Kedu n'ime mmeghachi omume ndị a ka ejiri Mepụta Peptides? Echiche ise na-ezighi ezi na otu ihe atụ

Azịza ngwa ngwa

Echiche ise na-ezighị ezi banyere mmeghachi omume na-emepụta peptides, ejiri usoro dozie ya, mgbagha nchekwa-otu, ihe akaebe agbụrụ, yana otu NRPS na-adịghị arụ ọrụ…

Okwu mmalite

Ndị na-eweta Peptides akpọrọ Foto ndị Peptides Ajụjụ "Kedu mmeghachi omume ndị a na-eji mepụta peptides" na-apụtakarị n'otu n'ime ntọala abụọ: ihe otutu nhọrọ ebe condensation, hydrolysis, nnọchi na esterification na-asọ mpi maka azịza ya, ma ọ bụ nsogbu bench ebe a ga-emekọrịta nha nhata akwụkwọ na usoro njikọ njikọ nke na-aga awa abụọ na DMF. Ntọala abụọ a na-akwụghachi otu ọdịiche ahụ. Mmeghachi omume nke na-emepụta njikọ peptide bụ njikọ amide site na nnọchi nucleophilic acyl na carbon carbon carbon arụ ọrụ.. Ngụkọta condensation ọtụtụ ọmụmụ na-ebipụta - carboxyl plus amine na-enye amide gbakwunyere mmiri - bụ stoichiometry net nke mgbanwe ahụ., ọ bụghị usoro onye ọ bụla na-agba dị ka e dere.

Echiche ise na-ezighị ezi na-esote site na ịdaba na ọdịiche ahụ, na onye ọ bụla na-agbaziri n'okpuru na ya usoro, ihe akaebe na ọnọdụ oke. Akụkụ nke isii na-ewelite ihe nlere anya nke ajụjụ a na-adịghị emetụta ma ọlị: synthetases na-abụghị ribosomal peptide, ebe na-enweghị njikọ njikọ na enweghị nchekwa-otu okirikiri dị. Ọ gwụla ma ekwuru ya ọzọ, Ihe ọ bụla a na-ekwu ebe a na-adabere na kemikal (enweghị ribosomal) njikọ nke peptides, na ihe atụ ọnụọgụgụ ka ewepụtara site na usoro na ọnọdụ akpọrọ aha, ọ bụghị site na peptide njikọ n'ozuzu.

Kedu n'ime mmeghachi omume ndị a ka ejiri Mepụta Peptides? Echiche ise na-ezighi ezi na otu ihe atụ

Echiche na-ezighi ezi 1: "Nha nhata condensation bụ mmeghachi omume ị na-agba"

Njehie a na-agụ nha nha nhata dị ka uzommeputa. Ịgwakọta acid carboxylic efu na amine efu na-enye nnu carboxylate ammonium, na nha nhata maka nhazi amide ozugbo na mmiri dabere na nnu karịa amide. Kpoo oku iji chụpụ mmiri abụghị ihe a na-arụ ọrụ mgbe ndị mmekọ na-ebu agbụ akụkụ na-emeghachi omume, epimerise ma ọ bụ decompose n'okpuru ọnọdụ ndị ahụ.

Ihe na-eme n'ezie na njikọta bụ usoro nke akụkụ abụọ. Nke mbụ, a na-atụgharị akụkụ carboxyl ka ọ bụrụ ụdị electrophilic ọzọ - O-acylisourea sitere na carbodiimide dị ka DCC., DIC ma ọ bụ EDC, ester nọ n'ọrụ sitere na HOBt, HOAt ma ọ bụ Oxyma, ma ọ bụ uronium/phosphonium sitere na ụdị arụ ọrụ. Mgbe ahụ, amine na-awakpo nke mere ka carbonyl rụọ ọrụ, na mgbakwunye ma ọ bụ ịhapụ otu na-apụ. OpenStax Organic Chemistry §26.7, bipụtara September 20, 2023, na-akọwa kpọmkwem nke a: Enwere ike ime amide dị mfe site n'ịgwọ amine na carboxylic acid na carbodiimide, mana njikọ peptide siri ike karị n'ihi na ọtụtụ njikọ amide dị iche iche ga-etolite n'usoro akọwapụtara kama ịbụ na enweghị usoro.. Ntuziaka njikọta-reagent nke Bachem depụtara ebighị ezinụlọ eji - acid halides, azides, symmetrical na agwakọta anhydrides, carbodiimides nwere ma ọ bụ na-enweghị ihe mgbakwunye - nke bụ ihe ncheta bara uru na "mmelite" bụ klas nke arụmọrụ., ọ bụghị otu reagent.

