We describe the in vitro evaluation and crystallographic analysis of a new class of potent and selective, non-amino acid-based, small-molecule thrombin inhibitors, exemplified by 14. This class of achiral inhibitors lacks an amide-based backbone, exhibits nM inhibition of thrombin, and is selective for thrombin. Compound 14 does not interact with the active-site catalytic apparatus and is anchored to the enzyme via a single network of hydrogen bonds to Asp189 of the S1 pocket.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(98)00290-x | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
TRPV4 as a Novel Regulator of Ferroptosis in Colon Adenocarcinoma: Implications for Prognosis and Therapeutic Targeting.
Dig Dis Sci
January 2025
Ningxia Medical University, Xing Qing Block, Shengli Street No.1160, Yin Chuan City, 750004, Ningxia Province, People's Republic of China.
Background: Colon adenocarcinoma (COAD) is a leading cause of cancer-related mortality worldwide. Transient receptor potential vanilloid 4 (TRPV4), a calcium-permeable non-selective cation channel, has been implicated in various cancers, including COAD. This study investigates the role of TRPV4 in colon adenocarcinoma and elucidates its potential mechanism via the ferroptosis pathway.
View Article and Find Full Text PDF∆-Tetrahydrocannabinol Increases Growth Factor Release by Cultured Adipose Stem Cells and Adipose Tissue in vivo.
Tissue Eng Regen Med
January 2025
Department of Plastic Surgery, Hand Surgery-Burn Center, University Hospital RWTH Aachen, Pauwelsstraße 30, 52074, Aachen, Germany.
Background: Because of its biocompatibility and its soft and dynamic nature, the grafting of adipose tissue is regarded an ideal technique for soft-tissue repair. The adipose stem cells (ASCs) contribute significantly to the regenerative potential of adipose tissue, because they can differentiate into adipocytes and release growth factors for tissue repair and neovascularization to facilitate tissue survival. The present study tested the effect of administering a chronic low dose of ∆-tetrahydrocannabinol (THC) on these regenerative properties, in vitro and in vivo.
View Article and Find Full Text PDFDesign, synthesis, and in vitro antitumor evaluation of novel benzimidazole acylhydrazone derivatives.
Mol Divers
January 2025
State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang, Guizhou, 550025, People's Republic of China.
This study focuses on the design, synthesis, and evaluation of benzimidazole derivatives for their anti-tumor activity against A549 and PC-3 cells. Initial screening using the MTT assay identified compound 5m as the most potent inhibitor of A549 cells with an IC of 7.19 μM, which was superior to the positive agents 5-Fluorouracil and Gefitinib.
View Article and Find Full Text PDFBackground: Neuroblastoma is a heterogeneous disease with adrenergic (ADRN)- and therapy resistant mesenchymal (MES)-like cells driven by distinct transcription factor networks. Here, we investigate the expression of immunotherapeutic targets in each neuroblastoma subtype and propose pan-neuroblastoma and cell state specific targetable cell-surface proteins.
Methods: We characterized cell lines, patient-derived xenografts, and patient samples as ADRN-dominant or MES-dominant to define subtype-specific and pan-neuroblastoma gene sets.
The Effect of Polyethylene Fiber and Flowable Resin Composite on Fracture Resistance in the Restoration of Large MOD Cavities.
J Esthet Restor Dent
January 2025
Department of Restorative Dentistry, Faculty of Dentistry, Kırıkkale University, Kırıkkale, Türkiye.
Objective: This in vitro study aims to evaluate the effect of placing polyethylene fibers used in large Class II MOD (mesio-occlusion-distal) cavities into different flowable resin composites and in different positions on the fracture resistance of the restoration.
Materials And Methods: Ninety healthy human molars were used in the study. No treatment was performed on 10 of these teeth and they were used as the control group.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!