Fmoc-赖氨酸,三氟乙酸酐置于n,N-二异丙基乙胺体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.33H,以90%的收率获得产物fmoc-N'-三氟乙酰基-L-赖氨酸 参考文献:Effects Of Lysine Acetylation In A β-Hairpin Peptide: Comparison Of An Amide−π And A Cation−π Interaction 标题:Effects Of Lysine Acetylation In A β-Hairpin Peptide: Comparison Of An Amide−π And A Cation−π Interaction 摘要:The Acetylation Of Lysine Is A Common Posttranslational Modification Of Histone Proteins,And The Interaction Of Acetylated Lysines With Aromatic Rings Is Commonly Observed In Transcriptionally Relevant Protein-Protein Interactions. To Determine The Nature Of This Interaction And Its Potential Role In Protein Structure And Function,The Effect Of Lysine Acetylation On Its Interaction With Tryptophan Has Been Investigated Within The Context Of A Beta-Hairpin Peptide. Acetylation Of Lys Results In The Replacement Of A Cation-Pi Interaction With An Amide-Pi Interaction. Despite The Loss Of Positive Charge,The Interaction Energy Is Not Significantly Perturbed,Although The Geometry Of Interaction Is Influenced Such That The Amide Nh Interacts Directly With The Trp Ring. Thermodynamic Analysis Indicates An Enthalpic Driving Force For The Stabilization,Indicating A Polar-Pi Interaction. Acyl Lysine Analogues Formyl Lysine And Trifluoroacetyl Lysine Were Used To Further Investigate The Sterics And Electronics Of The Interaction. DOI:10.1021/ja0648460
专利号:US-2025090698-A1 优先权日:2018-11-27 标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases 发明人:CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT 权利人:INDIAN INSTITUTE OF TECH INDORE 摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.
专利号:EP-0450715-B1 优先权日:1990-04-02 标题 :Immunogenic compounds, the process for their synthesis and their use in the preparation of antimalaria vaccines 发明人:PESSI ANTONELLO; BIANCHI ELISABETTA; CORRADIN GIAMPIETRO 权利人:ENIRICERCHE SPA 摘要:A class of immunogenic compounds is described, definable by the formula (I): where: D is L-lysine or branched poly(L-lysine) with a number n of L-lysine amino acid residues (Lys) of a and epsilon amide linkage; n is a whole odd number varying from 1 to 15; A and B, which can be the same or different, are a polypeptide consisting of one or more plasmodial B epitopes covalently bound to one or more peptides with an amino acid sequence corresponding to that of a T epitope such as FNNFTVSFWLRVPKVSASHLEA (TT3) and QYIKANSKFIGITE (TT2), a compound of adjuvant activity, or A-CO or B-CO represent a direct bond or R-A-CO or R-B-CO are a protecting group for the alpha or epsilon -amino group of the L-lysine amino acid residue, with the condition that A and B are not both simultaneously an adjuvant or a direct bond or a protecting group; X is an amino acid residue in which R1 is the side chain of a amino acid residue chosen from L-Asp, L-His, L-Cys, L-Gln, L-Thr, L-Ala, L-Leu, L-Met, L-Phe, L-Glu, L-Arg, L-Tyr, L-Asn, L-Ser, L-Gly, L-Val, L-Ileu, L-Pro and L-Trp, and R2 is OH or NH2; R is hydrogen or an acyl radical; and the corresponding pharmaceutically acceptable salts of acid or basic addition. Compounds of formula (I) are particularly suitable as immunogens for preparing genetically non-restricted antimalaria vaccines, and in diagnostics for determining anti-Plasmodium antibodies in blood, serum and blood spot samples.
专利号:IT-9019914-A1 优先权日:1990-04-02 标题:IMMUNOGENIC COMPOUNDS, THE PROCEDURE FOR THEIR SYNTHESIS AND THEIR USE FOR THE PREPARATION OF ANIMALARY VACCINES
专利号:EP-0450715-A1 优先权日:1990-04-02 标 题 :Immunogenic compounds, the process for their synthesis and their use in the preparation of antimalaria vaccines
专利号:CN-101857629-A 优先权日:2009-04-09 标题 :Solid-phase synthesis method of Bremelanotide
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1007/978-1-4939-8588-3_24 摘要:Kistemaker HAV, Voorneveld J, Filippov DV. ADPr-Peptide Synthesis. Methods Mol Biol. 2018;1813():345–69. doi: 10.1007/978-1-4939-8588-3_24. 参考文献:10.1007/0-306-46880-8_50 摘要:Zhang S, Liu G, Xia S, Ding Z. Parallel synthesis of muramyl peptides derivatives. 2002. In: Peptides Biology and Chemistry. : Kluwer Academic Publishers; 2002. 参考文献:10.1007/978-0-387-26575-9_217 摘要:Shan Y, Hu J, Wang L, Li W. Synthesis of Quantum Dot-Signal Peptides Bioconjugates and Targeting in Living Cells. 2006. In: Understanding Biology Using Peptides. : Springer New York; 2006.