Kedu n'ime mmeghachi omume ndị a ka ejiri Mepụta Peptides? Echiche ise na-ezighi ezi na otu ihe atụ

Oke ihe gbasara azịza ule yana maka nhazi bench. Ọ bụrụ na ajụjụ a jụrụ nke klas mmeghachi omume na-emepụta njikọ peptide, azịza ya bụ amide kpụrụ site nucleophilic acyl nnọchi na carbon carboxyl na-arụ ọrụ; condensation na-akọwa nguzozi atọm n'ozuzu ya. Ọ bụrụ na ajụjụ a jụrụ ihe ị ga-etinye na flask, ọbụghị nha nha ma ọ bụ aha klaasị zuru oke - reagent, mgbakwunye, ihe mgbaze, A ghaghị ịkọwa isi na okpomọkụ niile, na nhọrọ ndị ahụ bụ ihe ngalaba fọdụrụnụ gbasara.

Echiche na-ezighi ezi 2: "Ndị otu nchekwa bụ nhọrọ ma ọ bụrụ na ị kpachapụ anya"

Njehie a na-ewere nchekwa dị ka nkwalite mkpụrụ. Ọ bụ nhọrọ nhọrọ. Amino acid ọ bụla na-enye opekata mpe α-amine na α-carboxyl, na ọtụtụ ugbu a n'akụkụ-yinye nucleophile nakwa - thiol nke cysteine, imidazole nke histidine, ε-amine nke lysine, hydroxyl nke serine, Threonine ma ọ bụ tyrosine. Enweghị nchebe orthogonal, ngwakọta njikọ nwere ọtụtụ nucleophiles reactive na-asọ mpi maka otu carboxyl arụ ọrụ, na nkesa ngwaahịa bụ ọnụ ọgụgụ karịa usoro akọwapụtara.

Kedu n'ime mmeghachi omume ndị a ka ejiri Mepụta Peptides? Echiche ise na-ezighi ezi na otu ihe atụ

Ihe atụ ọrụ OpenStax's Ala-Leu na-eme ka mgbagha ahụ sie ike: ijikọta alanine na leucine, A na-echekwa amine nke alanine na carboxyl nke leucine, A na-emepụta amide chọrọ na EDC ma ọ bụ DCC, na-ewepụkwa otu nchebe - nzọụkwụ ise maka dipeptide. Otu akwụkwọ ahụ kwuru na a na-ebukarị otu amino dị ka Boc (wepụrụ site na obere acid siri ike dị ka TFA) ma ọ bụ, karia, dị ka Fmoc (wepụrụ site 20% piperidine na DMF), ebe a na-ejikarị otu carboxyl dị ka methyl ma ọ bụ benzyl esters. Nke Nchịkọta peptide synthesis Wikipedia okpokolo agba otu ebe n'ogo nke atụmatụ: Atụmatụ nchekwa-otu na-adịkarị mkpa iji gbochie mmeghachi omume n'akụkụ na agbụ akụkụ, na njikọ kemịkalụ na-amalitekarị na C-terminus wee gaa n'ihu N-terminus.

Ọnọdụ oke dị adị ma dị warara. Chemoselective ligation nso na mkpụmkpụ, Iberibe arụrụ arụ pụrụ iche nwere ike ibelata ibu nchebe, n'ihi na a na-ahọrọ ndị mmekọ na-emeghachi omume ka ọ bụrụ naanị otu ụzọ nwere ike jikọta. Ha anaghị ewepụ ya maka mgbakọ yinye nzọụkwụ nzọụkwụ, ebe agbụ na-eto eto na ihe fọdụrụ na-abata ma na-ebu ọtụtụ ebe reactive. Ihe nchọpụta bara uru: Ọ bụrụ na chromatogram crude na-egosi steepụ nke elu ugwu kewapụrụ site na otu ihe fọdụrụ karịa otu ngwaahịa kachasị., nsogbu na-abụkarị selectivity, ezughị ezu reagent.

