Horst Kessler

Solution structure and binding specificity of the p63 DNA binding domain.

Docking studies on alphavbeta3 integrin ligands: pharmacophore refinement and implications for drug design.

New oxazole-based peptidomimetics: useful building blocks for the synthesis of orthogonally protected macrocyclic scaffolds.

Synthesis and structure-activity relationship of mannose-based peptidomimetics selectively blocking integrin alpha4beta7 binding to mucosal addressin cell adhesion molecule-1.

[18F]Galacto-RGD: synthesis, radiolabeling, metabolic stability, and radiation dose estimates.

Evidence for hetero-association of transmembrane helices of integrins.

Expression of the GM2-activator protein in the methylotrophic yeast Pichia pastoris, purification, isotopic labeling, and biophysical characterization.

Combination of an SRC kinase inhibitor with a novel pharmacological antagonist of the urokinase receptor diminishes in vitro colon cancer invasiveness.

An easy and scalable method for the partial alignment of organic molecules for measuring residual dipolar couplings.

Backbone 1H, 15N and 13C resonance assignments of alpha-ADT and beta-ADT.

Activation of integrin function by nanopatterned adhesive interfaces.

NMR studies on the substrate-binding domains of the thermosome: structural plasticity in the protrusion region.

Two-step methodology for high-yield routine radiohalogenation of peptides: (18)F-labeled RGD and octreotide analogs.

First (18)F-labeled tracer suitable for routine clinical imaging of sst receptor-expressing tumors using positron emission tomography.

A structural model of EmrE, a multi-drug transporter from Escherichia coli.

1H, 13C and 15N resonance assignment of the nucleotide binding domain of KdpB from Escherichia coli.

A computational model of transmembrane integrin clustering.

Human integrin alphavbeta5: homology modeling and ligand binding.

Solution structure of Escherichia coli Par10: The prototypic member of the Parvulin family of peptidyl-prolyl cis/trans isomerases.

Inter-domain motions of the N-domain of the KdpFABC complex, a P-type ATPase, are not driven by ATP-induced conformational changes.

Stretched poly(dimethylsiloxane) gels as NMR alignment media for apolar and weakly polar organic solvents: an ideal tool for measuring RDCs at low molecular concentrations.

Improving implant materials by coating with nonpeptidic, highly specific integrin ligands.

ADAM15 decreases integrin alphavbeta3/vitronectin-mediated ovarian cancer cell adhesion and motility in an RGD-dependent fashion.

Stretched poly(vinyl acetate) gels as NMR alignment media for the measurement of residual dipolar couplings in polar organic solvents.

NMR studies reveal structural differences between the gallium and yttrium complexes of DOTA-D-Phe1-Tyr3-octreotide.

Noninvasive visualization of the activated alphavbeta3 integrin in cancer patients by positron emission tomography and [18F]Galacto-RGD.

Structure-activity relationship studies optimizing the antiproliferative activity of novel cyclic somatostatin analogues containing a restrained cyclic beta-amino acid.

Stretched gelatin gels as chiral alignment media for the discrimination of enantiomers by NMR spectroscopy.

Orientational properties of stretched polystyrene gels in organic solvents and the suppression of their residual 1H NMR signals.

Convenient synthesis of N-methylamino acids compatible with Fmoc solid-phase peptide synthesis.

Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists.

Cooperative binding of p53 to DNA: regulation by protein-protein interactions through a double salt bridge.

Diffusion NMR spectroscopy: folding and aggregation of domains in p53.

Structure refinement of cyclosporin A in chloroform by using RDCs measured in a stretched PDMS-gel.

Optimized selective N-methylation of peptides on solid support.

Titanium implant materials with improved biocompatibility through coating with phosphonate-anchored cyclic RGD peptides.

3-Substituted indolizine-1-carbonitrile derivatives as phosphatase inhibitors.

Benzylprotected aromatic phosphonic acids for anchoring peptides on titanium.

