Publications by Alessandro Zorzi

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

Luc Reymond, Christian Heinis, Alessandro Zorzi, Mischa Schüttel, Vanessa Carle, Tamara Maric, Patrick Andreas Gonschorek

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. ...

AMER CHEMICAL SOC2022

Molecular analysis and therapeutic applications of human serum albumin-fatty acid interactions

Alessandro Angelini, Alessandro Zorzi, Sara Linciano

Human serum albumin (hSA) is the major carrier protein for fatty acids (FAs) in plasma. Its ability to bind multiple FA moieties with moderate to high affinity has inspired the use of FA conjugation as a safe and natural platform to generate long-lasting t ...

ELSEVIER2022

Picomole-Scale Synthesis and Screening of Macrocyclic Compound Libraries by Acoustic Liquid Transfer

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Alessandro Zorzi, Gontran Sangouard, Julien Bortoli Chapalay, Sangram Shivdas Kale, Mischa Schüttel, Yu Teng Wu, Cristina Diaz Perlas

Macrocyclic compounds are an attractive class of therapeutic ligands against challenging targets, such as protein-protein interactions. However, the development of macrocycles as drugs is hindered by the lack of large combinatorial macrocyclic libraries, w ...

Wiley-VCH Verlag GmbH2021

Novel inhibitors of kallikrein proteases and uses thereof

Christian Heinis, Alessandro Zorzi, Patrick Andreas Gonschorek

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 ...

2021

Novel inhibitors of kallikrein proteases and uses thereof

Christian Heinis, Alessandro Zorzi, Patrick Andreas Gonschorek

The present invention relates to a cyclic inhibitor of a kallikrein protease comprising or consisting of (I) the peptide (X1 (X2)(X3)R(X4)(X5)(X6)(X7)(X8)(X9)(X10)(X11) (Formula (X)), wherein (X1) is present or absent and, is preferably present, and if pre ...

2021

A releasable disulfide-linked peptide tag facilitates the synthesis and purification of short peptides

Christian Heinis, Alessandro Zorzi, Yu Teng Wu, Jack Peter Christopher Williams

Combinatorial cyclization of hundreds to thousands of random linear peptides by structurally diverse chemical linkers offers access to large macrocyclic compound libraries. A bottleneck in the development of such libraries is the preparation of large numbe ...

Royal Society of Chemistry2020

Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Alessandro Angelini, Alessandro Zorzi, Julien Bortoli Chapalay, Sangram Shivdas Kale, Kaycie Marie Butler, Ganesh Kumar Mothukuri, Carl Leonard Stenbratt

Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three ...

2020

Non-covalent albumin-binding ligands for extending the circulating half-life of small biotherapeutics

Alessandro Angelini, Alessandro Zorzi, Sara Linciano

Peptides and small protein scaffolds are gaining increasing interest as therapeutics. Similarly to full-length antibodies, they can bind a target with a high binding affinity and specificity while remaining small enough to diffuse into tissues. However, de ...

ROYAL SOC CHEMISTRY2019

Cyclization of peptides with two chemical bridges affords large scaffold diversities

Christian Heinis, Alessandro Zorzi, Camille Villequey, Sangram Shivdas Kale, Xudong Kong

2018

Acylated heptapeptide binds albumin with high affinity and application as tag furnishes long-acting peptides

Christian Heinis, Alessandro Zorzi, Jonas Alfred Karl Wilbs, Simon Jan Middendorp, Kaycie Marie Butler

The rapid renal clearance of peptides in vivo limits this attractive platform for the treatment of a broad range of diseases that require prolonged drug half-lives. An intriguing approach for extending peptide circulation times works through a 'piggy-back' ...

Nature Research2017

Cyclic peptide therapeutics: past, present and future

Christian Heinis, Alessandro Zorzi, Kaycie Marie Butler

Cyclic peptides combine several favorable properties such as good binding affinity, target selectivity and low toxicity that make them an attractive modality for the development of therapeutics. Over 40 cyclic peptide drugs are currently in clinical use an ...

2017

Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics

Alessandro Zorzi

Peptides represent a promising format for the development of therapeutics since they combine the advantages of proteins and small molecules. Several techniques based on rational design or in vitro evolution can be used to develop peptides as therapeutics. ...

EPFL2017

A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation

Christian Heinis, Shiyu Chen, Vanessa Baeriswyl, Alessandro Zorzi, Luca Bologna

Coagulation factor XII (FXII) inhibitors are of interest for the study of the protease in the intrinsic coagulation pathway, for the suppression of contact activation in blood coagulation assays, and they have potential application in antithrombotic therap ...

American Chemical Society2015