Echiche na-ezighi ezi 3: "Mmalite na njikọta na-anọpụ iche na stereochemically"

Njehie a na-eche na reagent njikọ na-emetụta naanị ụdị ngwaahịa. Ọ na-emetụtakwa ụdị stereoisomer. Nke Molecules Nyochaa Duengo et al. (2023; 28:8017) na-akọwa ụzọ abụọ ntọala-catalysed maka nkwụsị nke nhazi: abstraction kpọmkwem nke α-proton iji nye enolate nke na-emegharị site na ihu ọ bụla, na nhazi nke oxazol-5(4H)-otu sitere na ihe fọdụrụ n'ọrụ, nke bụ ụzọ a na-ahụkarị mgbe ejiri carboxyl rụọ ọrụ. Ụzọ abụọ a na-agbakọta na otu ịdọ aka ná ntị - ihe fọdụrụ nke carboxyl na-arụ ọrụ bụ ebe kachasị ize ndụ na okirikiri., na ihe ize ndụ na-dobere site na ike isi, stric nnukwu na ogologo oge ụdị arụ ọrụ na-anọdụ ala tupu amine abịarute.

Nchịkọta nyocha nke onwe ya nke data ntụnyere kwesịrị ka ehota ya na oke ya adịghị mma. Na njikọ siri ike nke Gly-Phe-Pro-NH₂, kọrọ epimerisation bụ 29.8% na EDC/HOAt, 24.1% na EDC·HCl/HOAt na 4.2% na DIC/HOAt. Ndị a bụ ọnụ ọgụgụ n'usoro ihe nlere anya ekpokọtara site na ọmụmụ ihe izizi e zoro aka na ya; ha anaghị ewepụta ọkwa izugbe nke EDC megide DIC n'ofe usoro, na ntụleghachi n'ebe ọzọ na-ekwu na n'ụfọdụ ntụnyere ihe dị iche n'etiti EDC na DCC bụ obere. Nke abụọ, Ebe data ekepụtara iche na-abịa site na akwụkwọ teknụzụ ndị na-ere ahịa na-atụnyere ihe nrụpụta histidine: Fmoc-Ya(Trt)-OH tinyere HCTU/6-Cl-HOBt/DIPEA nyere 1% racemisation enweghị preactivation na 7.8% na nkeji ise nke preactivation, mgbe Fmoc-His(MBom)-OH n'okpuru otu preactivation nyere 0.3%. Nke ahụ bụ ntụnyere ndị na-ere ahịa nke usoro na ọnọdụ akọwapụtara, ọ bụghị nkwupụta na nchebe Trt adịghị mma maka histidine.

Nkwupụta ahụ emeziri bụ ọnọdụ: reagent, mgbakwunye, isi na oge mbido nke ọ bụla na-agbanwe nsonaazụ epimerisation, na nha nke ngbanwe ahụ dabere na ihe fọdụrụ na-arụ ọrụ yana n'otú njikọ ahụ si dị ngwa ngwa. Ngwakọta ngwa ngwa n'okpuru ọnọdụ ndị bụ isi bụ ebe ụdị ndị na-arụ ọrụ nwere oge ịgba ígwè. Ya mere a ga-atụta iguzosi ike n'ezi ihe stereochemical - site na nyocha chiral, Onye nrụpụta Marfey, ma ọ bụ chromatography dị elu nwere ike dozie diastereomer - kama ịpụta site na njikọ dị ọcha..

Echiche na-ezighi ezi 4: "Otu nọmba ịdị ọcha na-agwa gị na usoro ahụ ziri ezi"

Njehie ahụ bụ ịgụ pasentị ịdị ọcha dị ka nkwupụta njirimara. Mpaghara HPLC% na-aza ajụjụ dị warara: nke ihe na eluted na achọpụtara na ahọrọ ogologo wavelength, kedu ihe ntakiri dị n'isi kacha elu? O kwughị ihe ọnụ ọgụgụ ahụ bụ. Usoro ihichapụ, diastereomer sitere na epimerisation, ma ọ bụ ngwaahịa sitere na aspartimide nwere ike imekọrịta ihe na ebumnuche n'okpuru otu ọnọdụ gradient., na nke Molecules nyochaa n'ụzọ doro anya na ngwaahịa epimerised nwere ọdịdị anụ ahụ yiri nke ahụ, nke mere na ọ na-esiri ha ike ime ka ha dị ọcha. Nke Ntuziaka teknụzụ ChemPep Fmoc SPPS na-eme ka ihe yiri ya si n'akụkụ ọrụ: Ọnọdụ njikọ "ọkọlọtọ" nwere ike inye njikọ na ngwaahịa na-ezughị ezu gụnyere epimers., peptides ewepụghị na ngwaahịa nke mgbawa Fmoc akaghi aka.

