Kerstinginone, a new flavanone derivative from Commiphora kerstingii Engl. (Burseraceae) with potent apoptosis-inducing activity and inhibition of AKT/mTOR signaling pathway in non-sensitive prostate cancer cells.

Ethnopharmacological Relevance: Commiphora kerstingii Engl is a tree which is 20-30 m in height and commonly called "ararrabi" in Hausa. It is found in the Sahelian region (Cameroon, Chad, and Nigeria) where it is utilized for the treatment of several ailments including cancer.

Aim Of The Study: This study was aimed at investigating the chemical constituents and cytotoxic effect of extracts and isolates from the stem barks and leaves of C.

Comprehensive transcriptomic analysis of prostate cancer lung metastases.

Metastatic prostate cancer (mPCa) is a widespread disease with high mortality. Unraveling molecular mechanisms of disease progression is of utmost importance. The microenvironment in visceral organs and the skeletal system is of particular interest as a harbinger of metastatic spread.

Genome editing in plants using the TnpB transposase system.

Unlabelled: The widely used clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated nuclease (Cas) system is thought to have evolved from IS200/IS605 transposons. TnpB proteins, encoded by one type of IS200/IS605 transposon, are considered to be the evolutionary ancestors of Cas12 nucleases, which have been engineered to function as RNA-guided DNA endonucleases for genome editing in bacteria and human cells. TnpB nucleases, which are smaller than Cas nucleases, have been engineered for use in genome editing in animal systems, but the feasibility of this approach in plants remained unknown.

CEACAM6 Promotes Lung Metastasis Enhancing Proliferation, Migration and Suppressing Apoptosis of Prostate Cancer Cells.

Background/aim: Metastatic prostate cancer (mPCa) results in high morbidity and mortality. Visceral metastases in particular are associated with a shortened survival. Our aim was to unravel the molecular mechanisms that underly pulmonary spread in mPCa.

[Therapy sequences and duration in mCRPC: a retrospective review of the Lübeck mCRPC cohort].

Background: Prostate cancer is one of the most common cancers in men in Europe. Several classes of agents can be considered for the treatment of metastatic prostate carcinoma, and their use is supported by extensive guidelines. In the treatment of metastatic castration-resistant prostate cancer (mCRPC), it is currently unclear which sequence of systemic therapies is most effective.

Catalyst-free late-stage functionalization to assemble α-acyloxyenamide electrophiles for selectively profiling conserved lysine residues.

Covalent probes coupled with chemical proteomics represent a powerful method for investigating small molecule and protein interactions. However, the creation of a reactive warhead within various ligands to form covalent probes has been a major obstacle. Herein, we report a convenient and robust process to assemble a unique electrophile, an α-acyloxyenamide, through a one-step late-stage coupling reaction.

Multifunctional Biomass-Based Ionic Liquids/CuCl-Catalyzed CO-Promoted Hydration of Propargylic Alcohols: A Green Synthesis of α-Hydroxy Ketones.

α-Hydroxy ketones are a class of vital organic skeletons that generally exist in a variety of natural products and high-value chemicals. However, the traditional synthetic route for their production involves toxic Hg salts and corrosive HSO as catalysts, resulting in harsh conditions and the undesired side reaction of Meyer-Schuster rearrangement. In this study, CO-promoted hydration of propargylic alcohols was achieved for the synthesis of various α-hydroxy ketones.

The Gene Expression Landscape of Prostate Cancer BM Reveals Close Interaction with the Bone Microenvironment.

Bone metastatic (BM) prostate cancer (PCa) belongs to the most lethal form of PCa, and therapeutic options are limited. Molecular profiling of metastases contributes to the understanding of mechanisms defining the bone metastatic niche. Our aim was to explore the transcriptional profile of PCa BM and to identify genes that drive progression.

Targeting cyclin-dependent kinase 7-association between CDK7 and pMED1 expression in prostate cancer tissue.

Cyclin-dependent kinase (CDK) 7-mediated phosphorylation of Mediator-complex subunit 1 (MED1) enhances androgen receptor (AR) activity in prostate cancer (PCa). Hyperactive AR-signalling plays a key role for the development of castration resistance. Several CDK7 inhibitors are currently under investigation in Phase I/II trials addressing solid tumours, including PCa.

Inhibition of Cyclin-Dependent Kinase 8/Cyclin-Dependent Kinase 19 Suppresses Its Pro-Oncogenic Effects in Prostate Cancer.

Progression of prostate cancer (PCa) is characterized by metastasis and castration resistance after response to androgen deprivation. Therapeutic options are limited, causing high morbidity and lethality. Recent work reported pro-oncogenic implications of the Mediator subunits cyclin-dependent kinase (CDK) 8 and 19 for the progression of PCa.

Properties of S-Functionalized Nitrogen-Based MXene (TiNS) as a Hosting Material for Lithium-Sulfur Batteries.

Lithium-sulfur (Li-S) batteries have received extensive attention due to their high theoretical specific capacity and theoretical energy density. However, their commercialization is hindered by the shuttle effect caused by the dissolution of lithium polysulfide. To solve this problem, a method is proposed to improve the performance of Li-S batteries using TiN(TiNS) with S-functional groups as the sulfur cathode host material.

