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Concept

Coxib

Publications associées (22)

Modeling tumor size dynamics based on real-world electronic health records and image data in advanced melanoma patients receiving immunotherapy

Federico Amato

The development of immune checkpoint inhibitors (ICIs) has revolutionized cancer therapy but only a fraction of patients benefits from this therapy. Model-informed drug development can be used to assess prognostic and predictive clinical factors or biomark ...

2023

Lanthanide-Based Peptide-Directed Visible/Near-Infrared Imaging and Inhibition of LMP1

Jean-Claude Bünzli, Yue Wu

A lanthanide-based peptide-directed bioprobe LnP19 (Ln = Eu or Yb) is designed as an impressive example of a small molecule-based dual-functional probe for the EBV oncoprotein LMP1. The peptide P19 (Pra-KAhx-K-LDLALK-FWLY-K-IVMSDKW-K-RrRK) is designed to s ...

AMER CHEMICAL SOC2021

An Oculus to Profile and Probe Target Engagement In Vivo: How T-REX Was Born and Its Evolution into G-REX

Yimon Aye, Chloé Rogg

Here we provide a personal account of innovation and design principles underpinning a method to interrogate precision electrophile signaling that has come to be known as "REX technologies". This Account is framed in the context of trying to improve methods ...

American Chemical Society2021

Selective inhibition of STAT3 signaling using monobodies targeting the coiled-coil and N-terminal domains

Oliver Hantschel, Florence Pojer, Kelvin Ka Ching Lau, Tim Kükenshöner, Grégory La Sala

The transcription factor STAT3 is frequently activated in human solid and hematological malignancies and remains a challenging therapeutic target with no approved drugs to date. Here, we develop synthetic antibody mimetics, termed monobodies, to interfere ...

Nature Research2020

Atroxlysin-III, A Metalloproteinase from the Venom of the Peruvian Pit Viper Snake Bothrops atrox (Jergon) Induces Glycoprotein VI Shedding and Impairs Platelet Function

Augusto Martins Lima

Atroxlysin-III (Atr-III) was purified from the venom of Bothrops atrox. This 56-kDa protein bears N-linked glycoconjugates and is a P-III hemorrhagic metalloproteinase. Its cDNA-deduced amino acid sequence reveals a multidomain structure including a propro ...

2019

Activation of the STING-dependent type I interferon response reduces microglial reactivity and neuroinflammation

Hilal Lashuel, Ritwik Burai

Brain aging and neurodegeneration are associated with prominent microglial reactivity and activation of innate immune response pathways, commonly referred to as neuroinflammation. One such pathway, the type I interferon response, recognizes viral or mitoch ...

Cell Press2017

Generation and Characterization of Anti-VGLUT Nanobodies Acting as Inhibitors of Transport

The uptake of glutamate by synaptic vesicles is mediated by vesicular glutamate transporters (VGLUTs). The central role of these transporters in excitatory neurotransmission underpins their importance as pharmacological targets. Although several compounds ...

Amer Chemical Soc2017

Peptide macrocycle inhibitor of coagulation factor XII with subnanomolar affinity and high target selectivity

Christian Heinis, Jonas Alfred Karl Wilbs, Simon Jan Middendorp

Factor XII (FXII) is a plasma protease that has emerged in recent years as a potential target to treat or prevent pathological thrombosis, to inhibit contact activation in extracorporeal circulation, and to treat the swelling disorder hereditary angioedema ...

2017

Inflammatory lymphangiogenesis in postpartum breast tissue remodeling

Melody Swartz

Like many cancers, mammary carcinomas use lymphatic vessels to disseminate, and numerous clinical and experimental studies have documented a strong correlation between peritumoral lymphangiogenesis and tumor dissemination. At the same time, many other fact ...

