Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20.
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http://dx.doi.org/10.1016/j.bmcl.2007.09.047 | DOI Listing |
ACS Infect Dis
January 2025
Pharmaceutical Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science Pilani, Pilani Campus, Pilani, Vidya Vihar 333031, (RJ) India.
Antimicrobial drug resistance is a significant global health challenge, causing hundreds of thousands of deaths annually and severely impacting healthcare systems worldwide. Several reported antimicrobial compounds have a guanidine motif, as the positive charge on guanidine promotes cell lysis. Therefore, pyrrole- and indole-based allylidene hydrazine carboximidamide derivatives with guanidine motifs are proposed as antimicrobial agents that mimic cationic antimicrobial peptides (CAMPs).
View Article and Find Full Text PDFJ Med Chem
January 2025
Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, and Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, Theodor-Stern-Kai 7, Frankfurt am Main 60596, Germany.
The leukotriene B4 receptor 2 (BLT2) is a G-protein coupled receptor, which is endogenously activated by 12()-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT). BLT2 is gaining attention as a potential therapeutic target involved in various pathologies including diabetic wound healing, ophthalmic diseases, and colitis. However, validation of BLT2 as drug target requires chemical probes and pharmacological tools which will allow for application in vivo.
View Article and Find Full Text PDFRegen Biomater
December 2024
Department of Trauma Surgery, Orthopaedic Surgery and Plastic Surgery, University Medical Center Göttingen, University of Göttingen, Göttingen 37075, Germany.
Electrospinning is a remarkably straightforward and adaptable technique that can be employed to process an array of synthetic and natural materials, resulting in the production of nanoscale fibers. It has emerged as a novel technique for biomedical applications and has gained increasing popularity in the research community in recent times. In the context of tissue repair and tissue engineering, there is a growing tendency toward the integration of biomimetic scaffolds and bioactive macromolecules, particularly proteins and growth factors.
View Article and Find Full Text PDFBioeng Transl Med
January 2025
Translational NanoMedicine Laboratory, Department of Medicine, Surgery and Dentistry University of Salerno Baronissi SA Italy.
The advent of bioprinting has enabled the creation of precise three-dimensional (3D) cell cultures suitable for biomimetic in vitro models. In this study, we developed a novel protocol for 3D printing methacrylated collagen (ColMa, or PhotoCol®) combined with tendon stem/progenitor cells (hTSPCs) derived from human tendon explants. Although pure ColMa has not previously been proposed as a printable hydrogel, this paper outlines a robust and highly reproducible pipeline for bioprinting this material.
View Article and Find Full Text PDFLangmuir
January 2025
Department of Chemistry and Applied Chemistry, Saga University, 1 Honjo, Saga City, Saga 840-8502, Japan.
This study introduces a novel method for fabricating multicavity, honeycomb-shaped collagen aerogels characterized by continuous pores. We have taken a unique approach to lyophilizing collagen hydrogels, which are UV-irradiated collagen solutions gelatinized in a carbonate buffer solution. The focus of this study was to investigate the effect of UV irradiation times on collagen solutions on collagen hydrogels and aerogels.
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