COX-2 inhibitor

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

Olivier Michielin, Federico Amato, Monia Guidi, Nadia Terranova, Daniel Abler, Alexandre Wicky

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 ...

AMER CHEMICAL SOC2021

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

Florence Pojer, Kelvin Ka Ching Lau, Oliver Hantschel, 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

Andrea Volterra

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, Andrea Cavallini, Camilla Baj-Rossi

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

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