Photoswitched cell adhesion on surfaces with RGD peptides.

Molecular targeting with peptides or peptide-polymer conjugates: just a question of size?

The holo-form of the nucleotide binding domain of the KdpFABC complex from Escherichia coli reveals a new binding mode.

WT p53, but not tumor-derived mutants, bind to Bcl2 via the DNA binding domain and induce mitochondrial permeabilization.

Intrinsic inhibition of the Hsp90 ATPase activity.

Cellular unbinding forces of initial adhesion processes on nanopatterned surfaces probed with magnetic tweezers.

Lateral spacing of integrin ligands influences cell spreading and focal adhesion assembly.

Characterization of human saposins by NMR spectroscopy.

Prokaryotic Kdp-ATPase: recent insights into the structure and function of KdpB.

Growth promoting in vitro effect of synthetic cyclic RGD-peptides on human osteoblast-like cells attached to cancellous bone.

Solid-phase synthesis of 1,3-azole-based peptides and peptidomimetics.

Synthesis and stereochemical assignment of DNA spore photoproduct analogues.

Binding of small mono- and oligomeric integrin ligands to membrane-embedded integrins monitored by surface plasmon-enhanced fluorescence spectroscopy.

Positron emission tomography using [18F]Galacto-RGD identifies the level of integrin alpha(v)beta3 expression in man.

Inter-domain orientation and motions in VAT-N explored by residual dipolar couplings and 15N backbone relaxation.

Efficient enantioselective synthesis of condensed and aromatic-ring-substituted tyrosine derivatives.

p53--a natural cancer killer: structural insights and therapeutic concepts.

The conformation of cyclo(-D-Pro-Ala4-) as a model for cyclic pentapeptides of the DL4 type.

Influence of the internal disulfide bridge on the folding pathway of the CL antibody domain.

N-methylated cyclic pentaalanine peptides as template structures.

J-Spectroscopy in the presence of residual dipolar couplings: determination of one-bond coupling constants and scalable resolution.

Cell spreading and focal adhesion dynamics are regulated by spacing of integrin ligands.

Probing integrin selectivity: rational design of highly active and selective ligands for the alpha5beta1 and alphavbeta3 integrin receptor.

Mimicking cellular environments by nanostructured soft interfaces.

Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).

Synthesis of novel 1,4,7,10-tetraazacyclodecane-1,4,7,10-tetraacetic acid (DOTA) derivatives for chemoselective attachment to unprotected polyfunctionalized compounds.

The RGD motif in fibronectin is essential for development but dispensable for fibril assembly.

NMR-based screening: a powerful tool in fragment-based drug discovery.

Development of a peptidomimetic ligand for efficient isolation and purification of factor VIII via affinity chromatography.

Protein repellent properties of covalently attached PEG coatings on nanostructured SiO(2)-based interfaces.

Design and chemical synthesis of integrin ligands.

Specific integrin labeling in living cells using functionalized nanocrystals.

Development and evaluation of peptidic ligands targeting tumour-associated urokinase plasminogen activator receptor (uPAR) for use in alpha-emitter therapy for disseminated ovarian cancer.

J-ONLY-TOCSY: efficient suppression of RDC-induced transfer in homonuclear TOCSY experiments using JESTER-1-derived multiple pulse sequences.

Multiple N-methylation by a designed approach enhances receptor selectivity.

Conformational preference and potential templates of N-methylated cyclic pentaalanine peptides.

Assessment of alphavbeta3 integrin expression after myocardial infarction by positron emission tomography.

Improving oral bioavailability of peptides by multiple N-methylation: somatostatin analogues.

Phosphorus NMR spectroscopy as a versatile tool for compound library screening.

Chemical conjugation of linear and cyclic RGD moieties to a recombinant elastin-mimetic polypeptide--a versatile approach towards bioactive protein hydrogels.

The CLIP/CLAP-HSQC: pure absorptive spectra for the measurement of one-bond couplings.

