Concept

Pharmacophore

Publications associées (24)

Cyclic Peptides for Drug Development

Christian Heinis, Xinjian Ji, Alexander Lund Nielsen

Cyclic peptides combine a number of favorable properties that make them attractive for drug development. Today, more than 40 therapeutics based on cyclic peptides are in use, and new, powerful technologies for their development suggest that this number cou ...

2024

The combination of palladium salts and bipyridyl ligands can lead to the formation of a large variety of coordination complexes, with different shapes and sizes, displaying a very versatile host-guest chemistry. Increasing their structural complexity remai ...

EPFL2024

Multiple Surface Site Three-Dimensional Structure Determination of a Supported Molecular Catalyst

Moreno Lelli, Pierrick Berruyer, David Benjamin Roger Antoine Gajan, Zhuoran Wang

The structural characterization of supported molecular catalysts is challenging due to the low density of active sites and the presence of several organic/organometallic surface groups resulting from the often complex surface chemistry associated with supp ...

AMER CHEMICAL SOC2022

Protein Engineering, especially protein post-translational modification (PTM), ex-tends proteomes in a more complex way than one can expect from analysis of their encod-ing genomes. It can activate or deactivate certain catalytic functions, add new desired ...

EPFL2022

Chiral Alkyl Amine Synthesis via Catalytic Enantioselective Hydroalkylation of Enecarbamates

Xile Hu, Srikrishna Bera, Deyun Qian

Chiral alkyl amines are omnipresent as bioactive molecules and synthetic intermediates. The catalytic and enantioselective synthesis of alkyl amines from readily accessible precursors is challenging. Here we develop a nickel-catalyzed hydroalkylation metho ...

AMER CHEMICAL SOC2021

Synthesis of New Indole and Adamantane Amido Derivatives with Pharmacological Interest

Stewart Cole, Anthony Vocat

The synthesis and preliminary pharmacological evaluation of new indole and adamantane amido derivatives is described. The design was based on the pharmacophoric properties of 4-{4-[4-(trifluoromethoxy)phenoxy]piperidin-1-yl), 6-[4-(trifluoro methoxy)phenyl ...

WILEY-V C H VERLAG GMBH2019

Synthesis of DNA‐encoded disulfide‐ and thioether‐cyclized peptides

Christian Heinis, Van Manh Pham

DNA-encoded chemical library technologies enable the screening of large combinatorial libraries of chemically and structurally diverse molecules, including short cyclic peptides. A challenge in the combinatorial synthesis of cyclic peptides is the final st ...

2019

Allosteric regulation and targeting of Abl SH2-kinase interface and other cytoplasmic tyrosine kinases

Allan Joaquim Lamontanara

Due to their central role in normal cellular physiology, the activity of protein kinases is tightly regulated and their aberrant activation can lead to cancer. Chronic myelogenous leukemia (CML) is a blood cancer characterized by unregulated growth of myel ...

EPFL2016

Preclinical combination therapy of the investigational drug NAMI-A(+) with doxorubicin for mammary cancer

Paul Joseph Dyson, Tina Riedel, Gianni Sava

Aim of the study The tumor metastases targeting ruthenium complex NAMI-A synergistically improves the activity of gemcitabine in combination therapies. High-throughput screening was used to identify other potential drug combinations from a library of FDA a ...

Springer2015

New proposal for production of bioactive compounds by supercritical technology integrated to a sugarcane biorefinery

François Maréchal, Adriano Viana Ensinas

The construction of a supercritical fluid extraction (SFE) plant inside or in close proximity to a sugarcane biorefinery producing first and second generation ethanol demonstrated to be very promising, increasing the economic potential of the SFE process i ...

Springer Verlag2014

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