Targeting the activated allosteric conformation of the endothelin receptor B in melanoma with an antibody-drug conjugate: mechanisms and therapeutic efficacy.

Background: Endothelin 1 receptors are one of the drivers of tumor progression in many cancers. Inhibition of their signaling pathways with antagonist drugs has been the subject of numerous clinical trials, but the results have not met expectations probably due to the high endothelin concentrations in the tumor microenvironment and their unusually high affinity for their receptors.

Methods: We previously reported the rendomab B49 antibody (RB49) exhibiting a preferential affinity for the activated conformation of human endothelin B receptor (ET), not displaced by high endothelin levels, and without any pharmacological properties that could inhibit the division of melanoma cells.

Sulfur functionalized diamondoid phosphines enable building nanocomposites interfacing sp-carbon and gold nanolayers.

Interfacing metal frameworks with carbon-based materials is attractive for the bottom-up construction of nanocomposite functional materials. The stepwise layering of difunctionalized diamantanes and gold metal from physical and chemical vapor deposition for the preparation of nanocomposites inverts the conventional preparation of metal-organic frameworks (MOFs) and self-assemblies, where the metal is introduced first, and this method delivers metal surfaces with modified properties originating from the sp-carbon core. However, appropriate diamondoid candidates for such an approach are rare.

Engineering Nickel(II) Porphyrin-Conjugated Polymers with Different Aryl -Substituents for n-Type and p-Type Ammonia Sensors.

Conjugated polymers have revolutionized the field of conductometric gas sensors for sensing toxic gases arising from the fast urbanization and industrialization. In this work, we report the synthesis of a series of 5,15-diaryl Ni(II) porphyrin-conjugated polymers () and their integration as the top layer on an octafluorinated copper phthalocyanine () sublayer to construct bilayer heterojunction (BLH) devices for ammonia sensing. For the first time, we report the pioneering demonstration of polarity engineering within a BLH device by manipulating the -substituent of the 5,15-diaryl Ni(II) porphyrin-conjugated polymer constituting the top layer of the BLH device.

Thieno[3,2-]thiophene-based bridged BODIPY dimers: synthesis, electrochemistry, and one- and two-photon photophysical properties.

Four BODIPY dyes (6a-6d) with electron-donating or electron-withdrawing groups at the -position were synthesized by the Sonogashira coupling reaction of 2,5-diethynylthieno[3,2-]thiophene with mono-iodo-BODIPY moieties. All compounds were fully characterized by H NMR and MALDI-TOF MS. Their photophysical and electrochemical properties were studied by UV-visible absorption spectroscopy, steady-state and time-resolved fluorescence spectroscopy, two-photon excitation spectroscopy and cyclic voltammetry.

In-Depth Study of Ambipolar Charge-Transport Regime through External Triggers and Gas Sensing.

Ambipolar devices are a hot topic in research tables due to their unique advantage in reducing the size of the electrical system and enhancing its efficiency. Here, we report a bilayer heterojunction device constructed using octafluoro-vanadyl-phthalocyanine (VOFPc) and lutetium bisphthalocyanine (LuPc), which exhibits both p- and n-type behaviors under oxidizing (NO and O) and reducing gas (NH) species depending on the humidity level and temperature variations. The initial polarity of the device is identified as n-type by measuring a current decrease under oxygen exposure.

Bifunctional Hexadentate Pyclen-Based Chelating Agent for Mild Radiofluorination in Aqueous Solution at Room Temperature with a Ga-F Ternary Complex.

Positron Emission Tomography (PET) is used in oncology for tumor diagnosis, commonly relying on fluorine-18 (F) emission detection. The conventional method of F incorporation on to probes by covalent bonding is harsh for sensitive biomolecules, which are nonetheless compounds of choice for the development of targeted probes. This study explores gallium-F (GaF) coordination, a milder alternative method occurring in aqueous media at the final stage of radiosyntheses.

Postnatally overfed mice display cardiac function alteration following myocardial infarction.

Background: Cardiovascular (CV) pathologies remain a leading cause of death worldwide, often associated with common comorbidities such as overweight, obesity, type 2 diabetes or hypertension. An innovative mouse model of metabolic syndrome induced by postnatal overfeeding (PNOF) through litter size reduction after birth was developed experimentally. This study aimed to evaluate the impact of PNOF on cardiac remodelling and the development of heart failure following myocardial infarction.

Enantioselective Synthesis of P-Chirogenic 1,2,3-Triazolobenzophospholes.

An enantioselective synthesis of a new class of benzophosphole-based heterocycles bearing a fused triazole ring with enantioselectivities of ≤99% is reported. The key steps of the synthesis are based on an innovative stereospecific phosphinyl N → O migration of aminophosphine-boranes into phosphinites, followed by an intramolecular cyclization. Five X-ray structures of P-chirogenic triazolobenzophospholes and a gold(I) complex were established, for assigning absolute configurations, the stereochemistry of the reactions, and the placement of the triazole substituent at the position of the P center.