Biophysics: the sweetest candy for the virus.

Isothiocyanate-functionalized RGD peptides for tailoring cell-adhesive surface patterns.

Rational design of highly active and selective ligands for the alpha5beta1 integrin receptor.

Induction of cell polarization and migration by a gradient of nanoscale variations in adhesive ligand spacing.

Cell adhesion and polarisation on molecularly defined spacing gradient surfaces of cyclic RGDfK peptide patches.

N-methylation of peptides: a new perspective in medicinal chemistry.

Cooperativity in adhesion cluster formation during initial cell adhesion.

The structure of a folding intermediate provides insight into differences in immunoglobulin amyloidogenicity.

The solution structure of BMPR-IA reveals a local disorder-to-order transition upon BMP-2 binding.

Can N-methylated amino acids serve as substitutes for prolines in conformational design of cyclic pentapeptides?

Deuterated polymer gels for measuring anisotropic NMR parameters with strongly reduced artefacts.

The state of the art of chemical biology.

Perspectives on NMR in drug discovery: a technique comes of age.

Interaction of human heat shock protein 70 with tumor-associated peptides.

Impact of order and disorder in RGD nanopatterns on cell adhesion.

Breaking the dogma of the metal-coordinating carboxylate group in integrin ligands: introducing hydroxamic acids to the MIDAS to tune potency and selectivity.

Solid-phase synthesis of phosphinic dipepetide isosteres and beta amino acids via activated N-terminal acrylamides.

N-methylated cyclic pentapeptides as template structures.

Development of a small molecule peptidomimetic affinity ligand for efficient purification of the large protein factor VIII.

Making double-minded peptides strong-willed? The side chain impact on the backbone conformation of N-methylated cyclic pentapeptides.

Highly selective cyclic hexapeptides antagonist of GPIIb-IIIa by multiple N-methylation.

New perspective in peptide chemistry by N-alkylation.

Imaging of integrin alpha(v)beta(3) expression in patients with malignant glioma by [18F] Galacto-RGD positron emission tomography.

The HSP90 binding mode of a radicicol-like E-oxime determined by docking, binding free energy estimations, and NMR 15N chemical shifts.

Ligands for mapping alphavbeta3-integrin expression in vivo.

Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of beta-secretase (BACE1).

An unfolded CH1 domain controls the assembly and secretion of IgG antibodies.

The transmembrane structure of integrin alphaIIbbeta3: significance for signal transduction.

Hsp90 is regulated by a switch point in the C-terminal domain.

BclxL changes conformation upon binding to wild-type but not mutant p53 DNA binding domain.

Asymmetric activation of the hsp90 dimer by its cochaperone aha1.

The impact of amino acid side chain mutations in conformational design of peptides and proteins.

A conserved spider silk domain acts as a molecular switch that controls fibre assembly.

Multiple N-methylation of MT-II backbone amide bonds leads to melanocortin receptor subtype hMC1R selectivity: pharmacological and conformational studies.

Hsp12 is an intrinsically unstructured stress protein that folds upon membrane association and modulates membrane function.

Polymeric substrates with tunable elasticity and nanoscopically controlled biomolecule presentation.

Conformational control of integrin-subtype selectivity in isoDGR peptide motifs: a biological switch.

Optimized measurement temperature gives access to the solution structure of a 49 kDa homohexameric β-propeller.

Stimulation of cell adhesion at nanostructured teflon interfaces.

pH-dependent dimerization and salt-dependent stabilization of the N-terminal domain of spider dragline silk--implications for fiber formation.

NCO-sP(EO-stat-PO) surface coatings preserve biochemical properties of RGD peptides.

Stable functionalized PEGylated quantum dots micelles with a controlled stoichiometry.

Cilengitide: the first anti-angiogenic small molecule drug candidate design, synthesis and clinical evaluation.

The effect of multiple N-methylation on intestinal permeability of cyclic hexapeptides.