Mass spectrometry na-emechi akụkụ nke oghere ahụ mana ọ bụghị ya niile. Uka ahụrụ anya dabara na oke agbakọrọ na-akwado nhazi, bụghị usoro ọnọdụ - a scrambled usoro na otu ihe fọdụrụ ọdịnaya na-enye otu uka. Ozi ọnọdụ chọrọ tandem MS, Edman mmebi, ma ọ bụ NMR maka obere peptides. Iche iche, ụdị counterion (TFA na ndabara na ọtụtụ katalọgụ, na acetate, chloride ma ọ bụ ammonium mgbanwe dị), Ọdịnaya mmiri na ọdịnaya peptide net bụ ọnụọgụ dị iche na ịdị ọcha, na a 98% Ọnụ ọgụgụ HPLC ekwughị ihe ọ bụla gbasara nke ọ bụla n'ime ha.

Oke bụ na njirisi nnabata na-adabere na iji ebumnuche emebere ya. Reagenti ọkwa nyocha maka nyocha in-vitro yana ihe ezubere maka ọrụ izizi anaghị ebu otu nkọwapụta., na asambodo ọkwa ọkwa nyocha abụghị nkọwapụta ọgwụ. Tebụlụ dị n'okpuru bụ usoro nyocha maka ikpebi akara nyocha ga-ekpughe ọdịda; ọ bụghị usoro a kwadoro, na njedebe nchọpụta dabere na kọlụm, gradient, wavelength na ngwá eji.

Tebụl: Ebumnuche mmeghachi omume, njirimara akụkụ mmeghachi omume, na ihe akaebe diagnostic

Nzọụkwụ mmeghachi omume

Ebumnuche

Mmeghachi omume akụkụ nwere ike ime

Ihe akaebe nyocha

Carboxyl ịgbalite

Tụgharịa carboxyl ka ọ bụrụ ụdị amine nwere ike ịwakpo

Epimerisation site na oxazol-5(4H)-otu; N-acyl urea nwere carbodiimides; mmeghachi omume akaghi aka na nucleophiles n'akụkụ-agbụ

Diastereomer kacha elu na chiral ma ọ bụ nnukwu mkpebi HPLC; uka ọzọ kwekọrọ na urea acyl na LC-MS

Amide bond guzobere (njikọ)

Gbatịa yinye ahụ otu ihe fọdụrụ

Njikọ na-ezughị ezu na-enye usoro nhichapụ; mgbakwunye okpukpu abụọ; ngwaahịa guanylation nwere reagents uronium

-Ngbanwe oke AA na LC-MS; +Mgbanwe nke oke AA; njirimara guanidinium uka

Fmoc dep Ụlọ ọrụ Peptides akpọrọ ntụgharị

Wepu Nα-amine maka okirikiri na-esote

Nchekwa ezughị ezu; nhazi aspartimide na Asp-Xxx n'okpuru ọnọdụ ndị bụ isi; diketopiperazine guzobe mgbe mgbochi nke ụfọdụ dipeptidyl-resin intermediates

Fmoc fọdụrụnụ nke UV ma ọ bụ MS; +18/-18 Da ụkpụrụ si aspartimide mgbanaka oghere ruo α- na ngwaahịa β-aspartyl; ọnwụ nke oke dipeptide

Mkpuchi agbụ akụkụ Ndozigharị Peptide na mgbawa

Hapụ peptide ahụ ma wepụ otu nchebe nke agbụ akụkụ

Nkpọwa ezughị ezu na-ahapụ ihe fọdụrụ echedoro; ọgwụgwọ nke Cys, Met ma ọ bụ Trp site na cations cleavage-cocktail

