Concept

Non-competitive inhibition

Publications associées (85)

Structural Basis of the Allosteric Inhibition of Human ABCG2 by Nanobodies

Henning Paul-Julius Stahlberg, Dongchun Ni

ABCG2 is an ATP-binding cassette transporter that exports a wide range of xenobiotic compounds and has been recognized as a contributing factor for multidrug resistance in cancer cells. Substrate and inhibitor interactions with ABCG2 have been extensively ...

ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD2023

Role of the cystathionine beta-synthase / H2S pathway in the development of cellular metabolic dysfunction and pseudohypoxia in down syndrome

Theodora Panagaki

Background: Overexpression of the transsulfuration enzyme cystathionine-beta-synthase (CBS), and overproduction of its product, hydrogen sulfide (H2S) are recognized as potential pathogenetic factors in Down syndrome (DS). The purpose of the study was to d ...

ELSEVIER2022

Model-based scale-up of a continuously operated consolidated bioprocess based on a microbial consortium for the production of ethanol

David Beat Dempfle

This work demonstrated that consolidated bioprocessing is a promising concept for conversion of lignocellulose to ethanol at industrial scale. CBP offers great cost saving potential, is feasible to be operated continuously and may be scaled up due to exten ...

EPFL2022

Hetero-Bis-Conjugation of Bioactive Molecules to Half-Sandwich Ruthenium(II) and Iridium(III) Complexes Provides Synergic Effects in Cancer Cell Cytotoxicity

Paul Joseph Dyson, Lucinda Kate Batchelor, Mouna Hadiji

Four bipyridine-type ligands variably derivatized with two bioactive groups (taken from ethacrynic acid, flurbiprofen, biotin, and benzylpenicillin) were prepared via sequential esterification steps from commercial 2,2'-bipyridine-4,4'-dicarboxylic acid an ...

AMER CHEMICAL SOC2021

Treatment and prevention of aging related-disease and/or aging by the inhibition of sphingolipids

Johan Auwerx, Pirkka-Pekka Untamo Laurila

The present invention relates to an inhibitor of sphingolipids for use in the treatment or prevention of an aging related-disease and/or aging. ...

2021

Gαi1 inhibition mechanism of ATP-bound adenylyl cyclase type 5

Ursula Röthlisberger, Siri Camee van Keulen, Daniele Narzi

Conversion of adenosine triphosphate (ATP) to the second messenger cyclic adenosine monophosphate (cAMP) is an essential reaction mechanism that takes place in eukaryotes, triggering a variety of signal transduction pathways. ATP conversion is catalyzed by ...

2021

Crizotinib acts as ABL1 inhibitor combining ATP-binding with allosteric inhibition and is active against native BCR-ABL1 and its resistance and compound mutants BCR-ABL1(T315I) and BCR-ABL1(T315I-E255K)

Oliver Hantschel

Resistance remains the major clinical challenge for the therapy of Philadelphia chromosome-positive (Ph+) leukemia. With the exception of ponatinib, all approved tyrosine kinase inhibitors (TKIs) are unable to inhibit the common "gatekeeper" mutation T315I ...

SPRINGER2021

Non-site on site, représentation métaphorique in situ Projet de parc aux Jeunes-Rives, Neuchâtel

Paradigme de la manufacture de terrains artificiels et de l’avancée des terres sur le lac, le secteur des Jeunes-Rives à Neuchâtel est un véritable earth work. Construit entre 1960 et 1970 à l’aide de 850’000 m3 de remblais provenant de divers façonnages d ...

2020

Inhibition Mechanisms of Indoleamine 2,3-Dioxygenase 1 (IDO1)

Pierre Vogel, Florence Pojer, Somi Reddy Majjigapu

Indoleamine 2,3-dioxygenase 1 (IDO1) catalyzes the rate-limiting step in the kynurenine pathway of tryptophan metabolism, which is involved in immunity, neuronal function, and aging. Its implication in pathologies such as cancer and neurodegenerative disea ...

AMER CHEMICAL SOC2019

Highly sensitive enzymatic MWCNTs-based biosensors for detection of abiraterone in human serum

Giovanni De Micheli, Sandro Carrara, Nima Aliakbarinodehi

A highly-sensitive enzymatic biosensor is successfully experimented for detection of abiraterone in human serum with significance in personalized medicine and point-of-care chemotherapy of patients with metastatic prostate cancer. The dynamic range and lim ...

2018

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