Impact of local versus global ligand density on cellular adhesion.

PET Imaging of Integrin αVβ3 Expression.

Cell interactions with hierarchically structured nano-patterned adhesive surfaces.

PET imaging of CXCR4 receptors in cancer by a new optimized ligand.

Telethonin deficiency is associated with maladaptation to biomechanical stress in the mammalian heart.

Introducing lasso peptides as molecular scaffolds for drug design: engineering of an integrin antagonist.

Structural analysis of the interaction between Hsp90 and the tumor suppressor protein p53.

Design, synthesis, and functionalization of dimeric peptides targeting chemokine receptor CXCR4.

Increasing αvβ3 selectivity of the anti-angiogenic drug cilengitide by N-methylation.

PET of CXCR4 expression by a (68)Ga-labeled highly specific targeted contrast agent.

Synthesis and conformational analysis of efrapeptins.

Tailoring of integrin ligands: probing the charge capability of the metal ion-dependent adhesion site.

Spectroscopically well-characterized RGD optical probe as a prerequisite for lifetime-gated tumor imaging.

The architecture of functional modules in the Hsp90 co-chaperone Sti1/Hop.

Polymer-free immobilization of a cyclic RGD peptide on a nitinol stent promotes integrin-dependent endothelial coverage of strut surfaces.

Synthesis of N-methylated cyclic peptides.

Solid-phase-assisted synthesis of targeting peptide-PEG-oligo(ethane amino)amides for receptor-mediated gene delivery.

68Ga-NODAGA-RGD is a suitable substitute for (18)F-Galacto-RGD and can be produced with high specific activity in a cGMP/GRP compliant automated process.

Cyclic aza-peptide integrin ligand synthesis and biological activity.

Guiding plant virus particles to integrin-displaying cells.

Cell adhesion and proliferation on RGD-modified recombinant spider silk proteins.

Intestinal permeability of cyclic peptides: common key backbone motifs identified.

A conformationally frozen peptoid boosts CXCR4 affinity and anti-HIV activity.

Improvement of drug-like properties of peptides: the somatostatin paradigm.

Behavior of primary human osteoblasts on trimmed and sandblasted Ti6Al4V surfaces functionalized with integrin αvβ3-selective cyclic RGD peptides.

In support of the BMRB.

The regulatory domain stabilizes the p53 tetramer by intersubunit contacts with the DNA binding domain.

N-methylation of peptides and proteins: an important element for modulating biological functions.

Orthogonally protected artificial amino acid as tripod ligand for automated peptide synthesis and labeling with [(99m)Tc(OH(2))(3)(CO)(3)](+).

FOSL1 controls the assembly of endothelial cells into capillary tubes by direct repression of αv and β3 integrin transcription.

Functionalizing αvβ3- or α5β1-selective integrin antagonists for surface coating: a method to discriminate integrin subtypes in vitro.

Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids.

A cyclen-based tetraphosphinate chelator for the preparation of radiolabeled tetrameric bioconjugates.

Comparison of cyclic RGD peptides for αvβ3 integrin detection in a rat model of myocardial infarction.

The glycophorin A transmembrane sequence within integrin αvβ3 creates a non-signaling integrin with low basal affinity that is strongly adhesive under force.

A molecular toolkit for the functionalization of titanium-based biomaterials that selectively control integrin-mediated cell adhesion.

Hydrogel micropillars with integrin selective peptidomimetic functionalized nanopatterned tops: a new tool for the measurement of cell traction forces transmitted through αvβ3- or α5β1-integrins.

Tumor Targeting via Integrin Ligands.

Integrin modulators: a patent review.

Selective imaging of the angiogenic relevant integrins α5β1 and αvβ3.

The cyclic cystine ladder of theta-defensins as a stable, bifunctional scaffold: A proof-of-concept study using the integrin-binding RGD motif.

PET/CT imaging of integrin αvβ3 expression in human carotid atherosclerosis.

