Combination therapy of Lapatinib/Letrozole-based protein-vitamin nanoparticles to enhance the therapeutic effectiveness in drug-resistant breast cancer.

HER2-positive breast cancer constitutes 20 % of reported cases, characterized by excessive expression of HER2 receptors, pivotal in cell signaling and growth. Immunotherapy, the established treatment, often leads to multidrug resistance and tumor recurrence. There's a critical need for an effective strategy delaying drug resistance onset and ensuring cancer cell eradication.

Pharmacoinformatics-based prediction of Checkpoint kinase-1 inhibitors from Momordica charantia Linn. for cancer.

Checkpoint kinase 1 (Chk-1), a serine/threonine kinase family protein, is an emerging target in cancer research owing to its crucial role in cell cycle arrest. Therefore, we aimed to predict potential Chk-1 inhibitors from Momordica charantia Linn., using high-throughput molecular docking.

A Facile and Efficient Synthesis of BODIPY-Based Fluorescent Probes for Selective Detection of Hydrazine.

A facile and ratiometric BODIPY-based fluorescent probe 4 was developed for the selective detection of hydrazine in solution phase. The BODIPY-based fluorophores 3 and 4 were easily prepared in high yields from the L-proline catalyzed reaction between α/β-formyl BODIPY 1 a/1 b and 3-cyanoacetylindole 2. Use of easily accessible substrates, benign solvent, catalytic amount of L-proline and high product yields are the advantageous features of the developed protocol.

The TGF-β mimic TGM4 achieves cell specificity through combinatorial surface co-receptor binding.

The immunoregulatory cytokine TGF-β is pleiotropic due to the near-ubiquitous expression of the TGF-β receptors TβRI and TβRII on diverse cell types. The helminth parasite Heligmosomoides polygyrus has convergently evolved a family of TGF-β mimics (TGMs) that bind both these receptors through domains 1-3 of a 5-domain protein. One member of this family, TGM4, differs from TGF-β in acting in a cell-specific manner, failing to stimulate fibroblasts, but activating SMAD phosphorylation in macrophages.

Insights into the Solution Processing of Non-van der Waals Boron Carbide.

Exfoliation of non-layered materials is crucial to unleash their enormous potential in wide range of applications. However, the presence of strong non-van der Waals interactions in all three dimensions makes exfoliation challenging. Boron carbide (BC), known for its high hardness, holds great potential for diverse applications.

One-Step Nanoimprinting of FeO/AgBr Thin Films for Dark-Light Active Antibiofilm and Bacterial-Free Cell Culture Surfaces.

The resuscitation of bacteria through biofilms presents a critical challenge in controlling microbial pathogenesis and addressing antimicrobial resistance. Continuous antibiofilm activity, particularly on frequently contacted surfaces, is therefore critical. In this study, a scalable is introduced, one-step fabrication of FeO/AgBr nanoimprints using a polymerizable sol-gel (PSG) approach to create functional nanostructured thin films with strong antimicrobial properties.

Neurotensin Conjugated Polymeric Porous Microparticles Suppress Inflammation and Improve Angiogenesis Aiding in Diabetic Wound Healing.

Neurotensin (NT), a bioactive tridecapeptide aids in diabetic wound healing by modulating inflammation and angiogenesis. However, its rapid degradation in peptidase-rich wound environment (plasma half-life <2 min) limits its efficacy. To address this, neurotensin-conjugated polymeric porous microparticles (NT-PMP) were developed and loaded in gelatin (hydrogel 15% w/v) for topical application, enabling sustained NT release to enhance therapeutic outcomes.

Medicinal chemistry-based perspectives on thiophene and its derivatives: exploring structural insights to discover plausible druggable leads.

Thiophene is a privileged pharmacophore in medicinal chemistry owing to its diversified biological attributes. The thiophene moiety has been ranked 4th in the US FDA drug approval of small drug molecules, with around 7 drug approvals over the last decade. The present review covers USFDA-approved drugs possessing a thiophene ring system.

Can selenenyl sulfides be a substrate of glutathione reductase enzyme? A theoretical insight.

Glutathione reductase (GR) catalyzes the reduction of glutathione disulfide (GSSG) to glutathione. As selenium is a congener of sulfur, the possibility of reducing selenenyl sulfide (RSeSG) at the catalytic site of GR has been investigated using density functional theory. Calculations on the redox potential and the Se-S bond strength of some studied RSeSG compounds with a phenyl selenide backbone suggested that the unsubstituted and amine-based selenenyl sulfide intermediates could have a promising tendency to be reduced at the catalytic site of GR.

Fluorescent TICT Probe for Precise Monitoring of Cellular Lipid Droplets.

Lipid droplets (LD) are crucial in pathological processes or conditions associated with abnormal lipid metabolism, such as obesity, diabetes, atherosclerosis, fatty liver diseases, and cancers. Cancer cells frequently contain elevated levels of nonpolar lipid droplets (LDs), serving as energy reserves. The proliferation of LDs, accompanied by an increase in viscosity, is a characteristic feature of cancer cells that prompted us to devise a fluorescent sensor for LD detection at physiological pH.

Triphenylamine-Based Push-Pull Dyes for Chromogenic Detection of HSO Ion in Water: The Role of Anion in the Formation of Fluorescent Organic Nanoparticles.

Optical detection of the HSO ion in pure aqueous medium is rare, owing to the very high Gibbs free energy of hydration and ambiguity to distinguish with the isostructural HPO ion. Herein, a pair of triphenylamine-based push-pull dyes with different numbers of terminal pyridine fragments, connected via an acetylenic linker, were synthesized by Sonogashira cross-coupling reaction. These two dyes displayed highly selective (LOD = 15.

