Melanocortin-4 receptor antagonist TCMCB07 alleviates chemotherapy-induced anorexia and weight loss in rats.

Cancer patients undergoing chemotherapy often experience anorexia and weight loss that substantially deteriorates overall health, reduces treatment tolerance and quality of life, and worsens oncologic outcomes. There are currently few effective therapeutic options to mitigate these side effects. The central melanocortin system, which plays a pivotal role in regulating appetite and energy homeostasis, presents a logical target for treating anorexia and weight loss.

Dual-emission rare-earth fluorescent nanomaterials for ratiometric and visual detection of N-acetylneuraminic acid and applications in information encryption and anti-counterfeiting.

N-acetylneuraminic acid (NANA) can be used as a biomarker for many types of cancers. Currently, there are various methods for detecting NANA but showing some shortcomings that limit the real-time diagnosis of cancer. In contrast, fluorescence analysis has obvious advantages such as low cost, fast response time, and easy operation, and it also enables visual detection for real-time cancer monitoring.

Developing a Novel Enzalutamide-Resistant Prostate Cancer Model via AR F877L Mutation in LNCaP Cells.

Prostate cancer is a leading diagnosis and major cause of cancer-related deaths in men worldwide. As a typical hormone-responsive disease, prostate cancer is commonly managed with androgen deprivation therapy (ADT) to curb its progression and potential metastasis. Unfortunately, progression to castration-resistant prostate cancer (CRPC), a notably more aggressive phase of the disease, occurs within a timeframe of 2-3 years following ADT.

A smartphone-intergrated dual-emission fluorescent nanoprobe for visual and ratiometric detection of anthrax biomarkers.

A novel dual-emission fluorescent nanoprobe based on rare-earth nanosheets was fabricated to detect 2,6-pyridine dicarboxylic acid (DPA), which is the biomarker of Bacillus anthracis. 2-amino terephthalic acid (BDC-NH) and surfactant sodium dodecyl sulfate (SDS) were co-intercalated into layered europium hydroxide (LEuH) to prepare the organic/inorganic composite, which was delaminated to obtain the rare-earth nanosheets. The ratio detection of DPA is possible due to the antenna effect between DPA and Eu.

Fabrication of a ratiometric fluorescence nanoprobe for detecting tryptophan enantiomers.

A novel ratiometric fluorescence nanoprobe was developed to detect tryptophan enantiomers with high selectivity and sensitivity. Fluorescein (FL) was doped into SiO nanoparticles with little dye leakage, acting as an internal reference signal. The chiral center of L-histidine (L-His) was introduced by partially replacing the carboxyl on the surface of SiO.

A core-shell structure ratiometric fluorescent probe based on carbon dots and Tb for the detection of anthrax biomarker.

A novel core-shell structure ratiometric fluorescent probe was developed, which can selectively and sensitively detect 2,6-dipicolinic acid (DPA) as an anthrax biomarker. Carbon dots (CDs) was embedded into SiO nanoparticles, which was acted as an internal reference signal. Tb with green emission was connected to the carboxyl functionalized SiO, which was acted as a responsive signal.

Fluorescence on and off sensing platform based on europium nanosheets for the detection of DPA and Cu ions.

With the development of society, the modern environment has put forward higher requirements for analysis and detection. This work proposes a new strategy for the construction of fluorescent sensors based on rare-earth nanosheets. Organic/inorganic composites were obtained by the intercalation of 4,4'-stilbene dicarboxylic acid (SDC) into layered europium hydroxide, and then the composites were exfoliated to form nanosheets.

Fluoroalkane modified cationic polymers for personalized mRNA cancer vaccines.

Messenger RNA (mRNA) vaccines, while demonstrating great successes in the fight against COVID-19, have been extensively studied in other areas such as personalized cancer immunotherapy based on tumor neoantigens. In addition to the design of mRNA sequences and modifications, the delivery carriers are also critical in the development of mRNA vaccines. In this work, we synthesized fluoroalkane-grafted polyethylenimine (F-PEI) for mRNA delivery.

DNA Engineered Lymphocyte-Based Homologous Targeting Artificial Antigen-Presenting Cells for Personalized Cancer Immunotherapy.

Artificial antigen-presenting cells (aAPCs) constructed by integrating T cell activation ligands on biocompatible materials hold great potential in tumor immunotherapy. However, it remains challenging to develop aAPCs, which could mimic the characteristics of natural APCs, thereby realizing antigen-specific T cells activation . Here, we report the first effort to construct natural lymphocyte-based homologous targeting aAPCs (LC-aAPCs) with lipid-DNA-mediated noninvasive live cell surface engineering.

Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD).

We previously described the discovery of a novel indole series compounds as oral SERD for ER positive breast cancer treatment. Further SAR exploration focusing on substitutions on indole moiety of compound 12 led to the discovery of a clinical candidate LX-039. We report herein its profound anti-tumor activity, desirable ER antagonistic characteristics combined with favorable pharmacokinetic and preliminary safety properties.

Rare-Earth hydroxide nanosheets based ratio fluorescence nanoprobe for dipicolinic acid detection.

We demonstrate a novel ratio fluorescence nanoprobe for dipicolinic acid (DPA) as an anthrax biomarker based on layered rare-earth hydroxide (LRH). 3-Amino-benzenesulfonic acid (AS) was intercalated into layered terbium hydroxide to form composite and then delaminated into nanosheets in formamide. The monolayer nanosheets were beneficial to expose the Ln luminescence centers to the environment more completely, contributing a high sensitive detection to the environment.

Effect of polyfluoroalkyl chemicals on the occurrence of urge urinary incontinence: a population-based study.

