Cancer accounts for a number of deaths each year. Consequently, prevention of this deadly disease is more challenging and hence the invention of new anticancer agents is of utmost importance. The current review elaborates the importance of indole designs as patented in the form of anticancer druglike molecules targeting different cites of biological arena. Specific attention was given to kinases such as platelet-derived growth factor receptor, vascular endothelial growth factor receptor and fibroblast growth factor receptor, Bruton's tyrosine kinase, anaplastic lymphoma kinase, Janus kinase, cyclin-dependent kinase aurora kinases A, B and C, checkpoint kinases, protein kinase R, Pim kinases, phosphoinositide 3- kinase, altered proteins kinases, polo-like kinase and many more. Moreover, the article summarizes the mode of action through the particular functions of kinases and the inhibitory potential of indole derivatives toward specific kinase. Certain patents gathered in the existing review article suggest that indole core can be a versatile foundation to discover drug-like kinase inhibitor molecules and modification of substituents existing on the indole moiety may have important impact on the pharmacokinetic and pharmacodynamics aspects of the resultant scaffolds. The information presented here would gather a great deal of interest to identify the new molecular designs bearing indole nucleus presenting novel anticancer drugs with a wide variety of biological targets involved in cancer pathology focusing on the inhibition of tyrosine kinases, serine/threonine-specific protein kinases, cyclin-dependent kinases, lipid kinases and altered protein kinases.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.2174/1574892811666161003112119 | DOI Listing |
Biomater Adv
December 2024
Departamento de Química en Ciencias Farmacéuticas, Facultad de Farmacia, Universidad Complutense de Madrid, Instituto de Investigación Sanitaria Hospital 12 de Octubre i+12, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain; CIBER de Bioingeniería, Biomateriales y Nanomedicina, Instituto de Salud Carlos III, 28040 Madrid, Spain. Electronic address:
Local delivery of therapeutic ions from bioactive mesoporous glasses (MBGs) is postulated as one of the most promising strategies for regenerative therapy of critical bone defects. Among these ions, Sr cation has been widely considered for this purpose as part of the composition of MBGs. MBGs of chemical composition 75SiO-25-x CaO-5PO-xSrO with x = 0, 2.
View Article and Find Full Text PDFJ Drug Target
January 2025
Department of Pharmacology, Orotta College of Medicine and Health Sciences, Asmara University, Asmara, P.O. Box: 10549, Eritrea; (I.P).
Mutations that overexpress the epidermal growth factor receptor (EGFR) are linked to cancers like breast (15-20%), head and neck (10-15%), colorectal (5-8%), and non-small cell lung cancer (10-50%), especially in East Asian populations. EGFR activation stimulates "RAS/RAF/MEK/ERK, PI3K/Akt, and MAPK" pathways, which enhance cell division, survival, angiogenesis, and tumor growth while inhibiting apoptosis and metastasis. Secondary mutations (e.
View Article and Find Full Text PDFAngiogenesis
January 2025
Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, USA.
Reduction-oxidation factor-1 or apurinic/apyrimidinic endonuclease 1 (Ref-1/APE1) is a crucial redox-sensitive activator of transcription factors such as NF-κB, HIF-1α, STAT-3 and others. It could contribute to key features of ocular neovascularization including inflammation and angiogenesis; these underlie diseases like neovascular age-related macular degeneration (nAMD). We previously revealed a role for Ref-1 in the growth of ocular endothelial cells and in choroidal neovascularization (CNV).
View Article and Find Full Text PDFCurr Microbiol
January 2025
Engineering Technological Center of Fungus Active Substances of Fujian Province, College of Biological Sciences and Technology, Minnan Normal University, Zhangzhou, 363000, China.
Translation initiation, which involves numerous protein factors and coordinated control steps, represents the most complicated process during eukaryotic translation. However, the roles of eukaryotic translation initiation factor (eIF) in filamentous fungi are not well clarified. In this study, we investigated the function of eIF2Bα in Aspergillus oryzae, an industrially important filamentous fungus.
View Article and Find Full Text PDFArch Dermatol Res
January 2025
Department of Dermatology, Zhejiang Provincial Hospital of Dermatology, Huzhou, 313200, China.
Psoriasis is a long-lasting inflammatory skin condition characterized by excessive keratinocyte growth. Recent studies have confirmed abnormal regulation of microRNAs (miRNAs/miRs) in individuals with psoriasis. This study aimed to investigate the function and specific mechanism of action of miR-128a-3p in interleukin-22 (IL-22)-stimulated HaCaT cells.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!