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Synthesis and evaluation of KX-01 analogs with an exploration of linker attachment points for antibody-drug conjugates.
Bioorg Med Chem Lett
January 2025
Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon 34114 Republic of Korea; Medicinal Chemistry & Pharmacology, University of Science & Technology, Daejeon 34113 Republic of Korea. Electronic address:
KX-01 (tirbanibulin, Klisyri®) is a recently FDA-approved drug for treating actinic keratosis, with a distinct dual mechanism of action combining microtubule disruption and non-ATP-competitive Src inhibition. This unique mechanism and novel chemotype highlight KX-01's potential as a payload for antibody-drug conjugates. In this study, we synthesized and evaluated KX-01 derivatives to enhance anticancer potency and explore functional groups suitable for antibody conjugation.
View Article and Find Full Text PDFFrom basic to clinical and therapeutic insights: news on actinic keratosis and skin squamous cell carcinoma.
Curr Opin Oncol
December 2024
Dermatology department, Hôpital Erasme-HUB.
Purpose Of Review: Squamous cell carcinoma (SCC) is the second most common skin cancer, with an increasing incidence. This review highlights this past year's advances regarding the understanding of its pathogenesis, newly introduced diagnostic methods and updates in prevention and treatment.
Recent Findings: While the pathogenesis of SCC progression remains unclear, new sequencing techniques are helping to better characterize these tumours at the molecular level.
Computational network analysis of two popular skin cancers provides insights into the molecular mechanisms and reveals common therapeutic targets.
Heliyon
January 2025
Department of Biotechnology and Genetic Engineering, Mawlana Bhashani Science and Technology University, Santosh, Tangail-1902, Bangladesh.
Basal Cell Carcinoma (BCC) and Actinic Keratosis (AK) are prevalent skin conditions with significant health complications. The molecular mechanisms underlying these conditions and their potential shared pathways remain ambiguous despite their prevalence. Therefore, this study aims to elucidate the common molecular pathways and potential therapeutic targets for BCC and AK through comprehensive computational network analysis.
View Article and Find Full Text PDFEpidemiology and Management of Actinic Keratosis in France: A General Population Survey (REAKT).
Acta Derm Venereol
January 2025
Department of Dermatology, Saint-André Hospital, Bordeaux University Hospital, Bordeaux, France.
The objective of this retrospective observational study was to estimate the prevalence of actinic keratosis (AK) in individuals aged ≥ 40 years in France, to describe the characteristics of affected patients, and to describe treatments. A representative panel of 20,000 households with ≥ 1 member aged ≥ 40 years were invited to participate. Participants who reported AK lesions diagnosed by a physician were eligible.
View Article and Find Full Text PDFSelf-Applied Daylight Photodynamic Therapy: A Paradigm Shift?
Int J Mol Sci
January 2025
Dermatology Department, Hospital Universitario Ramon y Cajal, Carretera M-607 km 9.1, 28034 Madrid, Spain.
Photodynamic therapy (PDT) involves the topical application of a photosensitizer and its activation by visible light, leading to the generation of protoporphyrin IX (PpIX) and reactive oxygen species. Daylight photodynamic therapy (dPDT), a variant utilizing natural sunlight as the energy source, enhances procedural flexibility by eliminating the need for specialized equipment. dPDT has been effectively used in dermatology to treat various cutaneous disorders, including neoplastic and infectious diseases.
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