PET digitization chain for Monte Carlo simulation in GATE.

. We introduce a versatile methodology for the accurate modelling of PET imaging systems via Monte Carlo simulations, using the Geant4 application for tomographic emission (GATE) platform. Accurate Monte Carlo modelling involves the incorporation of a complete analytical signal processing chain, called the digitizer in GATE, to emulate the different count rates encountered in actual positron emission tomography (PET) systems.

Ambipolar Heterojunction Sensors: Another Way to Detect Polluting Gases.

Gas sensors based on ambipolar materials offer significant advantages in reducing the size of the analytical system and enhancing its efficiency. Here, bilayer heterojunction devices are constructed using different octafluorinated phthalocyanine complexes, with Zn and Co as metal centers, combined with a lutetium bisphthalocyanine complex (LuPc). Stable p-type behavior is observed for the ZnFPc/LuPc device under both electron-donating (NH) and -oxidizing (NO and O) gaseous species, while the CoFPc/LuPc device exhibits n-type behavior under reducing gases and p-type behavior under oxidizing gases.

Small molecular donor materials based on --bridged BODIPY dimers with a triphenylamine or carbazole unit for efficient organic solar cells.

Herein, we have designed and synthesized two novel BODIPY dimer-based small molecules, denoted as ZMH-1 and ZMH-2, covalently linked and functionalized with triphenylamine (TPA) (ZMH-1) and carbazole (C) (ZMH-2) units as the electron donor at the 3- and 5-positions of the BODIPY core, respectively. Their optical and electrochemical properties were investigated. We have fabricated all small molecule bulk heterojunction organic solar cells using these BODIPY-based small molecules as electron donors along with fullerene derivative (PCBM) and medium bandgap non-fullerene acceptor IDT-TC as electron acceptors.

CoCorrole-Functionalized PCN-222 for Carbon Monoxide Selective Adsorption.

The high risk of CO poisoning justifies the need for indoor air quality control and warning systems based on the detection of low concentrations (ppm-ppb) of CO. Cobalt corrole complexes selectively bind CO vs. O, CO, N, opening new fields of applications.

Synthesis and characterization of new acid-functionalized porphyrins displaying antimicrobial activity against gram positive bacteria, yeasts and filamentous fungi with or without ultra-high irradiance.

The antimicrobial activity of new acid-functionalized porphyrins, with or without ultra-high irradiance, was investigated. Antibacterial efficacy was evaluated against Staphylococcus aureus (methicillin-resistant or methicillin-sensitive strains) and antifungal efficacy was evaluated against the yeast Candida albicans and the filamentous fungi Aspergillus fumigatus. Overall, the porphyrins tested are more effective against S.

Multi-modality multi-label ocular abnormalities detection with transformer-based semantic dictionary learning.

Blindness is preventable by early detection of ocular abnormalities. Computer-aided diagnosis for ocular abnormalities is built by analyzing retinal imaging modalities, for instance, Color Fundus Photography (CFP). This research aims to propose a multi-label detection of 28 ocular abnormalities consisting of frequent and rare abnormalities from a single CFP by using transformer-based semantic dictionary learning.

From the Design of Innovative Ti-Pt Heterometallic Complexes to the Development of Highly Anti-Proliferative Water-Soluble Cationic Titanocenes.

Two innovative early/late Ti-Pt-heterobimetallic complexes were synthesized, characterized, and screened in cell-based assays using several human (SW480 and MDA-MB-231) and murine cancer cell lines (CT26 and EMT6) as well as a non-cancerous cell line (HMEC). The combination of the two metals - titanium(IV) and platinum (IV) - in a single molecule led to a synergistic biological activity (higher anti-proliferative properties than a mixture of each of the corresponding monometallic complexes). This study also investigated the benefits of associating a metal-free terpyridine moiety (with intrinsic biological activity) with a water-soluble titanocene fragment.

Phosphonate-substituted porphyrins as efficient, cost-effective and reusable photocatalysts.

Recent advances in visible light photocatalysis represent a significant stride towards sustainable catalytic chemistry. However, its successful implementation in fine chemical production remains challenging and requires careful optimization of available photocatalysts. Our work aims to structurally modify bioinspired porphyrin catalysts, addressing issues related to their laborious synthesis and low solubility, with the goal of increasing their efficiency and developing reusable catalytic systems.

Effects of Visible Light on Gas Sensors: From Inorganic Resistors to Molecular Material-Based Heterojunctions.

