Publications associées à Inhibiteur compétitif

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 Portfolio2024

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

Beyond worst-case analysis, with or without predictions

Andreas Maggiori

In this thesis we design online combinatorial optimization algorithms for beyond worst-case analysis settings. In the first part, we discuss the online matching problem and prove that, in the edge arrival model, no online algorithm can achieve a competiti ...

EPFL2023

Low temperature and mTOR inhibition favor stem cell maintenance in human keratinocyte cultures

Kai Johnsson, Yann Barrandon, Johannes Alexander Mosig, Thomas Michael Braschler, Ariane Rochat, Jean-Baptiste Bureau, Fahd Azzabi Zouraq, Mako Kamiya

Adult autologous human epidermal stem cells can be extensively expanded ex vivo for cell and gene therapy. Identifying the mechanisms involved in stem cell maintenance and defining culture conditions to maintain stemness is critical, because an inadequate ...

WILEY2023

Microfluidic device combining hydrodynamic and dielectrophoretic trapping for the controlled contact between single micro-sized objects and application to adhesion assays

Philippe Renaud, Arnaud Bertsch, Clémentine Sophie Sarah Lipp

The understanding of cell-cell and cell-matrix interactions via receptor and ligand binding relies on our ability to study the very first events of their contact. Of particular interest is the interaction between a T cell receptor and its cognate peptide-m ...

ROYAL SOC CHEMISTRY2023

A 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 ...

2023

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

Alternative dimerization is required for activity and inhibition of the HEPN ribonuclease RnlA

Gabriela Garcia Rodriguez

The rnlAB toxin-antitoxin operon from Escherichia co/ifunctions as an anti-phage defense system. RnlA was identified as a member of the HEPN (Higher Eukaryotes and Prokaryotes Nucleotide-binding domain) superfamily of ribonucleases. The activity of the tox ...

OXFORD UNIV PRESS2021

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

Novel broad-spectrum virucidal antivirals

Matteo Gasbarri

The current COVID-19 pandemic has showed the threats that viruses can cause to the whole world. Over 200 million infections and over 4.5 million deaths and enormous socio-economic impact were the output of the emergence of a single new pathogen: SARS-CoV-2 ...

EPFL2021

A high-throughput cell- and virus-free assay shows reduced neutralization of SARS-CoV-2 variants by COVID-19 convalescent plasma

Didier Trono, Priscilla Turelli, Florence Pojer, Charlène Mireille Raymonde Raclot, Valeria Cagno, Jérémy Campos, Céline Pellaton

The detection of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)-specific antibodies in the serum of an individual indicates previous infection or vaccination. However, it provides limited insight into the protective nature of this immune resp ...

AMER ASSOC ADVANCEMENT SCIENCE2021

Engineering of ecological niches to create stable artificial consortia for complex biotransformations

Jeremy Luterbacher

The design of controllable artificial microbial consortia has attracted considerable interest in recent years to capitalize on the inherent advantages in comparison to monocultures such as the distribution of the metabolic burden by division of labor, the ...

2020

Microbial 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 ...

Frontiers Media SA2020

Nano-sized iron oxides supported on polyester textile to remove fluoroquinolones in hospital wastewater

Sami Rtimi

In this study, we examined the removal kinetics of two fluoroquinolones (FQs), flumequine (FLU) and ciprofloxacin (CIP), in synthetic wastewater (SWW) and real hospital wastewater (RHW) using FeOx thin films, peroxymonosulfate (PMS) and visible light. Nano ...

ROYAL SOC CHEMISTRY2020

Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms

Matteo Dal Peraro, Florence Pojer, Sandrine Madeleine Suzanne Georgeon, Maria Josefina Marcaida Lopez, Oliver Hantschel, Allan Joaquim Lamontanara, Tim Kükenshöner, Daniel Pereira Duarte, Grégory La Sala

Bruton's tyrosine kinase (Btk) is critical for B-cell maturation and activation. Btk loss-of-function mutations cause human X-linked agammaglobulinemia (XLA). In contrast, Btk signaling sustains growth of several B-cell neoplasms which may be treated with ...

Nature Publishing Group2020

The (h, k)-Server Problem on Bounded Depth Trees

Marek Elias

We study the k-server problem in the resource augmentation setting, i.e., when the performance of the online algorithm with k servers is compared to the offline optimal solution with h

ASSOC COMPUTING MACHINERY2019

Nested Convex Bodies are Chaseable

Marek Elias

In the Convex Body Chasing problem, we are given an initial point v0. Rd and an online sequence of n convex bodies F1,..., Fn. When we receive Ft, we are required to move inside Ft. Our goal is to minimize the total distance traveled. This fundamental onli ...

SPRINGER2020

A novel psychoanalytical approach: An electrochemical ligand-binding assay to screen antipsychotics

Sandro Carrara, Tugba Kilic

Schizophrenia treatment may see a paradigm shift due to development of new atypical antipsychotic drugs (APDs), with better tolerability due to more selective dopamine (DA) receptor blockade. Monitoring of these APD candidates in biological fluids is of gr ...

2018

Photoinduced disinfection in sunlit natural waters: Measurement of the second order inactivation rate constants between E-coli and photogenerated transient species

César Pulgarin, Stefanos Giannakis, Jean Arnaud Troyon

This work uncovers the implications of the estimation of exogenous inactivation rates for E. coli after the initial lag phase, and presents a strategy for the determination of the second-order inactivation rate constants (k2nd) of these bacteria with relev ...

PERGAMON-ELSEVIER SCIENCE LTD2018

Reactive species monitoring and their contribution for removal of textile effluent with photocatalysis under UV and visible lights: Dynamics and mechanism

Sami Rtimi

In this study, the photocatalytic activities were investigated for the treatment of Reactive Green 12 (RG 12) solution under UV and visible irradiation using Cu doped TiO2, and TiO2 impregnated on (1) cellulose and (2) UV-C activated polyester catalysts. T ...

ELSEVIER SCIENCE SA2018