Publications by Christian Heinis

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The present invention relates to a cyclic inhibitor of a kallikrein protease comprising or consisting of (I) the peptide (X)(X)(X)R(X)(X)(X)(X)(X)(X)(X)(X) (Formula (X)), wherein (X) is present or absent and, is prefer ...

Newer solid-phase peptide synthesis and release strategies enable the production of short peptides with high purity, allowing direct screening for desired bioactivity without prior chromatographic purification. However, the maximum number of peptides that ...

Cyclic peptides binding to targets of interest can be generated efficiently with powerful in vitro display techniques, such as phage display or mRNA display. The cyclic peptide libraries screened with these methods are generated by altering in a combinator ...

Many naturally occurring cyclic peptides or derivatives thereof are used as therapeutics such as the human hormones vasopressin and oxytocin or the antibiotics vancomycin and daptomycin. The success of cyclic peptide therapeutics is based on their ability ...

Two polar hinges for cyclization of peptides have been developed, leading to bicyclic peptides and cyclized peptides with improved solubility and biological activity. Increasingly, we note that a good aqueous solubility of peptides is an absolute prerequis ...

A conjugate which is capable of specific binding to and inhibition of urokinase-type plasminigen activator (UPA) comprising a polypeptide molecule and a scaffold molecule, wherein said polypeptide molecule is attached to said scaffold molecule by at least ...

Naturally evolved peptides, such as the hormone oxytocin or the anti-bacterial vancomycin, have seen decades of success as powerful therapeutics due to many of the favorable properties of peptides. Not every desired target has a naturally occurring bioacti ...

The present invention relates to a method for preparing a library of peptides or an isolated peptide comprising (a) releasing one or more linear dithiol peptides carrying a sulfhydryl group in the N-terminal region of the one or more peptides and being imm ...

The specific reaction of O6-alkylguanine-DNA alkyltransferase (AGT) with O6-benzylguanine (BG) derivatives allows for a specific labeling of AGT fusion proteins with chemically diverse compounds in living cells and in vitro. The efficiency of the labeling ...

Peptide 3 is an 18‐amino acid linear peptide binding with sub‐micromolar affinity to the inflammation marker calprotectin. Its application in point‐of‐care diagnostic assays has shown promising results, yet improving its affinity for calprotectin could fac ...

Kallikrein-related peptidases 5 (KLK5) and 7 (KLK7) are serine proteases with homeostatic functions in the epidermis that play a critical role in Netherton syndrome (NS), a rare yet life-threatening genetic disorder that currently lacks specific treatment. ...

The visualization of complex cellular processes involving multiple proteins requires the use of spectroscopically distinguishable fluorescent reporters. We have previously introduced the SNAP-tag as a general tool for the specific labeling of SNAP-tag fusi ...

Christian Heinis

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Novel inhibitors of kallikrein proteases and uses thereof

Solid-phase peptide synthesis in 384-well plates

Improving the binding affinity of in-vitro-evolved cyclic peptides by inserting atoms into the macrocycle backbone

Directed Evolution of Bicyclic Peptides for Therapeutic Application

Chemical Biology and Drug Discovery Symposium at the LS2 Annual Meeting 2021

Polar Hinges as Functionalized Conformational Constraints in (Bi) cyclic Peptides

Polypeptide inhibitors of urokinase type plasminogen activator

Drugs Based on de novo-developed Peptides are Coming of Age

Method for preparing a library of peptides or a peptide

Biodiversity2Drugs—Renaissance of exploring nature‐derived peptides for GPCR ligand discovery

Directed evolution of O6-alkylguanine-DNA alkyltransferase for applications in protein labeling

Structure‐affinity relationship analysis and affinity maturation of a calprotectin‐binding peptide

Development of protease-resistant peptide ligands for oral delivery

Chemical biology & drug discovery

Phage Display Selected Cyclic Peptide Inhibitors of Kallikrein-Related Peptidases 5 and 7 and Their In Vivo Delivery to the Skin

Towards the development of orally available cyclic peptides

Does spatial propagation of blood coagulation predict FXI bleeding phenotype?

An engineered protein tag for multi-protein labeling in living cells

Evolving the substrate specificity of O6-alkylguanine-DNA alkyltransferase through loop insertion for applications in molecular imaging

The Partnership of DMCCB and LS2