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12-Hydroxy-Lauric Acid Tethered Self-Assembled Heterochiral Diphenylalanine-Based Mechanoresponsive and Proteolytically Stable Hydrogel: A Dual Player for Handling Cancer and Bacterial Challenges.
ACS Appl Bio Mater
January 2025
Department of Applied Chemistry, Rajiv Gandhi Technological University, Bhopal 462033, Madhya Pradesh, India.
Deciphering the most promising strategy for the evolution of cancer patient management remains a multifaceted, challenging affair to date. Additionally, such approaches often lead to microbial infections as side effects, probably due to the compromised immunity of the patients undergoing such treatment. Distinctly, this work delineates a rational combinatorial strategy harnessing stereogenic harmony in the diphenylalanine fragment, tethering it to an amphiphile 12-hydroxy-lauric acid at the N-terminus (compounds -) such that a potential therapeutic could be extracted out from the series.
View Article and Find Full Text PDFUnleashing the Power of Covalent Drugs for Protein Degradation.
Med Res Rev
January 2025
Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, China.
Targeted protein degradation (TPD) has emerged as a significant therapeutic approach for a variety of diseases, including cancer. Advances in TPD techniques, such as molecular glue (MG) and lysosome-dependent strategies, have shown substantial progress since the inception of the first PROTAC in 2001. The PROTAC methodology represents the forefront of TPD technology, with ongoing evaluation in more than 20 clinical trials for the treatment of diverse medical conditions.
View Article and Find Full Text PDFA patent review of von Hippel-Lindau (vhl)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019-present).
Expert Opin Ther Pat
January 2025
Centre for Targeted Protein Degradation, School of Life Sciences, University of Dundee, Dundee, UK.
Introduction: The von Hippel-Lindau (VHL) E3 ubiquitin ligase has seen extensive research due to its involvement in the ubiquitin proteasome system and role as a tumor suppressor within the hypoxia signaling pathway. VHL has become an attractive target for proteolysis targeting chimeras (PROTACs), bifunctional molecules that can induce degradation of neo-substrate proteins. The development of VHL inhibitors and PROTACs has seen rapid development since disclosure of the first non-peptidic VHL ligand (2012).
View Article and Find Full Text PDFCathepsins: Novel opportunities for antibody therapeutics in cancer.
Br J Pharmacol
January 2025
IRCM, INSERM U1194, University of Montpellier, ICM, Montpellier, France.
Cathepsins, the most abundant lysosomal proteases, have key functions in cell maintenance and homeostasis. They are overexpressed and hypersecreted in cancer and associated with poor prognosis. Secreted cathepsins display pro-tumour activities in the tumour microenvironment and thus represent interesting molecular targets in oncology.
View Article and Find Full Text PDFThe interplay of senescence and MMPs in myocardial infarction: implications for cardiac aging and therapeutics.
Biogerontology
January 2025
Centre for Global Health Research, Saveetha Medical College, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, India.
Aging is associated with a marked increase in cardiovascular diseases, such as myocardial infarction (MI). Cellular senescence is also a crucial factor in the development of age-related MI. Matrix metalloproteinases (MMPs) interaction with cellular senescence is a critical determinant of MI development and outcomes, most notably in the aged heart.
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