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Pd(II)-catalyzed cyclization of alkyne-tethered malononitriles nitrile insertion.
Chem Commun (Camb)
January 2025
Department of Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology (CSIR-IICT), Hyderabad 500007, India.
Herein, we have developed a Pd(II)-catalyzed cyclization of prochiral alkyne-tethered malononitriles to access five-membered carbocycles having a nitrile-containing all-carbon quaternary center. The reaction pathway involves a -acetoxypalladation, nitrile group insertions into the carbon-palladium bond and sequential deacetylation followed by -acetylation. Initial studies on asymmetric cyclization were also performed with chiral Pyox ligands.
View Article and Find Full Text PDFAdvanced 3D bioprinted liver models with human-induced hepatocytes for personalized toxicity screening.
J Tissue Eng
January 2025
Engineering Research Center of Pulmonary and Critical Care Medicine Technology and Device (Ministry of Education), Tianjin Institutes of Health Science, Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin, China.
The development of advanced models for assessing liver toxicity and drug responses is crucial for personalized medicine and preclinical drug development. 3D bioprinting technology provides opportunities to create human liver models that are suitable for conducting high-throughput screening for liver toxicity. In this study, we fabricated a humanized liver model using human-induced hepatocytes (hiHeps) derived from human fibroblasts via a rapid and efficient reprogramming process.
View Article and Find Full Text PDFProtein N-terminal modifications: molecular machineries and biological implications.
Trends Biochem Sci
January 2025
Department of Biomedicine, University of Bergen, Bergen, Norway; Department of Surgery, Haukeland University Hospital, Bergen, Norway. Electronic address:
The majority of eukaryotic proteins undergo N-terminal (Nt) modifications facilitated by various enzymes. These enzymes, which target the initial amino acid of a polypeptide in a sequence-dependent manner, encompass peptidases, transferases, cysteine oxygenases, and ligases. Nt modifications - such as acetylation, fatty acylations, methylation, arginylation, and oxidation - enhance proteome complexity and regulate protein targeting, stability, and complex formation.
View Article and Find Full Text PDFEfficient and reproducible differentiation protocol for pluripotent stem cells into functional endothelial cells: Unveiling the path to vascular regeneration.
Arch Med Res
January 2025
Department of Stem Cells and Developmental Biology, Cell Science Research Center, Royan Institute for Stem Cell Biology and Technology, Tehran, Iran; Department of Regenerative Medicine, Cell Science Research Center, Royan Institute for Stem Cell Biology and Technology, Tehran, Iran.
Introduction: Endothelial cells (ECs) play a crucial role in many treatments for cardiovascular diseases, such as blood vessel repair, tissue engineering, and drug delivery. The process of differentiating these cells is complex and involves various sources and numerous molecular and cellular events. Differentiating pluripotent stem cells (PSCs) into endothelial cells are one of the most effective sources for creating ECs in the lab and offers great potential for regenerative medicine.
View Article and Find Full Text PDFRepurposing Linezolid in Conjunction with Histone Deacetylase Inhibitor Access in the Realm of Glioblastoma Therapies.
J Med Chem
January 2025
School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan.
Since decades after temozolomide was approved, no effective drugs have been developed. Undoubtedly, blood-brain barrier (BBB) penetration is a severe issue that should be overcome in glioblastoma multiforme (GBM) drug development. In this research, we were inspired by linezolid through structural modification with several bioactive moieties to achieve the desired brain delivery.
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