American Society for Clinical Investigation2014

Continuous monitoring of Naproxen by a cytochrome P450-based electrochemical sensor

Giovanni De Micheli, Sandro Carrara, Camilla Baj-Rossi, Andrea Cavallini

This paper reports the characterization of an electrochemical biosensor for the continuous monitoring of Naproxen based on cytochrome P450. The electrochemical biosensor is based on the drop-casting of multi-walled carbon-nanotubes (MWCNTs) and microsomal ...

Elsevier2014

DprE1-from the Discovery to the Promising Tuberculosis Drug Target

Joao Pedro De Almeida Neres

Several groups working in the field of the development of new antituberculosis drugs have recently reported active compounds targeting mycobacterial enzyme DprE1. Along with its counterpart, DprE2, it catalyses a unique epimerization reaction resulting in ...

Bentham Science Publ Ltd2014

Multitarget Drug Discovery for Tuberculosis and Other Infectious Diseases

Stewart Cole, Benoit Lechartier

We report the discovery of a series of new drug leads that have potent activity against Mycobacterium tuberculosis as well as against other bacteria, fungi, and a malaria parasite. The compounds are analogues of the new tuberculosis (TB) drug SQ109 (1), wh ...

Amer Chemical Soc2014

Identification of MAGI1 as a tumor-suppressor protein induced by cyclooxygenase-2 inhibitors in colorectal cancer cells

Cyclooxyganase-2 (COX-2), a rate-limiting enzyme in the prostaglandin synthesis pathway, is overexpressed in many cancers and contributes to cancer progression through tumor cell-autonomous and paracrine effects. Regular use of non-steroidal anti-inflammat ...

2012

An integrative in silico methodology for the identification of modulators of macrophage migration inhibitory factor (MIF) tautomerase activity

Hilal Lashuel, Bruno Claude Daniel Fauvet

Macrophage migration inhibitory factor (MIF) is a major proinflammatory cytokine that has been increasingly implicated in the pathogenesis of several inflammatory, autoimmune, infectious and oncogenic diseases. Accumulating evidence suggests that the tauto ...

Elsevier2010

Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC

Ruben Hartkoorn

center dot Antiretroviral protease inhibitors such as lopinavir and saquinavir have been shown to be substrates of ABCB1. Co-administration with the potent ABCB1 and CYP3A4 inhibitor, ritonavir, has shown improved pharmacokinetics and subsequent therapeuti ...

2009

Thioredoxin reductase: A target for gold compounds acting as potential anticancer drugs

Angela Casini

The thioredoxin system plays a key role in regulating the overall intracellular redox balance. It basically comprises the small redox protein thioredoxin (Trx), nicotinamide adenine dinucleotide phosphate, in its reduced form (NADPH), and thioredoxin reduc ...

2009

Fetal cells for intervertebral disc regeneration

Degeneration of the intervertebral disc (IVD) is thought to be one main factor in the development of back pain. It is not a symptom by itself but can lead to painful pathological conditions. Current treatments aim at relieving pain by conservative care, me ...

EPFL2009

Combination therapy using aspirin-enhanced photodynamic selective drug delivery

Hubert van den Bergh, Elodie Debefve

In photodynamic therapy (PDT), excitation of a drug by light leads to a cascade of biochemical processes that can cause closure of blood vessels. It has been observed clinically that significant short-term leakage from the irradiated vasculature can occur ...

Elsevier2007

Development of new anticancer agents based on [alpha]-mannosidase inhibition

Hélène Fiaux

Enzymes that are involved in the synthesis and processing of oligosaccharides, such as glycosidases, are important catalysts for the specific assembly of oligosaccharide structures on proteins. Design and preparation of selective inhibitors of these enzyme ...

EPFL2007

Pyrrolidine derivatives as new inhibitors of alpha-mannosidases and growth inhibitors of human cancer cells

Pierre Vogel, Sandrine Gerber, Hélène Fiaux

New pyrrolidine-3,4-diol derivatives were prepared from D-(-)- and L(+)-phenylglycinol and tested for their ability to inhibit 25 commercial glycosidases. The influence of the substitution of the lateral side chain and of the pyrrolidine ring on the enzyme ...

2006