Concept

Biological target

Related publications (117)

Bicyclic peptide ligands pulled out of cysteine-rich peptide libraries

Christian Heinis, Petr Leiman, Shiyu Chen, Jeremy Touati, Julia Morales Sanfrutos

Bicyclic peptide ligands were found to have good binding affinity and target specificity. However, the method applied to generate bicyclic ligands based on phage-peptide alkylation is technically complex and limits its application to specialized laboratori ...

2013

Polycyclic Peptide Therapeutics

Christian Heinis, Vanessa Baeriswyl

Owing to their excellent binding properties, high stability, and low off-target toxicity, polycyclic peptides are an attractive molecule format for the development of therapeutics. Currently, only a handful of polycyclic peptides are used in the clinic; ex ...

Wiley-V C H Verlag Gmbh2013

Phage selection of bicyclic peptides

Christian Heinis, Inmaculada Rentero Rebollo

Bicyclic peptides are small, constrained peptides that can bind with high affinity and selectivity to protein targets. Their small size provides a number of advantages over larger protein-based ligands, including access to chemical synthesis, better tissue ...

Academic Press Inc Elsevier Science2013

Functional single-cell hybridoma screening using droplet-based microfluidics

Christoph Merten

Monoclonal antibodies can specifically bind or even inhibit drug targets and have hence become the fastest growing class of human therapeutics. Although they can be screened for binding affinities at very high throughput using systems such as phage display ...

2012

Cell biology: a key driver of therapeutic innovation

Oliver Hantschel

All processes associated with cellular function are likely to contribute to disease. Particularly in the cancer field, most major therapeutic innovations have originated from the elucidation of basic molecular mechanisms by academic researchers. Recent bre ...

2012

Automated design of ligands to polypharmacological profiles

Daniel Constam

The clinical efficacy and safety of a drug is determined by its activity profile across many proteins in the proteome. However, designing drugs with a specific multi-target profile is both complex and difficult. Therefore methods to design drugs rationally ...

Nature Publishing Group2012

The Angiotensin-Converting Enzyme 2/Angiotensin-(1-7)/Mas receptor axis: A potential target for treating thrombotic diseases

Nikolaos Stergiopoulos, Danielle Gomes Passos Silva

Despite many therapeutic advances leading to increasingly effective drug treatments, thrombotic events (such as ischaemic stroke, pulmonary embolism, deep venous thrombosis and acute myocardial infarction) still represent a major worldwide cause of morbidi ...

Schattauer Gmbh-Verlag Medizin Naturwissenschaften2012

DprE1 as a Drug Target from Mycobacterium Tuberculosis

Claudia Trefzer

Benzothiazinones (BTZs) form a new class of potent antimycobacterial agents with a minimal inhibitory concentration of 1 ng/mL against Mycobacterium tuberculosis. Although the target of BTZs has been identified as decaprenylphosphoryl--D-ribose 2- oxidase ...

EPFL2012

Calibration and use of the polar organic chemical integrative sampler-a critical review

The implementation of strict environmental quality standards for polar organic priority pollutants poses a challenge for monitoring programs. The polar organic chemical integrative sampler (POCIS) may help to address the challenge of measuring low and fluc ...

Society of Environmental Toxicology and Chemistry Press2012

Structure and function of the transketolase from Mycobacterium tuberculosis and comparison with the human enzyme

Stewart Cole, Florence Pojer, Elizabeth Fullam

The transketolase (TKT) enzyme in Mycobacterium tuberculosis represents a novel drug target for tuberculosis treatment and has low homology with the orthologous human enzyme. Here, we report on the structural and kinetic characterization of the transketola ...

Royal Soc2012

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