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Studies of Glutathione Transferase P1-1 Bound to a Platinum(IV)-Based Anticancer Compound Reveal the Molecular Basis of Its Activation

Publications associées (76)

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A Photoactivatable Probe for Super-Resolution Imaging of Enzymatic Activity in Live Cells

Pablo Rivera Fuentes, Zacharias Thiel, Nils Trapp

A dual-activatable, fluorogenic probe was developed to sense esterase activity with single-mol. resoln. Without enzymic preactivation, the diazoindanone-based probe has an electron-poor core and, upon irradn., undergoes Wolff rearrangement to give a ring-e ...

2017

Site-Specific Polymer Attachment to HR2 Peptide Fusion Inhibitors against HIV-1 Decreases Binding Association Rates and Dissociation Rates Rather Than Binding Affinity

Harm-Anton Klok, Frederik Roman Wurm, Maarten Danial

A popular strategy for overcoming the limited plasma half-life of peptide heptad repeat 2 (HR2) fusion inhibitors against HIV-1 is conjugation with biocompatible polymers such as poly(ethylene glycol) (PEG). However, despite improved resistance to proteoly ...

2017

Alkaline phosphatase-fused repebody as a new format of immuno-reagent for an immunoassay

Oliver Hantschel

Enzyme-linked immunoassays based on an antibody-antigen interaction are widely used in biological and medical sciences. However, the conjugation of an enzyme to antibodies needs an additional chemical process, usually resulting in randomly cross-linked mol ...

Elsevier2016

Metal-based drugs that break the rules

Paul Joseph Dyson, Claire Samantha Allardyce

Cisplatin and other platinum compounds have had a huge impact in the treatment of cancers and are applied in the majority of anticancer chemotherapeutic regimens. The success of these compounds has biased the approaches used to discover new metal-based ant ...

2016

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Tryptophan metabolites in the kynurenine pathway are up-regulated by pro-inflammatory cytokines or glucocorticoids, and are linked to anti-inflammatory and immunosuppressive activities. In addition, they are up-regulated in pathologies such as cancer, auto ...

Amer Soc Biochemistry Molecular Biology Inc2015

Mono layer graphene field-effect sensors operating in liquid have been widely deployed for detecting a range of analyte species often under equilibrium conditions. Here we report on the real-time detection of the binding kinetics of the essential human enz ...

Amer Chemical Soc2015

Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Pierre Vogel, Somi Reddy Majjigapu

Since the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) as an attractive target for anticancer therapy in 2003, the search for inhibitors has been intensely pursued both in academia and in pharmaceutical companies. Many novel IDO1 inhibitor scaffolds h ...

Amer Chemical Soc2015

Background Mycetoma is a neglected, chronic, and deforming infectious disease caused by fungi and actinomycetes. In Mexico, N. brasiliensis is the predominant etiologic agent. Therapeutic alternatives are necessary because the current drug regimens have se ...

Public Library of Science2015

Field-portable optofluidic plasmonic biosensor for wide-field and label-free monitoring of molecular interactions

Hatice Altug, Arif Engin Cetin

We demonstrate a field-portable optofluidic plasmonic sensing device, weighing 40 g and 7.5 cm in height, which merges plasmonic microarrays with dual-wavelength lensfree on-chip imaging for real-time monitoring of protein binding kinetics. ...

IEEE2015

Reaction Mechanism and Catalytic Fingerprint of Allantoin Racemase

Matteo Dal Peraro, Marco Stenta, Thomas Lemmin, Matteo Thomas Degiacomi, Christophe Bovigny

The stereospecific oxidative decomposition of urate into allantoin is the core of purine catabolism in many organisms. The spontaneous decomposition of upstream intermediates and the nonenzymatic racemization of allantoin lead to an accumulation of (R)-all ...

Amer Chemical Soc2014