CAS: 2222-07-3; Cucurbitacin I

上下游产品

cucurbitacin I 2-O-β-D-glucopyranoside cucurbitacin E cucurbitacin D

葫芦素 D置于溴苯,N,N-二甲基乙酰胺,Sodium Acetate,Palladium Diacetate体系中,化学反应 24.0H,以38%的收率获得葫芦素
参考文献:Cucurbitacin D Is A Disruptor Of The Hsp90 Chaperone Machinery
标题:Cucurbitacin D Is A Disruptor Of The Hsp90 Chaperone Machinery
摘要:Heat Shock Protein 90 (Hsp90) Facilitates The Maturation Of Many Newly Synthesized And Unfolded Proteins (Clients) Via The Hsp90 Chaperone Cycle,In Which Hsp90 Forms A Heteroprotein Complex And Relies Upon Cochaperones,Immunophilins,Etc.,For Assistance In Client Folding. Hsp90 Inhibition Has Emerged As A Strategy For Anticancer Therapies Due To The Involvement Of Clients In Many Oncogenic Pathways. Inhibition Of Chaperone Function Results In Client Ubiquitinylation And Degradation Via The Proteasome,Ultimately Leading To Tumor Digression. Small Molecule Inhibitors Perturb Atpase Activity At The N-Terminus And Include Derivatives Of The Natural Product Geldanamycin. However,N-Terminal Inhibition Also Leads To Induction Of The Pro-Survival Heat Shock Response (Hsr),In Which Displacement Of The Hsp90-Bound Transcription Factor,Heat Shock Factor-1,Translocates To The Nucleus And Induces Transcription Of Heat Shock Proteins,Including Hsp90. An Alternative Strategy For Hsp90 Inhibition Is Disruption Of The Hsp90 Heteroprotein Complex. Disruption Of The Hsp90 Heteroprotein Complex Is An Effective Strategy To Prevent Client Maturation Without Induction Of The Hsr. Cucurbitacin D,Isolated From Cucurbita Texana,And 3-Epi-Isocucurbitacin D Prevented Client Maturation Without Induction Of The Hsr. Cucurbitacin D Also Disrupted Interactions Between Hsp90 And Two Cochaperones,Cdc37 And P23.
Doi:10.1021/acs.Jnatprod.5B00054

专利信息

专利号:US-2024336679-A1
优先权日:2021-08-06
标题 :Methods for the treatment of cancer
发明人：LINARES LÆTITIA; FIRMIN NELLY; MANTEAUX GABRIELLE
权利人:INST REGIONAL CANCER MONTPELLIER; INST NAT SANTE RECH MED; UNIV MONTPELLIER
摘要:The present disclosure relates to an Interleukin-6 (IL-6) signaling inhibitor selected from an IL-6 inhibitor, an IL-6 receptor inhibitor, an IL-6/IL-6 receptor complex inhibitor, a gp130 inhibitor and a STAT3 inhibitor or a pharmaceutical composition comprising such an IL-6 signaling inhibitor. for use in a method for treating and/or preventing cancer in a subject in need thereof. wherein the subject has been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin. The inventors have observed that cancers exhibiting recruitment of MDM2 to chromatin have been shown to secrete IL-6 that in turn acts on myoblast cells to activate serine synthesis. Following these surprising and unexpected observations. the inventors set up methods of treatment that are able to induce cancer cells death in subjects that have been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin.