Concept
Inhibiteur compétitif
Publications associées (110)
Antibody-peptide conjugates for targeted inhibition of cysteine proteases
We developed a rational approach to design peptide-based covalent inhibitors and coupled the inhibitors with antibodies for cell-specific delivery. We used this platform to generate antibody-peptide inhibitor conjugates (APICs) that target a family of prot ...
Nature Portfolio2024Structural 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 LTD2023A molecular device for the redox quality control of GroEL/ES substrates
Camille Véronique Bernadette Goemans
Hsp60 chaperonins and their Hsp10 cofactors assist protein folding in all living cells, constituting the paradigmatic example of molecular chaperones. Despite extensive investigations of their structure and mechanism, crucial questions regarding how these ...
2023Hetero-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 SOC2021Crizotinib 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)
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 ...
SPRINGER2021Microbial Ecology of Methanotrophy in Streams Along a Gradient of CH4 Availability
Tom Ian Battin, Hannes Markus Peter, Paraskevi Pramateftaki, Alexandre Bagnoud
Despite the recognition of streams and rivers as sources of methane (CH4) to the atmosphere, the role of CH4 oxidation (MOX) in these ecosystems remains poorly understood to date. Here, we measured the kinetics of MOX in stream sediments of 14 sites to res ...
2020