Mwepu oke nke dabara na otu nchekwa echekwabara; na-agbapụta ọtụtụ mmadụ

Ikewapụ ikpeazụ

Wepu nnu, mgbanwe counterion, lyophilise

Mfọdụ TFA; nnukwu mmiri ọdịnaya; obere peptide net net

Ion chromatography maka TFA fọdụrụnụ; Karl Fischer maka mmiri; elemental ma ọ bụ quantitative amino acid analysis maka net peptide

Isi okwu: Usoro nyocha, ọ bụghị ụkpụrụ kwadoro. Mgbama ọ bụla na-egosi ihe ị ga-achọ; ma usoro enyere nwere ike ịchọpụta ya n'ogo dị mkpa dabere na oke nke usoro ahụ.

Echiche na-ezighi ezi 5: "Ọ bụrụ na njikọ ahụ na-arụ ọrụ, nke fọdụrụ n'ogbe ahụ dị mma"

Njehie a na-agbakọta site na otu nzọụkwụ na-aga nke ọma ruo n'ọgbọ dum. Ịrụ ọrụ njikọta na-adabere n'usoro, na ọdịda ụdịdị nke dị mkpa kasị pụta dị ka efu residues kama dị ka o doro anya na obere mkpụrụ. Nke Molecules nyochaa na-ekwu ụkpụrụ ozugbo: njikọta na nrụpụta arụmọrụ na-adalata na ogologo yinye peptide, na-emepụta mkpochapụ amino acid na usoro ezughị ezu, na iberibe C-n'ikpeazụ arụ ọrụ nwere akụkụ N-n'efu na-abawanye ohere nke epimerisation.. Ntuziaka ChemPep na-agbakwụnye nkọwa bara uru na nchịkọta peptide n'oge nhazi bụ isi ihe na-akpata nsogbu., siri ike ibu amụma, dabere n'usoro, na enweghị ngwọta zuru ụwa ọnụ - nke mere na otu usoro ahụ nwere ike ịrụ ọrụ nke ọma na otu usoro ma daa na nke ọzọ nke ogologo oge..

Atụmatụ usoro atọ kwesịrị nlebara anya kpọmkwem. Ogologo hydrophobic na-agbatị na-akwalite nchịkọta na resin na njikọ ezughị ezu, nke na-egosi dị ka usoro ihichapụ. Asp-Xxx motifs na-adịkarị mfe ịmepụta aspartimide n'okpuru ọnọdụ bụ isi nke nchebe Fmoc., inye α- na β-aspartyl ngwaahịa mgbe mgbanaka meghere. Ụfọdụ dipeptidyl-resin intermediates nwere ike ịgba ọsọ gaa diketopiperazines mgbe nchebe., na-agbaji agbụ ahụ tupu njikọ ọzọ. Ọ dịghị nke ọ bụla n'ime ihe ndị a na-ekwupụta onwe ya dị ka obere njikọ njikọ n'oge ahụ; nke ọ bụla na-apụta ma emechaa dị ka adịghị ọcha gbanwere oke.

Nzọrọ agbaziri bụ na a na-ewepụta ogo batch site na data nyocha akọwapụtara n'ofe ụzọ orthogonal., na ihe akaebe kwesịrị ekwesị setịpụrụ dabere na ogologo usoro, hydrophobicity na mgbanwe ọdịnaya. Nke dị mkpirikpi, hydrophilic, peptide na-agbanweghị agbanwe yana peptide hydrophobic 40-residue nwere disulfides abụọ anaghị akwado otu nnwale ntọhapụ., na-emeso ha dị ka hà bụ otú nkọwa nke anya siri ike ejedebe na-ekwu obere ihe.

Ihe atụ: ebe ajuju adighi etinye

Ndị na-abụghị ribosomal peptide synthetases bụ ikpe ebe "mmeghachi omume na-emepụta peptide" nwere azịza dị iche n'ezie., na ebe kemịkalụ-njikọta framing adịghị enyefe. Nke nyochaa nhazi nke NRPS enzymology na-akọwa enzymes modular nke modul ọ bụla na-etinye otu ihe fọdụrụ n'ime ya. A na-arụ ọrụ amino acid dị ka acyl-adenylate site na ngalaba adenylation, wee bufee ya dị ka thioester na ogwe aka phosphopantetheine nke protein na-ebu peptidyl., na njikọ peptide na-etolite na ngalaba condensation nke nwere ebumnuche HHxxxDG echekwara echekwara. Ngalaba thioesterase ọnụ na-ewepụta ngwaahịa ahụ.

