Gyaran Peptide
Peptide pegylation
Menene Peptide Pegylation?
Peptide polyethylene glycolization shine tsari na haɗin gwiwa ɗaya ko fiye da polyethylene glycol. (PEG) sarƙoƙi zuwa kwayoyin peptide. Polyethylene glycolization yana ƙara nauyin kwayoyin peptide, yana kare peptide daga hydrolysis ta hanyar gina jiki hydrolases, kuma a ƙarshe yana inganta pharmacokinetics na peptide.
Peptides suna taka muhimmiyar rawa a cikin masana'antar harhada magunguna da haɓakar magungunan ƙwayoyi. Duk da haka, aikace-aikacen in vivo na peptides yana iyakance saboda saurin lalacewa ta hanyar enzymes proteolytic, rashin ƙarfi mai narkewa, halayen antigenic, da glomerular tacewa a cikin koda. Covalent mahada na polyethylene glycol (PEG) yana rage rigakafi, yana inganta narkewa kuma yana rage cirewar koda. Ƙarin sarƙoƙi na monodissperse PEG shine mabuɗin mahimmanci a cikin ci gaban warkewa na peptides PEGylated.. Wadannan peptides masu aminci da inganci na polyethylene glycolated suna da mahimmanci don ingantaccen ingantaccen warkewa..
Peptide Pegylation masana kimiyya
Masu haɗin PEG na gama gari da gajarta
· Danna Chemistry, wanda ke faruwa tsakanin ƙungiyar azide na PEG reagent da ƙungiyar alkyne na peptide, ko akasin haka.
· Suzuki-Miyaura Coupling, wanda ke faruwa tsakanin ƙungiyar iodophenyl na PEG reagent da ƙungiyar aryl boronic acid na peptide., ko akasin haka..
· Sonogashira Coupling, wanda ke faruwa tsakanin ƙungiyar iodophenyl na PEG reagent da ƙungiyar alkyne na peptide., ko akasin haka.
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Abbrev.
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Cikakken Sunan Sarkar PEG
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PEG |
tetraethylene glycol |
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mini-PEG2 |
8-amino-3,6-dioxaoctanoic acid |
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mini-PEG3 |
amino-3,6,9-trioxaundecanoic acid |
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NH2-PEG2-acid |
3-(2-(2-Aminoethoxy)ethoxy)-propanoic acid |
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PEG750 |
Poly(ethylene glycol) methyl ether (matsakaicin Mn 750) |
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PEG1000 |
Poly(ethylene glycol) methyl ether (matsakaicin Mn 1000) |
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PEG2000 |
Poly(ethylene glycol) methyl ether (matsakaicin Mn 2000) |
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PEG5000 |
Poly(ethylene glycol) methyl ether (matsakaicin Mn 5000) |
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Ester (OTBzl) |
p-Nitroanilide |
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KLH (-COOH na tashar C) |
tBu |
Fitattun Bayani
Haɓaka Alamar Radiyo mai suna Peptide Ligand don Hoto na PET na Fahimtar Ci gaban Ƙwararrun Ƙwararru
