CAS: 1252003-15-8; N-Hydroxy-4-((2-Methyl-1,2,3,4-Tetrahydro-5H-Pyrido[4,3-B]Indol-5-yl)Methyl)Benzamide

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CAS号1239262-52-2 N-羟基-4-[(1,2,3,...

📜Tubastatina三氟乙酸盐置于羟胺体系中,化学反应生成化合物tubastatina
参考文献:Hdac6 Inhibitor Accelerates Wound Healing By Inhibiting Tubulin Mediated Il-1β Secretion In Diabetic Mice
标题:Hdac6 Inhibitor Accelerates Wound Healing By Inhibiting Tubulin Mediated Il-1β Secretion In Diabetic Mice
摘要:Delayed Wound Healing In Diabetes Is Characterized By Sustained Activation Of Inflammasome And Increased Expression Of Il-1 Beta In Macrophages. Identification And Validation Of Novel Pathways To Regulate Il-1 Beta Expression Will Provide Therapeutic Targets For Diabetic Wounds. Here We Report Sustained Over-Expression Of Histone Deacetylase 6 (Hdac6) In Wounds Of Diabetic Mice And Its Role In Delayed Wound Healing. Topical Application Of Hdac6 Inhibitor; Tubastatin A (Tsa) Gel Promoted The Wound Healing In Diabetic Mice. Tsa Hydrogel Reduced The Infiltration Of Neutrophils,T-Cells And Macrophages In The Early Phase Of Wound Healing. Tsa Treatment Promoted The Wound Healing By Inducing Collagen Deposition,Angiogenesis (Cd31) And Fibrotic Factors (Tgf-Beta 1) In The Late Phase Of Healing. Protein Analysis Of The Diabetic Wounds Treated With Tsa Showed Increased Acetylated Alpha-Tubulin And Decreased Levels Of Mature Il-1 Beta With No Significant Effect On The Expression Of Pro-Il-1 Beta,Pro-Caspase-1 And Active Caspase-1. In In Vitro Assays,Macrophages Exhibited Upregulation Of Hdac6,Il-1 Beta And Downregulation Of Il-10 Upon Stimulation With High Glucose And Lps. Tsa Inhibited The Il-1 Beta Secretion And Promoted Il-10 In Stimulated Macrophages With High Glucose And Lps. Further Investigations Showed That Tsa Inhibits Il-1 Beta Release By Inhibiting Tubulin Dependent Lysosomal Exocytosis Without Affecting Its Transcription And Maturation. Nocodazole (Known Acetylation Inhibitor) Pre-Treatment Inhibited Tsa Effect On Il-1 Beta Secretion In High Glucose Stimulated Macrophages. Overall,Our Findings Indicate That Sustained Hdac6 Expression In Diabetic Wounds Contributes To Impaired Healing Responses And Hdac6 May Represent A New Therapeutic Target For Diabetic Wounds.
Doi:10.1016/j.Bbadis.2020.165903

专利信息

专利号:US-11666569-B2
优先权日:2013-10-24
标题 :Treatment of polycystic diseases with an HDAC6 inhibitor
发明人：GRADILONE SERGIO A; LARUSSO NICHOLAS F
权利人:MAYO FOUND MEDICAL EDUCATION & RES; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT
摘要:An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and β-catenin phosphorylation and/or acetylation while reducing bile duct β-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.

专利号:US-2025064840-A1
优先权日:2021-12-16
标 题 :Drug delivery systems based on endoperoxides useful in diagnosis and therapy, and methods thereof
发明人：SILVA MAGALHAES DIOGO; MOREIRA RUI; LOPES FRANCISCA; RODRIGUES CECILIA; MARQUES VANDA
权利人:FACULDADE DE FARMACIA DA UNIV DE LISBOA
摘要:The present invention relates to novel drug delivery systems based on endoperoxide moieties such as 1,2,4,5-tetraoxanes, namely compounds of formula I, appropriately modified to release active pharmaceutical ingredients (API) in the presence of higher levels of Fe (II), in a subject, whereinIron metabolism dysregulation occurs in diseases such as malaria and cancer. Therefore, the present invention also relates to biomarkers comprising said compounds of formula I.Another aspect, the present invention relates to a process of synthesis of compounds of formula I and respective intermediaries.Further, the present invention also relates to a process for labelling, detection, and identification of tumours in a tissue sample.The present invention is thus applicable to the medical and pharmacological areas, in related to particular the ones cancer detection and treatment, and malaria treatment.

专利号:US-9108943-B2
优先权日:2013-06-18
标题:Photoreactive benzamide probes for histone deacetylase 2
发明人：PETUKHOV PAVEL
权利人:UNIV ILLINOIS
摘要:The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein.

专利号:CN-114685496-A
优先权日:2022-04-08
标 题:Synthesis and Application of HDAC6 Inhibitors Based on Hydroxamic Acids

专利号:CN-114685496-B
优先权日:2022-04-08
标 题 :Synthesis and use of HDAC6 inhibitors based on hydroxamic acid