Fmoc-hArg(Pbf)-OH he pärönaki waikawa amino koretake e mau ana ki nga roopu tiaki orthogonal, i tino arotauhia mo te whakahiato peptide-waa toka Fmoc paerewa (SPSS). Ma te whakauru i te homoarginine (h Te riri)—kei roto i te roopu methylene kotahi atu i te arginine maori—ki te raupapa peptide, ka tino whakanui ake i te pumau o te proteolytic me te kaha o te whakaurunga o nga raau taero peptide. Ko tana mekameka taha e tiakina ana e te roopu Pbf paerewa-ahumahi, he tino koretake i te wa o te waikawa trifluoroacetic (TFA) wehewehenga, whai hua te whakaiti i nga tauhohenga taha. He poraka hanga pai mo te whakahiato i te parakore teitei, peptides whakarerekē matatini.
Raupapa
Fmoc-hArg(Pbf)-OH
Tau CAS
1159680-21-3
Tātai rāpoi
C35H42N4O7S
Taumaha rāpoi
662.80
Te matū & Nga Painga Whakakotahitanga Fmoc-hArg(Pbf)-He pai te hono a OH ki nga rautaki whakahiato peptide toka-waa Fmoc/tBu hou. I roto i te whakahiato peptide, Ko te whakamarumaru me te whakakore i te roopu guanidino tino kaha he wero matua. Ko te mekameka taha o tenei hua ka whakamahi i te Pbf (2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl) rōpū tiaki. Ka whakatauritea ki nga roopu Pmc, Mtr ranei, Ka whakawhiwhia e te Pbf nga painga nui:
- Te Waahi Tere: I roto i te taahiraa wehenga TFA whakamutunga, ko te tere tangohanga o te Pbf he tere ake i era atu roopu whakamarumaru sulfonyl.
- Te whakakore i nga tauhohenga taha: Ko te whakaheke tere ka whakaiti i te tupono o nga tauhohenga taha alkylation na te warowaihā i runga i nga mekameka taha o nga waikawa amino tairongo penei i te tryptophan. (Trp), na reira ka tino whakapai ake i te ma me te hua o te peptide masivesivá.
Tuhinga o mua i roto i te Peptide Drug Discovery Hei waikawa amino koretake, homoarginine (h Te riri) he anga waro he kotahi te methylene te roa ake i te arginine maori. I roto i te hoahoa tarukino auaha, ko tenei whakarereketanga iti o te hanganga ka whai hua nui te koiora:
- Pūmautanga Enzymatic: Ko nga protease taiao (penei ko Trypsin) ka mohio me te wehe i te C-terminus o Arg, Lys ranei. Ko te whakakapi i a Arg me te hArg rerekee ka taea e te peptide te karo i te tohu protease., na reira ka tino roa te haurua o nga raau taero peptide i roto i te plasma.
- Whakanuia te Whakaaetanga Pūkoro: I roto i nga rangahau e pa ana ki nga peptides-puu-nui-a-Guanidino (CPPs), ko te taapiri mokowhiti e whakaratohia ana e te hArg ka arotau i te aratau here i waenga i te roopu guanidino me te heparan sulfate i runga i te mata o te membrane pūtau., na reira ka tino pai ake te pai o te tuku whakawhiti o nga raau taero macromolecular.
COA
HPLC
MS
- Te Whanaketanga Tuatahi me nga Painga Matū o te Roopu Tiaki Pbf:
Hornbeam, L. A., Shroff, H., Triol, S. A., Mansour, E. M., Wenschuh, H., & Albericio, F. (1993). “Ko te roopu 2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl (Pbf) hei parenga mekameka taha arginine.” Journal of the American Chemical Society, 115(10), 4397-4398. Puna Whakamana: DOI: 10.1021/ja00063a082
- Nga Kawa Paerewa mo te Fmoc SPPS me te Tono Pbf:
Chan, W. C., & Mā, P. D. (2000). Fmoc Wāhanga Mārō Peptide Synthesis: He Tikanga Mahinga. Oxford University Press. (Tirohia nga wharangi 58-60 mo nga tono paerewa mo te whakamarumaru taha-mekameka o arginine). Puna Whakamana: ISBN: 978-0199637249
- Te Whakamana Koiora mo te Roa-Taha-Taha (Homoarginine) i runga i te Whakapai ake i te Mahinga Pūkoro:
Wender, P. A., Mitchell, D. J., Pattabiraman, K., Pelkey, E. T., Steinman, L., & Rothbard, J. B. (2000). “Ko te hoahoa, whakahiato, me te arotakenga o nga ngota ngota ka taea, ka whakakaha ake ranei i te tango i nga waea: Kaikawe ngota ngota peptoid.” Nga Mahi a te National Academy of Sciences, 97(24), 13003-13008. Puna Whakamana: DOI: 10.1073/pnas.97.24.13003