Ma'aikatan hoto dangane da binciken peptide suna da kyawawan kaddarorin pharmacokinetic idan har suna da alaƙa da maƙasudin su a cikin vivo.. Hanyar inganta alaƙar peptide ligand don manufarta ita ce sanya wannan hulɗar ta kasance mai daidaituwa kuma ba za ta iya jurewa ba.. Don wannan dalili, mun kimanta alamar peptide mai alamar 64Cu, 64Ku-L19K-(5-fluoro-2,4-dinitrobenzene) (64Cu-L19K-FDNB), wanda ke ɗaure covalently da irreversibly zuwa jijiyar endothelial girma factor (VEGF) a matsayin wakilin hoto na PET. Mun kwatanta abubuwan da ke cikin vivo na 64Cu-L19K-FDNB a cikin VEGF-bayyanar da ƙari xenografts tare da analogs ɗin da ba a haɗa su ba., 64Ku-L19K-(2,4-dinitrophenyl) (64Ku-L19K-DNP) da 64Cu-L19K. Hanyoyin: L19K peptide (GGNECDIARMWEWECFERK-CONH2) An gina shi tare da 1,4,7-triazacyclononane-1,4,7-triacetic acid a tashar N don yin lakabin rediyo tare da 64Cu tare da polyethylene glycol spacer tsakanin peptide da chelate.. 1,5-difluoro-2,4-dinitrobenzene an haɗa shi a C-terminal lysine don haɗin kai zuwa VEGF, Saukewa: L19K-FDNB. 64Cu-L19K-FDNB an gwada shi don haɗin haɗin gwiwa zuwa VEGF a cikin vitro. A matsayin sarrafawa, An haɗa L19K zuwa 1-fluoro-2,4-dinitrobenzene, Saukewa: L19K-DNP. PET Hoto da Nazarin Rarraba Halittu na 64Cu-L19K-FDNB, 64Ku-L19K-DNP, kuma an kwatanta 64Cu-L19K na asali a cikin HCT-116 xenografts.. Toshe binciken na 64Cu-L19K-FDNB an yi shi tare da haɓakar wuce haddi na L19K-FDNB mara lakabi.. Sakamako: Nazarin dauri na in vitro sun tabbatar da haɗin kai da rashin jurewa na 64Cu-L19K-FDNB zuwa VEGF, alhali 64Cu-L19K-DNP da 64Cu-L19K ba su ɗaure gaba ɗaya ba.. Hoto na PET ya nuna haɓakar ƙari mai girma tare da 64Cu-L19K-FDNB fiye da 64Cu-L19K-DNP da 64Cu-L19K, tare da daidaitattun ƙimar ɗauka na 0.62 ± 0.05, 0.18 ± 0.06, kuma 0.34 ± 0.14, bi da bi, a 24 h bayan allura (P < 0.05), kuma 0.53 ± 0.05, 0.32 ± 0.14, kuma 0.30 ± 0.09, bi da bi, a 48 h bayan allura (P < 0.05). Toshe binciken tare da 64Cu-L19K-FDNB a gaban wuce haddi na peptide mara alama ya nuna 53% raguwa a cikin ciwon daji a 48 h bayan allura. Kammalawa: A cikin wannan binciken hujja-na-ra'ayi, Yin amfani da covalent peptide ligand da VEGF yana inganta tarawar ganowa a wurin ciwon daji a cikin vivo., idan aka kwatanta da analog ɗin sa na peptide mai ɗaure marasa ƙarfi. Wannan dabarar kayan aiki ce mai ban sha'awa don haɓaka ƙarfin binciken peptide a matsayin wakilai na hoto.
Abubuwan Gyaran Peptide masu alaƙa
peptide glycosylation
peptide glycosylation
Peptide glycosylation shine gyare-gyare na covalent wanda zai iya inganta halayen physicochemical na peptides.
Kara karantawapeptide phosphorylation
peptide phosphorylation
Phosphoralation na iya faruwa akan Serine (S, Don zama), Threonine (T, Thr) da kuma Tyrosine (Y, Tyr) sarƙoƙi na gefe ta hanyar haɗin phosphoester
Kara karantawaPeptides masu tasowa
Peptides masu tasowa
Gabatarwar amino acid guda biyu marasa dabi'a wadanda ke dauke da α-methyl, Ƙungiyoyin α-alkenyl yayin haɓakaccen lokaci mai ƙarfi na sarƙoƙi na peptide.
Kara karantawaCyclic Peptide
Cyclic Peptide
Juyin hawan peptide yana haɓaka kwanciyar hankali na peptides (dangane da analogues na layin su) kuma dabara ce ta gama gari a cikin ci gaban peptide.
Kara karantawapeptide gyara
Ƙwarewa mai zurfi a cikin gyaran peptide, samar da hanyoyi masu dacewa da yawa don binciken peptide.