Ọdịiche atọ na-eme ka usoro kemịkal ghara ịdị irè. Ọ dịghị exogenous njikọ njikọ reagent - ebighị bụ enzymatic na ATP-dabere. Enweghị okirikiri nchekwa Nα, n'ihi na protein ndị na-ebu ibu na-ejide mkpụrụ osisi ma na-ebuga ya na ngalaba ziri ezi. Na stereochemistry ka edobere site na nhọrọ enzyme karịa site na ọnọdụ ịgbalite, nke bụ ka ụzọ NRPS si ejikọta D-amino acid na-enweghị nsogbu epimerisation nke na-etinye Molecules nyochaa. Akpadoro Peptides N'ogbe

Nyocha ahụ doro anya gbasara oke nke ya, na oke ndị ahụ kwesịrị iji ihe atụ na-aga njem. Akụkụ akụkụ condensation dịnụ enweghị njikọ nke ala na saịtị nọ n'ọrụ, Ya mere, a ka ga-eguzobe kpọmkwem ọrụ nke ihe fọdụrụ na saịtị na-arụ ọrụ na njide na catalysis, na ike nke condensation ngalaba adịghị edozi. Ya mere ihe nlere anya a na-akwado ọdịiche dị n'ụdị - mgbakọ enzymatic nke e depụtara na njikọ kemịkalụ reagent na-ebugharị - ọ bụghị usoro nhazi zuru ezu n'etiti ha abụọ..

Ihe ị ga-arịọ mgbe ị na-enweghị ike ịme nyocha ahụ n'onwe gị

Maka ndị na-agụ akwụkwọ na-arụ ọrụ nhazi kama ịme ya, nghọtahie ise ahụ na-atụgharị n'ime ndepụta dị mkpirikpi nke ihe ị ga-arịọ. Isi ihe abụghị ịchọ ihe ọ bụla maka peptide ọ bụla, mana iji dakọtara ihe akaebe na ụdị ọdịda a na-ekpughe usoro a n'ezie.

  • Otutu HPLC nwere ọtụtụ usoro. Ogidi, gradient, wavelength na oge ịgba ọsọ, ya mere enwere ike ịkọwa ọnụ ọgụgụ dị ọcha kama iburu ntụkwasị obi. Otu esi agwakọta Peptides

  • MS nwere ahụrụ anya na oke gbakọọ. Ụkpụrụ abụọ a, ya mere enwere ike ịlele ntụnyere ahụ.

  • Saịtị mgbanwe na kemistri. Kedu ihe fọdụrụ na-ebu akara, Kedu otu nchekwa ejiri mee ihe, na ihe mgbanwe uka a na-atụ anya ya bụ.

  • Ụdị mgbochi. TFA na ndabara na ọtụtụ katalọgụ, na acetate, chloride ma ọ bụ ammonium mgbanwe dị na arịrịọ.

  • Nnwale stereochemical ma ọ bụ ọdịnaya ebe usoro kwadoro ya. Nyocha nke Chiral maka ihe fọdụrụ na-adịkarị mfe nke epimerisation; peptide ọdịnaya site na elemental ma ọ bụ quantitative amino acid analysis ebe peptide net dị mkpa karịa mpaghara%.

Mgbanwe MOL na-eji data ntọhapụ HPLC na MS na-arụ njikọ omenala ma na-enye mkpebi ọdịnaya nhọrọ, Nnwale endotoxin na ule ịmụ nwa maka usoro ebe nkọwapụta ndị ahụ metụtara; Usoro akọwapụtara na iji ebumnuche ezuru ezu iji rịọ maka nkọwa dabara adaba. Ụdị ihe nyocha nke ụdị a bụ maka ọrụ ụlọ nyocha, ọ bụghịkwa ngwaahịa ọgwụ ma ọ bụ ihe a kpochapụrụ maka ojiji mmadụ..

Nkpughe: MOL Mgbanwe bụ onye na-emepụta peptide azụmahịa ma nwee mmasị azụmahịa na ụkpụrụ àgwà ndị a tụlere ebe a.

