Identification of small-molecule ligand-binding sites on and in the ARNT PAS-B domain.

Transcription factors are challenging to target with small-molecule inhibitors due to their structural plasticity and lack of catalytic sites. Notable exceptions include naturally ligand-regulated transcription factors, including our prior work with the hypoxia-inducible factor (HIF)-2 transcription factor, showing that small-molecule binding within an internal pocket of the HIF-2α Per-Aryl hydrocarbon Receptor Nuclear Translocator (ARNT)-Sim (PAS)-B domain can disrupt its interactions with its dimerization partner, ARNT. Here, we explore the feasibility of targeting small molecules to the analogous ARNT PAS-B domain itself, potentially opening a promising route to modulate several ARNT-mediated signaling pathways.

Microcapsules of Poly(butylene adipate--terephthalate) (PBAT) Loaded with Aliphatic Isocyanates for Adhesive Applications.

This work introduces the encapsulation of hexamethylene diisocyanate derivatives (HDI, TriHDI, and PHDI) with the biodegradable polymer poly(butylene adipate--terephthalate) (PBAT) through a solvent evaporation method. These microcapsules (MCs) were then employed in adhesive formulations for footwear. Moreover, MCs containing PHDI were produced in a closed vessel, demonstrating the potential for recovering and reusing organic solvents for the first time.

Computational investigation of turmeric phytochemicals targeting PTR1 enzyme of species.

In this study, we used techniques to identify available parasite treatments, representing a promising therapeutic avenue. Building upon our computational initiatives aimed at discovering natural inhibitors for various target enzymes from parasites causing neglected tropical diseases (NTDs), we present novel findings on three turmeric-derived phytochemicals as inhibitors of pteridine reductase I (PTR1) through methodologies. PTR1, a crucial enzyme in the unique folate metabolism of trypanosomatid parasites, holds established therapeutic significance.

Novel Calcium Phosphate Promotes Interbody Bony Fusion in a Porcine Anterior Cervical Discectomy and Fusion Model.

Study Design: Experimental porcine anterior cervical discectomy and fusion (ACDF) model: a proof-of-concept study.

Objective: The effect of monetite synthetic bone graft (SBG) containing calcium pyrophosphate and β-tricalcium phosphate on cervical spinal fusion in a noninstrumented two-level large animal model.

Summary Of Background Data: ACDF is the gold standard surgical technique for the treatment of degenerative cervical spinal diseases.