Pharmacophore modeling, 3D-QSAR, and MD simulation-based overture for the discovery of new potential HDAC1 inhibitors.

Histone deacetylases (HDACs) are important epigenetic regulators that modulate the activity of histone and non-histone proteins leading to various cancers. Histone deacetylase 1 (HDAC1) is a member of class 1 HDAC family related to different cancers. However, the nonselective profile of existing HDAC1 inhibitors restricted their clinical utility.

Optimization of sandstone processing waste, electric arc furnace slag, and fly ash-based ternary blended eco-friendly geopolymers.

Over the years, ordinary Portland cement (OPC) has been used to meet growing demands of land and housing facilities arising out of population overburdens. It is well documented that OPCs, besides their outstanding qualities as building materials, are also significant contributors to global greenhouse gases (GHG). Consequently, recent years have noticed an emerging interest in the search for alternatives to Portland cement-based binders.

Correction: Understanding selective sensing of human serum albumin using a D-π-A probe: a photophysical and computational approach.

Correction for 'Understanding selective sensing of human serum albumin using a D-π-A probe: a photophysical and computational approach' by Anamika Bandyopadhyay , , 2024, , 10719-10735, https://doi.org/10.1039/D4TB01229A.

Energetics of Oligosaccharide Adsorption on Ionic Liquid-Clay Composites.

Well-Tempered Metadynamics (WT-MetaD) simulations indicate that composite materials made up of Na-Montmorillonite (Na-MMT) coated with ionic liquids (ILs) having hydrophilic cations serve as good adsorbents for a hexameric (1,4) linked β-D-glucopyranoside (BGLC). Hydrophilic IL cations are effectively coated on the negative charges lining the Na-MMT surface while attracting simultaneously the polar oligosaccharides. In this work we have used two less conventional polyethylene glycol (PEG) based IL cations, [mim peg] and [mim peg], paired with [tfN] and Cl anions.

Ruthenium(II)-Catalyzed C-H/C-H (4+2) Annulation of 2-Aryl-N-heterocycles with Vinylene Carbonate.

A ruthenium(II)-catalyzed direct C-H/C-H (4+2) annulation of 2-aryl-N-heterocycles such as 2-aryl-4H-pyrido[1,2-a]pyrimidin-4-ones, 2-arylimidazo[1,2-a]pyridines, 2-aryl-2H-indazoles and 2-arylquinolin-4(1H)-ones with vinylene carbonate has been described. This one-pot cascade strategy provided the diversely substituted fused-polyheterocycles such as 7H-benzo[h]pyrido[2,1-b]quinazolin-7-ones, naphtho[1',2':4,5]imidazo[1,2-a]pyridines, indazolo[2,3-a]quinolines and benzo[c]acridin-7(12H)-ones in moderate to excellent yields. The developed protocol exhibited a broad substrate scope with good functional group tolerance and acid/base-free conditions.

siRNA-based nanotherapeutic approaches for targeted delivery in rheumatoid arthritis.

Rheumatoid arthritis (RA), characterized as a systemic autoimmune ailment, predominantly results in substantial joint and tissue damage, affecting millions of individuals globally. Modern treatment modalities are being explored as the traditional RA therapy with non-specific immunosuppressive drugs showcased potential side effects and variable responses. Research potential with small interfering RNA (siRNA) depicted potential in the treatment of RA.

Biotinylated platinum(IV)-conjugated graphene oxide nanoparticles for targeted chemo-photothermal combination therapy in breast cancer.

Graphene oxide (GO) and GO-based nanocomposites are promising in drug delivery and photothermal therapy due to their exceptional near-infrared optical absorption and high specific surface area. In this study, we have effectively conjugated an oxaliplatin (IV) prodrug, PEGylated graphene oxide, and PEGylated biotin (PB) in a single platform for breast cancer treatment. This platform demonstrates promising prospects for targeted drug delivery and the synergistic application of photothermal-chemotherapy when exposed to NIR-laser irradiation.

Biogenic Nanoparticles as Safer Alternatives for Gastric Ulcers: An Update on Green Synthesis Methods, Toxicity, and Their Efficacy in Controlling Inflammation.

Peptic ulcers, affecting approximately 10% of the global population, can result from factors such as stress, alcohol use, smoking, NSAIDs, Helicobacter pylori infection, and genetic predisposition. Plant-based medicines are gaining recognition for their therapeutic potential, including in the treatment of peptic ulcers. Green chemistry methods for the biological synthesis of nanoparticles (NPs) provide a sustainable alternative to traditional chemical techniques.

Phenoxy-1,2-dioxetane-based activatable chemiluminescent probes: tuning of photophysical properties for tracing enzymatic activities in living cells.

The use of chemiluminophores for tracing enzymatic activities in live-cell imaging has gained significant attention, making them valuable tools for diagnostic applications. Among various chemiluminophores, the phenoxy-1,2-dioxetane scaffold exhibits significant structural versatility and its activation is governed by the chemically initiated electron exchange luminescence (CIEEL) mechanism. This mechanism can be initiated by enzymatic activity, changes in pH, or other chemical stimuli.

New epigenome players in the regulation of PCSK9-H3K4me3 and H3K9ac alterations by statin in hypercholesterolemia.

Statins are the most effective drugs used worldwide to lower the serum LDL-C by inhibiting the rate-limiting step, HMG-CoA reductase, in cholesterol biosynthesis. Despite its prevalent use, statins are known to increase proprotein convertase subtilisin/kexin type 9 (PCSK9) expression, hindering its efficiency. However, the underlying mechanisms remain elusive.