Isi mmalite

FAQ

Kedu klas mmeghachi omume na-emepụta njikọ peptide, na gịnị ka activation na-agbakwụnye? Mwepụta nke njikọ amide site na nnọchi nucleophilic acyl na carbon carboxyl. Nrụ ọrụ na-atụgharị carboxyl ka ọ bụrụ electrophile ka mma - O-acylisourea, ester na-arụ ọrụ, ma ọ bụ ụdị uronium / phosphonium enwetara - ya mere amine nwere ike ịwakpo n'okpuru ọnọdụ dị nro. Ngụkọta condensation bụ nguzozi atọm net nke mgbanwe ahụ, ọ bụghị usoro.

Fmoc ma ọ bụ Boc ọ ka mma maka usoro ịgba ọsọ na-adịkarị mfe? Ọ dabere na ihe fọdụrụ na ọnọdụ njikọ, na ihe akaebe anaghị akwado azịza blanketị. Nke Molecules nyochaa na-ekwu na Fmoc deprotection na-eji ntọala, nke dabara na residues nwere mmetụta, ebe Boc chemistry na-eji acid; ma otu nyochaa na-egosi na njikọ njikọ reagent, nhọrọ mgbakwunye na isi na-achịkwa nsonaazụ epimerisation. Maka otu usoro, azịza bara uru bụ ịchọpụta ihe fọdụrụ nwere nnukwu ihe ize ndụ wee rịọ maka usoro nyocha nke ga-achọpụta epimers ha..

Nwere ike ịbụ peptide 98% dị ọcha site na HPLC ma ka bụrụ molekul na-ezighi ezi? Ee. Mpaghara% na-akọwa akụkụ dị nta nke ihe achọpụtara na isi elu, ọ bụghị ihe kacha elu ahụ bụ. Usoro ihichapụ, diastereomer ma ọ bụ ngwaahịa na-emekọrịta ihe nwere ike ịchịkwa chromatogram n'okpuru otu ọnọdụ.. Identity chọrọ MS gbakwunyere usoro na-enye ozi ọnọdụ, na ọdịnaya, counterion na mmiri bụ nha dị iche iche ọzọ.

mmeghachi omume condensation na-akọwakwa ka mkpụrụ ndụ na enzymes NRPS si eme peptides? Mba. Ribosomal na ndị na-abụghị ribosomal biosynthesis na-etolite amide bond, ma site n'ụdị enzymatic nke template - arụ ọrụ acyl-adenylate, thioester tethering na protein na-ebu, na condensation-ngalaba catalysis - na-enweghị exogenous njikọta reagent na enweghị usoro nchebe-otu.. Ntụle atọm net yiri nke ahụ; kemistri na-enweta ya abụghị.

Nkpughe nke onye mbipụta: MOL Mgbanwe na-enye ọrụ peptide ma nwee mmasị azụmahịa na isiokwu a. Ogo ọrụ na nkwupụta ikike bụ nkwupụta ndị na-ebubata ya; nnweta na ịrụ ọrụ maka otu ihe owuwu chọrọ ihe akaebe akọwapụtara nke ọma.

Xiaoxia Chen

Xiaoxia Chen

Ọgwụ ọhụrụ R&D nka nka Ọkachamara isi: Nchọpụta ebumnuche, nhazi-mmekọrịta ọrụ (SAR) nyocha, peptide-ọgwụ conjugates (Ndị PDC), na mmepe nke mgbochi ịka nká na metabolic peptides.

Profaịlụ: Xiaoxia Chen eduzila nchọpụta mmalite na nyocha nke ọma maka ọtụtụ ọgwụ peptide nke metabolic na etuto ezubere iche.. Ọ bụghị naanị na ọ maara nke ọma na nyocha ụlọ akwụkwọ peptide dị elu kamakwa ọ makwara nke ọma n'iji usoro mgbakọ na mwepụ na-enyere AI aka maka imewe usoro peptide de novo.. Ugbu a, ọ na-eduga otu ndị raara onwe ha nye nyocha miri emi na mmepe nke agonists multifunctional ọgbọ na-abịa (dị ka dual- ma ọ bụ peptides na-ebelata abụba ebumnobi okpukpu atọ) na anụ ahụ na-arụsi ọrụ ike nke ukwuu-ndozi peptides.

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