In the last two decades, many research works have been focused on enhancing the properties of gas sensors by utilising external triggers like temperature and light. Most interestingly, the light-activated gas sensors show promising results, particularly using visible light as an external trigger that lowers the power consumption as well as improves the stability, sensitivity and safety of the sensors. It effectively eliminates the possible damage to sensing material caused by high operating temperature or high energy light.

Navigating the nuances: comparative analysis and hyperparameter optimisation of neural architectures on contrast-enhanced MRI for liver and liver tumour segmentation.

In medical imaging, accurate segmentation is crucial to improving diagnosis, treatment, or both. However, navigating the multitude of available architectures for automatic segmentation can be overwhelming, making it challenging to determine the appropriate type of architecture and tune the most crucial parameters during dataset optimisation. To address this problem, we examined and refined seven distinct architectures for segmenting the liver, as well as liver tumours, with a restricted training collection of 60 3D contrast-enhanced magnetic resonance images (CE-MRI) from the ATLAS dataset.

Validation of a discovery MI 4-ring model according to the NEMA NU 2-2018 standards: from Monte Carlo simulations to clinical-like reconstructions.

Background: We propose a comprehensive evaluation of a Discovery MI 4-ring (DMI) model, using a Monte Carlo simulator (GATE) and a clinical reconstruction software package (PET toolbox). The following performance characteristics were compared with actual measurements according to NEMA NU 2-2018 guidelines: system sensitivity, count losses and scatter fraction (SF), coincidence time resolution (CTR), spatial resolution (SR), and image quality (IQ). For SR and IQ tests, reconstruction of time-of-flight (TOF) simulated data was performed using the manufacturer's reconstruction software.

π-Extended Porphyrin-Phthalocyanine Heterojunction Devices Exhibiting High Ammonia Sensitivity with a Remarkable Light Effect.

π-Extended porphyrins represent an attractive class of organic compounds because of their unique photophysical, optoelectronic, and physicochemical properties. Herein, cross-conjugated (Ace-PQ-Ni) and linear-conjugated (AM6) porphyrins are used to build double-layer heterojunction devices by combining them with a lutetium bisphthalocyanine complex (LuPc). The heterojunction effect at the porphyrin-phthalocyanine interface plays a key role in the charge transport properties.

Tuning of Interfacial Charge Transport in Organic Heterostructures via Aryl Electrografting for Efficient Gas Sensors.

Modulation of interfacial conductivity in organic heterostructures is a highly promising strategy to improve the performance of electronic devices. In this endeavor, the present work reports the fabrication of a bilayer heterojunction device, combining octafluoro copper phthalocyanine (CuFPc) and lutetium bis-phthalocyanine (LuPc) and tunes the charge transport at the Cu(FPc)-(LuPc) interface by aryl electrografting on the device electrode to improve the device NH-sensing properties. Dimethoxybenzene (DMB) and tetrafluoro benzene (TFB) electrografted by an aryldiazonium electroreduction method form a few-nanometer-thick organic film on ITO.

P(III)-Chirogenic Phosphinite Building Blocks by Stereospecific N→O Phosphinyl Migration.

In the recent past, the chirality borne by a phosphorus center has aroused growing interest in many fields, and the development of new methodologies, notably using inexpensive reagents and simple experimental conditions, has become topical. An efficient stereoselective synthesis of P-chirogenic phosphinites useful as chiral phosphorus building blocks is herein described thanks to a new intramolecular phosphorus rearrangement based on P*(III)-phosphinyl N→O migration. This rearrangement was performed by heating at 50 °C aminophosphine-boranes, easily prepared from chiral amino alcohols, with DABCO in toluene overnight.

Pre-treatment dosimetry inY-SIRT: Is it possible to optimise SPECT reconstruction parameters and calculation methods for accurate dosimetry?

Purpose: The aim of this study was (a) to optimise theTc-SPECT reconstruction parameters for the pre-treatment dosimetry ofY-selective internal radiation therapy (SIRT) and (b) to compare the accuracy of clinical dosimetry methods with full Monte-Carlo dosimetry (fMCD) performed with Gate.

Methods: To optimise the reconstruction parameters, two hundred reconstructions with different parameters were performed on a NEMA phantom, varying the number of iterations, subsets, and post-filtering. The accuracy of the dosimetric methods was then investigated using an anthropomorphic phantom.

Advancing precision oncology through systematic germline and tumor genetic analysis: The oncogenetic point of view on findings from a prospective multicenter clinical trial of 666 patients.

Introduction: With the emergence of targeted therapies, there is a need to accurately identify more tumor biomarkers. The EXOMA trial was designed to offer tumor and germline exome sequencing (ES) to patients with solid malignant tumors and facing therapeutic failure. As hereditary cancer predispositions could be identified, with genetic counseling and health management implications, a genetic consultation was systematically established.