservation remain elusive. Here we report widespread DNA demethylation of enhancers during the phylotypic period in zebrafish, Xenopus tropicalis and mouse. ...
17-Feb-2016
Nanoscale, 2016, 8, 8101-8110, DOI: 10.1039/C5NR08163G
Effective and controlled drug delivery systems with on-demand release and targeting abilities have received enormous attention for biomedical applications. Here, we describe a novel enzyme-based cap system for mesoporous silica nanoparticles (MSNs) that is directly combined with a targeting ligand via bio-orthogonal click chemistry. The capping system is based on ...
10-Feb-2016
ACS Chem. Biol., 11 (5), pp 1245–1254, DOI: 10.1021/acschembio.5b01063
ACS Chem. Biol., online article
Many protein kinases are valid drug targets in oncology because they are key components of signal transduction pathways. The number of clinical kinase inhibitors is on the rise, but these molecules often exhibit polypharmacology, potentially eliciting desired and toxic effects. Therefore, a comprehensive assessment of a compound’s target space is desirable for a ...
10-Feb-2016
PLOS ONE, DOI:10.1371/journal.pone.0148608
PLOS ONE, online article
The aim of this study was to design, synthesize and validate a multifunctional antidepressant probe that is modified at two distinct positions. The purpose of these modifications was to allow covalent linkage of the probe to interaction partners, and decoration of probe-target complexes with fluorescent reporter molecules. The strategy for the design of such a ...
10-Feb-2016
Quarterly Reviews of Biophysics, 49, e5, pages 1 of 32, doi:10.1017/S0033583515000268
Quarterly Reviews of Biophysics, online article
Nucleotide excision repair (NER) is a highly versatile and efficient DNA repair process, which is responsible for the removal of a large number of structurally diverse DNA lesions. Its extreme broad substrate specificity ranges from DNA damages formed upon exposure to ultraviolet radiation to numerous bulky DNA adducts induced by mutagenic environmental chemicals ...
03-Feb-2016
Eur. J. Org. Chem., Volume 2016, Issue 5, Pages 930–945, DOI: 10.1002/ejoc.201501576
Eur. J. Org. Chem., online article
Much research effort has been devoted to the synthesis of fluorinated organic compounds in medicinal chemistry programs. For instance, incorporation of fluorine substituents and trifluoromethyl groups has become a widespread lead optimization strategy owing to the often favorable influence of such moieties on affinity and physicochemical properties. However, ...
26-Jan-2016
Molecular & Cellular Proteomics, 15, 1424-1434. doi: 10.1074/mcp.M115.052175
Molecular & Cellular Proteomics, online article
The study of male infertility after spinal cord injury (SCI) has enhanced the understanding of seminal plasma (SP) as an important regulator of spermatozoa function. However, the most important factors leading to the diminished sperm motility and viability observed in semen of men with SCI remained unknown. Thus, to explore SP related molecular mechanisms ...
One-Pot Synthesis of Functionalized β-Fluoroalkylated Mannich- Type Products from N-Aryl N,O-Acetals
26-Jan-2016
Synthesis 2016; 48(08): 1167-1176, DOI: 10.1055/s-0035-1561324
Synthesis, online article
A variety of functionalized β-amino-β-fluoroalkyl carbonyl compounds are accessible via a novel one-pot Mannich-type reaction of CF2- and CF3-containing N-aryl N,O-acetals with lithium enolates of ketones, esters, and nitriles. The resulting β-fluoroalkylated β-aminocarbonyl compounds are promising peptide surrogates to be used in drug development and for ...
25-Jan-2016
ACS Chem. Biol., 2016, 11 (4), pp 1082–1089, DOI: 10.1021/acschembio.5b00905
ACS Chem. Biol., online article
The epipolythiodioxopiperazine (ETP) gliotoxin mediates toxicity via its reactive thiol groups and thereby contributes to virulence of the human pathogenic fungus Aspergillus fumigatus. Self-intoxication of the mold is prevented either by reversible oxidation of reduced gliotoxin or by irreversible conversion to bis(methylthio)gliotoxin. The latter is produced by ...
21-Jan-2016
Protein Engineering, Design & Selection, vol. 29 no. 3, pp. 105–115, doi: 10.1093/protein/gzv065
Protein Engineering, Design & Selection, online article
Although prostate carcinoma (PCa) is by far the most commonly diagnosed neoplasia in men, corresponding diagnostic and therapeutic modalities have limited efficacy at present. Anticalins comprise a novel class of binding proteins based on a non-immunoglobulin scaffold that can be engineered to specifically address molecular targets of interest. Here we report the ...
11-Jan-2016
Chem. Eur. J., Volume 22, Issue 14, Pages 4666–4678, DOI: 10.1002/chem.201504419
Chem. Eur. J., online article
Biological selection makes natural products promising scaffolds for drug development and the ever growing number of newly identified, structurally diverse molecules helps to fill the gaps in chemical space. Elucidating the function of a small molecule, such as identifying its protein binding partners, its on- and off-targets, is becoming increasingly important. ...
08-Jan-2016
Chem. Eur. J., Volume 22, Issue 5, Pages 1622–1630, DOI: 10.1002/chem.201503981
Chem. Eur. J., online article
Methicillin-resistant Staphylococcus aureus (MRSA) causes severe infections with only few effective antibiotic therapies currently available. To approach this challenge, chemical entities with a novel and resistance-free mode of action are desperately needed. Here, we introduce a new hydroxyamide compound that effectively reduces the expression of devastating ...