Investigation of early cell-surface interactions of human mesenchymal stem cells on nanopatterned β-type titanium-niobium alloy surfaces.

Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity.

Benefits of NOPO as chelator in gallium-68 peptides, exemplified by preclinical characterization of (68)Ga-NOPO-c(RGDfK).

The integrin ligand c(RGDf(NMe)Nal) reduces neointimal hyperplasia in a polymer-free drug-eluting stent system.

Single cell tracking assay reveals an opposite effect of selective small non-peptidic α5β1 or αvβ3/β5 integrin antagonists in U87MG glioma cells.

N-Methylated sst2 Selective Somatostatin Cyclic Peptide Analogue as a Potent Candidate for Treating Neurogenic Inflammation.

Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.

Protein folding by interaction.

Cytoplasmic salt bridge formation in integrin αvß3 stabilizes its inactive state affecting integrin-mediated cell biological effects.

Receptor-bound conformation of cilengitide better represented by its solution-state structure than the solid-state structure.

Direct prediction of residual dipolar couplings of small molecules in a stretched gel by stochastic molecular dynamics simulations.

Mimicking bone extracellular matrix: integrin-binding peptidomimetics enhance osteoblast-like cells adhesion, proliferation, and differentiation on titanium.

Interface Immobilization Chemistry of cRGD-based Peptides Regulates Integrin Mediated Cell Adhesion.

Disclosing the CXCR4 expression in lymphoproliferative diseases by targeted molecular imaging.

Hsp90 regulates the dynamics of its cochaperone Sti1 and the transfer of Hsp70 between modules.

Enantiomeric cyclic peptides with different Caco-2 permeability suggest carrier-mediated transport.

Segregation versus colocalization: orthogonally functionalized binary micropatterned substrates regulate the molecular distribution in focal adhesions.

Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.

Minimal synthetic cells to study integrin-mediated adhesion.

cis-Peptide Bonds: A Key for Intestinal Permeability of Peptides? .

Caveolin-1-negative head and neck squamous cell carcinoma primary tumors display increased epithelial to mesenchymal transition and prometastatic properties.

In vivo biokinetic and metabolic characterization of the ⁶⁸Ga-labelled α5β1-selective peptidomimetic FR366.

Complementary, Selective PET Imaging of Integrin Subtypes α5β1 and αvβ3 Using 68Ga-Aquibeprin and 68Ga-Avebetrin.

Stable Peptides Instead of Stapled Peptides: Highly Potent αvβ6-Selective Integrin Ligands.

Small Cause, Great Impact: Modification of the Guanidine Group in the RGD Motif Controls Integrin Subtype Selectivity.

Substrate engagement of integrins α5β1 and αvβ3 is necessary, but not sufficient, for high directional persistence in migration on fibronectin.

Selective binding and lateral clustering of α5β1 and αvβ3 integrins: Unraveling the spatial requirements for cell spreading and focal adhesion assembly.

Non-invasive assessment of inter-and intrapatient variability of integrin expression in metastasized prostate cancer by PET.

The influence of different metal-chelate conjugates of pentixafor on the CXCR4 affinity.

Variation of Specific Activities of 68Ga-Aquibeprin and 68Ga-Avebetrin Enables Selective PET Imaging of Different Expression Levels of Integrins α5β1 and αvβ3.

αvβ3- or α5β1-Integrin-Selective Peptidomimetics for Surface Coating.

Rational Design of Cyclic Peptide Inhibitors of U2AF Homology Motif (UHM) Domains To Modulate Pre-mRNA Splicing.

Integrin-Targeted Hybrid Fluorescence Molecular Tomography/X-ray Computed Tomography for Imaging Tumor Progression and Early Response in Non-Small Cell Lung Cancer.

In Vivo PET Imaging of the Cancer Integrin αvβ6 Using (68)Ga-Labeled Cyclic RGD Nonapeptides.

A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins.