(2S,3R)-1,2-Epoxy-4-Penten-3-Ol置于吡啶,咪唑,盐酸,4-二甲氨基吡啶,Copper(L) Iodide,四氧化锇,Sodium Azide,四丁基氟化铵,水,Sodium Acetate,Potassium Carbonate,O-(4-氯苯甲酰)氢奎宁,三乙胺,Lithium Bromide,Potassium Hexacyanoferrate(III)体系中,用 四氢呋喃,甲醇,二氯甲烷,溶剂黄146,N,N-二甲基甲酰胺,叔丁醇 用作溶剂,化学反应 48.5H,反应生成茴香霉素 参考文献:Enantioselective Syntheses Of (−)-Anisomycin And Its Propionate Derivative (3097-B1) 标题:Enantioselective Syntheses Of (−)-Anisomycin And Its Propionate Derivative (3097-B1) 摘要:Facile Syntheses Of(-)-Anisomycin And 3097-B1 From Divinylcarbinol 3 In An Overall Yield Of 12.2% And 13.2%,Respectively Are Described. Doi:10.1016/0957-4166(95)00383-5
专利号:US-8703812-B2 优先权日:2005-07-29 标 题 :Protein synthesis required for long-term memory is induced by PKC activation on days preceding associative learning 发明人:ALKON DANIEL L 权利人:ALKON DANIEL L; BRNI NEUROSCIENCES INST 摘要:The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.
专利号:US-2013331427-A1 优先权日:2006-07-28 标题:Methods of stimulating cellular growth, synaptic, remodeling and consolidation of long-term memory 发明人:ALKON DANIEL L 权利人:BRNI NEUROSCIENCES INST; BRNI NEUROSCIENCES INST 摘要:The present invention provides methods of slowing or reversing the loss of memory and learning comprising the steps of contacting an effective amount of a PKC activator with a protein kinase C (PKC) in a subject identified with memory loss slowing or reversing memory loss. The present invention provides methods of stimulating cellular growth, neuronal growth, dendritic growth, dendritic spine formation, dendritic spine density, and the translocation of ELAV to proximal dendrites, and synaptic remodeling. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.
专利号:US-2006057069-A1 优先权日:2004-06-07 标 题 :Detection of protein expression in vivo using fluorescent puromycin conjugates 发明人:STARCK-GREEN SHELLEY R; GREEN HARRY M; ALBEROLA-ILA JOSE; ROBERTS RICHARD W; SCHUMAN ERIN; SMITH WILLIAM B; HAY BRUCE A 权利人:CALIFORNIA INST OF TECHN 摘要:Disclosed is a class of reagents for examining protein expression in vivo that does not require transfection, radiolabeling, or the prior choice of a candidate gene. Further, a series of puromycin conjugates was constructed bearing various labeling moieties. These conjugates were readily incorporated into expressed protein products in cell lysates in vitro and efficiently cross cell membranes to function in protein synthesis in vivo as indicated by flow cytometry, selective enrichment studies, and western analysis. The present invention demonstrates that labeled-puromycin conjugates offer a general means to examine protein expression in vivo.
专利号:US-2010247433-A1 优先权日:2005-10-14 标题:Use of non-canonical amino acids as metabolic markers for rapidly-dividing cells 发明人:TIRRELL DAVID; DIETERICH DANIELA C; LINK AARON J; SCHUMAN ERIN 权利人:CALIFORNIA INST OF TECHN 摘要:The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handleâ€? to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.
专利号:US-8912150-B2 优先权日:2001-08-03 标题:Ribosome structure and protein synthesis inhibitors 发明人:STEITZ THOMAS A; MOORE PETER B; SUTCLIFFE JOYCE A; OYELERE ADEGBOYEGA K; IPPOLITO JOSEPH A 权利人:RIB X PHARMACEUTICALS INC; UNIV YALE; MELINTA THERAPEUTICS INC 摘要:The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.
专利号:US-2007299102-A1 优先权日:2004-04-08 标题:Diphenyl Ox-Indol-2-One Compounds and Their Use in the Treatment of Cancer 发明人:FELDING JAKOB; PEDERSEN HANS C; KROG-JENSEN CHRISTIAN; PRAESTEGAARD MORTEN; BUTCHER STEVEN P; LINDE VIGGO; COULTER THOMAS S; MONTALBETTI CHRISTIAN; UDDIN MOHAMMED; REIGNIER SERGE 权利人:TOPOTARGET AS 摘要:The present invention relates to substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds, and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal. It is postulated that treatment of cancers is achieved in which inhibition of protein synthesis and/or inhibition of activation of the mTOR pathway is an effective method for reducing cell growth. Examples of such cancers are breast cancer, renal cancer, multiple myeloma, leukemia, glia blastoma, rhabdomyosarcoma, prostate, soft tissue sarcoma, colorectal sarcoma, gastric carcinoma, head and neck squamous cell carcinoma, uterine, cervical, melanoma, lymphoma, and pancreatic cancer. A particular subclass of compounds are represented by the formula (II) n n nwherein at least one of X 1 and X 2 is a heteroatom substituent, e.g. 6-chloro-3,3-bis-(4-hydroxy-phenyl)-7-methyl-1,3-dihydro-indol-2-one.
1: Hu R, Ma Q, Kong Y, Wang Z, Xu M, Chen X, Su Y, Xiao T, He Q, Wang X, Xu W, Yang Y, Wang X, Li X, Liu Y, Chen S, Zhao R, Guo M, Wang G, Li W. A Compound Screen Based on Isogenic hESC-Derived β Cell Reveals an Inhibitor Targeting ZnT8-Mediated Zinc Transportation to Protect Pancreatic β Cell from Stress- Induced Cell Death. Adv Sci (Weinh). 2025 Apr 7:e2413161. doi: 10.1002/advs.202413161. Epub ahead of print. 44(4):174-185. doi: 10.1089/dna.2024.0247. Epub 2025 Feb 26. 209:106329. doi: 10.1016/j.pestbp.2025.106329. Epub 2025 Feb 13. 25(1):58. doi: 10.1007/s10142-025-01572-7. 44(3):115391. doi: 10.1016/j.celrep.2025.115391. Epub 2025 Mar 8.
合成参考文献
参考文献:10.1101/lm.1633710 摘要:Markham CM, Taylor SL, Huhman KL. Role of amygdala and hippocampus in the neural circuit subserving conditioned defeat in Syrian hamsters. Learn Mem. 2010 Feb;17(2):109–16. 参考文献:10.1074/jbc.m111.233122 摘要:Wu X, Wang X, Wu S, Lu J, Zheng M, Wang Y, Zhou H, Zhang H, Han J. Phosphorylation of Raptor by p38β Participates in Arsenite-induced Mammalian Target of Rapamycin Complex 1 (mTORC1) Activation. Journal of Biological Chemistry. 2011 Sep;286(36):31501–11. doi: 10.1074/jbc.m111.233122. 参考文献:10.1101/lm.25705 摘要:Gainutdinova TH, Tagirova RR, Ismailova AI, Muranova LN, Samarova EI, Gainutdinov KL, Balaban PM. Reconsolidation of a context long-term memory in the terrestrial snail requires protein synthesis. Learn Mem. 2005 Nov;12(6):620–5. 参考文献:10.1124/jpet.111.183640 摘要:Needham LA, Davidson AH, Bawden LJ, Belfield A, Bone EA, Brotherton DH, Bryant S, Charlton MH, Clark VL, Davies SJ, Donald A, Day FA, Krige D, Legris V, McDermott J, McGovern Y, Owen J, Patel SR, Pintat S, Testar RJ, Wells GMA, Moffat D, Drummond AH. Drug Targeting to Monocytes and Macrophages Using Esterase-Sensitive Chemical Motifs. The Journal of Pharmacology and Experimental Therapeutics. 2011 Oct;339(1):132–42. doi: 10.1124/jpet.111.183640.