Cracking it - successful mRNA extraction for digital gene expression analysis from decalcified, formalin-fixed and paraffin-embedded bone tissue.

With the advance of precision medicine, the availability of tumor tissue for molecular analysis has become a limiting factor. This is particularly the case for bone metastases which are frequently occurring in cancer types such as prostate cancer. Due to the necessary decalcification process it was long thought that transcriptome analysis will not be feasible from decalcified formalin-fixed, paraffin-embedded (DFFPE) in a large manner.

Analysis of tripartite motif (TRIM) family gene expression in prostate cancer bone metastases.

Tripartite motif (TRIM) family proteins are post-translational protein modifiers with E3-ubiquitin ligase activity, thereby involved in various biological processes. The molecular mechanisms driving prostate cancer (PCa) bone metastasis (BM) are incompletely understood, and targetable genetic alterations are lacking in the majority of cases. Therefore, we aimed to explore the expression and potential functional relevance of 71 TRIM members in bone metastatic PCa.

Pyroptosis: A pro-inflammatory type of cell death in cardiovascular disease.

Pyroptosis is a pro-inflammatory type of regulated cell death (RCD) characterized by gasdermin D (GSDMD)-mediated membrane pore formation, cell swelling and rapid lysis, followed by the massive release of pro-inflammatory mediators such as interleukin-1β and interleukin-18. There are two main pathways of pyroptosis: the caspase-1-mediated canonical pathway and the caspase-4/5/11-mediated noncanonical pathway. However, the caspase-3-gasdermin E (GSDME) pathway and caspase-8-GSDMD pathway also induce pyroptosis.

Hydride Transfer Initiated Redox-Neutral Cascade Cyclizations of Aurones: Facile Access to [6,5] Spirocycles.

Reported herein is the hydride transfer initiated redox-neutral cascade cyclizations of aurones, providing a variety of [6,5] spiro-heterocycles in satisfactory yields and good diastereoselectivities.

Synthesis of Tetrahydro[1,3,4]triazepines via Redox-Neutral α-C(sp)-H Amination of Cyclic Amines.

A Brønsted acid-catalyzed α-C(sp)-H amination of cyclic amines using hydrazines as coupling partners has been reported. This methodology provides a unique protocol to the one-step assembly of tetrahydro[1,3,4]triazepines via [1,5]-hydride transfer-initiated C(sp)-H amination. This reaction features mild conditions, good yields, and high atom economy.

Cascade [1,5]-Hydride Transfer/Cyclization for Synthesis of [3,4]-Fused Oxindoles.

The scandium-catalyzed redox-neutral cascade [1,5]-hydride transfer/cyclization between C4-amine-substituted isatins and 1,3-dicarbonyl compounds has been developed. This protocol enabled the synthesis of tricyclic [3,4]-fused oxindoles in good to high yields and excellent diastereoselectivities, featuring high atom- and step economy as well as good functional group tolerance.

Hydride Transfer Involved Redox-Neutral Cascade Cyclizations for Construction of Spirocyclic Bisoxindoles Featuring a [3,4]-Fused Oxindole Moiety.

The hydride transfer involved redox-neutral cascade cyclization has been developed to construct the spirocyclic bisoxindoles featuring a [3,4]-fused oxindole moiety from rationally designed C4-amine-substituted isatins, affording the diverse tricyclic [3,4]-fused oxindoles with three consecutive chiral centers in good yields and excellent diastereoselectivities (>20:1).

Aromatization-Driven Cascade [1,5]-Hydride Transfer/Spirocyclization Promoted by Fluorinated Alcohols.

The aromatization-driven redox-neutral cascade [1,5]-hydride transfer/spirocyclization and cascade [1,5]-hydride transfer/hydrolysis from para-quinone methide in HFIP were developed. These protocols enabled the synthesis of azaspirocyclohexadienones and ortho-benzylated anilines in good to high yields under mild conditions, featuring room temperature, additive-free, and good functional group tolerance.

Pressure-induced structural and spin transitions of FeS.

Greigite (FeS), isostructural with FeO has recently attracted great scientific interests from material science to geology due to its complicated structure and electronic and magnetic configurations. Here, an investigation into the structural, magnetic and electronic properties of FeS under high pressure has been conducted by first-principle calculations based on density functional theory. The results show that a first-order phase transition of FeS would occur from the inverse spinel (SP) structure to the CrS-type (CS) structure at 3.

Tetrabromobisphenol A and heavy metal exposure via dust ingestion in an e-waste recycling region in Southeast China.

This study was designed to investigate a prevalent brominated flame retardant tetrabromobisphenol A (TBBPA) and four heavy metals of Pb, Cr, As, Cd in dust samples (52 indoor and 52 outdoor) collected from residential houses in an e-waste recycling area in Southeast China. For TBBPA, the mean concentration in indoor dust (3435 ng/g, dw) was higher than that in outdoor dust (1998 ng/g, dw). For heavy metals, the mean concentrations of Pb, Cr, As, Cd were 399, 151, 48.