Background: The artificial fluorinated group of compounds polyfluoroalkyl chemicals (PFCs) has been applied extensively in daily life for decades, and is present in food, drinking water, and indoor dust. The nephrotoxicity of PFCs has been widely studied for its characteristics of being mainly excreted through passing urine and affecting urodynamics. This work aimed to investigate the relationship between PFCs and the occurrence of urge urinary incontinence (UUI) in the United States (US) population.

Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD).

Most estrogen receptor positive (ER +) breast cancers depend on ER signaling pathway to develop. Clinical application of SERD fulvestrant effectively degraded ER, blocked its function and prolonged progression free survival of ER + breast cancer patients. However, current SERD suffers from limited bioavailability, therefore is given as intramuscular (IM) injection.

Tissue-specific transcription reprogramming promotes liver metastasis of colorectal cancer.

Metastasis, the development of secondary malignant growths at a distance from a primary tumor, is the cause of death for 90% of cancer patients, but little is known about how metastatic cancer cells adapt to and colonize new tissue environments. Here, using clinical samples, patient-derived xenograft (PDX) samples, PDX cells, and primary/metastatic cell lines, we discovered that liver metastatic colorectal cancer (CRC) cells lose their colon-specific gene transcription program yet gain a liver-specific gene transcription program. We showed that this transcription reprogramming is driven by a reshaped epigenetic landscape of both typical enhancers and super-enhancers.

Co-Al nanosheets derived from LDHs and their catalytic performance for syngas conversion.

Layered double hydroxides (LDHs) were innovatively employed in this study as catalyst for synthesis gas conversion to chemicals, such as oxygenates. Cobalt-aluminium layered double hydroxides (Co-Al LDHs) was prepared at different temperatures. and lactate was successfully intercalated into the LDHs by ion-exchange method and then the material was further delaminated in water at ambient temperature.

The Hippo pathway effector TAZ induces TEAD-dependent liver inflammation and tumors.

The Hippo signaling pathway regulates organ size and plays critical roles in maintaining tissue growth, homeostasis, and regeneration. Dysregulated in a wide spectrum of cancers, in mammals, this pathway is regulated by two key effectors, YAP and TAZ, that may functionally overlap. We found that TAZ promoted liver inflammation and tumor development.

Nanostructured Layered Terbium Hydroxide Containing NASIDs: Physicochemical and Biological Evaluations.

Diclofenac sodium (abrr. DS) and indomethacin (abrr. IMC) have been intercalated into the layered terbium hydroxide (LTbH) by anion exchange method.

Antitumor effects of regorafenib and sorafenib in preclinical models of hepatocellular carcinoma.

The purpose of this study was to investigate the antitumor activity of regorafenib and sorafenib in preclinical models of HCC and to assess their mechanism of action by associated changes in protein expression in a HCC-PDX mouse model. Both drugs were administered orally once daily at 10 mg/kg (regorafenib) or 30 mg/kg (sorafenib), which recapitulate the human exposure at the maximally tolerated dose in mice. In a H129 hepatoma model, survival times differed significantly between regorafenib versus vehicle (p=0.

Establishing a patient-derived xenograft model of human myxoid and round-cell liposarcoma.

Myxoid and round cell liposarcoma (MRCL) is a common type of soft tissue sarcoma. The lack of patient-derived tumor xenograft models that are highly consistent with human tumors has limited the drug experiments for this disease. Hence, we aimed to develop and validate a patient-derived tumor xenograft model of MRCL.

Aldehyde dehydrogenase-2 (ALDH2) opposes hepatocellular carcinoma progression by regulating AMP-activated protein kinase signaling in mice.

Unlabelled: Potential biomarkers that can be used to determine prognosis and perform targeted therapies are urgently needed to treat patients with hepatocellular carcinoma (HCC). To meet this need, we performed a screen to identify functional genes associated with hepatocellular carcinogenesis and its progression at the transcriptome and proteome levels. We identified aldehyde dedydrogenase-2 (ALDH2) as a gene of interest for further study.

Fabrication of a nano-drug delivery system based on layered rare-earth hydroxides integrating drug-loading and fluorescence properties.

We demonstrate the first example of intercalation of naproxen (abbr. NPX) into layered europium hydroxide (LEuH) and investigate the structure, chemical composition, thermostability, morphology, luminescence properties, cytotoxic effect, and controlled-release behaviors. Different deprotonation degrees lead to NPX-LEuH composites with diverse structures (horizontal or vertical arrangement), and the thermal stability of organics is enhanced after intercalation.

Activating JAK1 mutation may predict the sensitivity of JAK-STAT inhibition in hepatocellular carcinoma.

Hepatocellular carcinoma (HCC) is the fifth most common type of cancers worldwide. However, current therapeutic approaches for this epidemic disease are limited, and its 5-year survival rate hasn't been improved in the past decades. Patient-derived xenograft (PDX) tumor models have become an excellent in vivo system for understanding of disease biology and drug discovery.

Genomic characterization of a large panel of patient-derived hepatocellular carcinoma xenograft tumor models for preclinical development.

Lack of clinically relevant tumor models dramatically hampers development of effective therapies for hepatocellular carcinoma (HCC). Establishment of patient-derived xenograft (PDX) models that faithfully recapitulate the genetic and phenotypic features of HCC becomes important. In this study, we first established a cohort of 65 stable PDX models of HCC from corresponding Chinese patients.

Controllable luminescence of layered rare-earth hydroxide composites with a fluorescent molecule: blue emission by delamination in formamide.

We demonstrate the first example of exfoliated layered europium hydroxide (LEuH) composites with a fluorescent molecule that exhibit blue luminescence. Co-quenching in the solid state, blue emission (440 nm) in formamide, and green emission (514 nm) in water-formamide were found, for which delamination and swollen states account for the versatile luminescence behaviors.