姘ㄥ熀閰告槸妲嬫垚铔嬬櫧璩殑鍩烘湰鍠綅锛屼篃鏄敓鐗╅珨鐢熷懡娲诲嫊鎵€蹇呴渶鐨勯噸瑕佹湁姗熷寲鍚堢墿銆傚畠鍊戜笉鍍呭湪铔嬬櫧璩悎鎴愪腑璧烽棞閸典綔鐢紝閭勫弮鑸囦簡瑷卞鐢熺悊閬庣▼锛屽浠ｈ瑵瑾跨瘈銆佺缍撳偝灏庡拰鍏嶇柅鍙嶆噳銆傝繎骞翠締锛岄毃钁楃敓鐗╅啱瀛告妧琛撶殑鐧煎睍锛屾皑鍩洪吀鐨勭爺绌堕牁鍩熷緱鍒颁簡妤靛ぇ鐨勬摯灞曪紝灏ゅ叾鏄湪鐤剧梾娌荤檪銆佺嚐椁婅鍏呭拰鍚堟垚鐢熺墿瀛镐腑鐨勬噳鐢紝鍌欏彈闂滄敞銆�
楹ュ厠鏋楁彁渚涘悇椤炴皑鍩洪吀瑭﹀姂鍙婂叾琛嶇敓鐢㈠搧锛屽叿鏈夌磾搴︾瓑绱氶珮銆佺敓鐢㈠伐钘濆厛閫层€佹敮鎸佺爺鐧煎畾鍒剁瓑鐗归粸锛岃兘琚唬娉涢仼鐢ㄤ簬鍚勯绉戠爺闋呯洰銆佺爺绌跺椹椾腑锛屾杩庨伕璩笺€�
鏈枃閫氶亷浠ヤ笅骞鹃粸绨″柈浠嬬垂楹ュ厠鏋楁皑鍩洪吀瑭﹀姂鐨勭敘鍝佺壒鎬у強鐩搁棞鎳夌敤锛�
1. 姘ㄥ熀閰哥殑鍩烘湰鎬ц唱鍜屽垎椤�
2. 闈炲ぉ鐒舵皑鍩洪吀鐨勬噳鐢ㄨ垏鐮旂┒
3. 淇濊姘ㄥ熀閰稿湪鍖栧鍚堟垚涓殑閲嶈鎬�
4. 姘ㄥ熀閰哥殑鎳夌敤
5. 楹ュ厠鏋楁皑鍩洪吀瑭﹀姂鍙婅鐢熺敘鍝佷粙绱�
姘ㄥ熀閰哥殑鍩烘湰鎬ц唱鍜屽垎椤�
姘ㄥ熀閰稿垎瀛愮敱涓€鍊嬫皑鍩猴紙-NH?锛夈€佷竴鍊嬬晶鍩猴紙-COOH锛夈€佷竴鍊嬫矮鍘熷瓙浠ュ強涓€鍊嬬壒瀹氱殑鍋撮張锛圧鍩哄湗锛夌祫鎴愩€傛牴鎿歊鍩哄湗鐨勪笉鍚岋紝姘ㄥ熀閰稿叿鏈変笉鍚岀殑鐗╃悊鍖栧鎬ц唱锛岄€欎簺鎬ц唱鐩存帴褰遍熆瀹冨€戝湪铔嬬櫧璩腑鐨勫姛鑳藉拰绲愭绌╁畾鎬с€傛皑鍩洪吀鍙互鏍规摎鍏朵締婧愬拰鍚堟垚閫斿緫閫茶鍒嗛锛屽寘鎷ぉ鐒舵皑鍩洪吀鍜岄潪澶╃劧姘ㄥ熀閰搞€傚ぉ鐒舵皑鍩洪吀鏄嚜鐒剁晫涓父瑕嬬殑20绋婧栨皑鍩洪吀锛岃€岄潪澶╃劧姘ㄥ熀閰稿墖鏄€氶亷鍖栧鍚堟垚銆侀叾淇冨弽鎳夋垨鍩哄洜宸ョ▼鎶€琛撳紩鍏ュ埌铔嬬櫧璩腑鐨勪笉甯歌姘ㄥ熀閰搞€傞€欎簺闈炲ぉ鐒舵皑鍩洪吀鐨勫紩鍏ユ摯灞曚簡姘ㄥ熀閰哥殑鍔熻兘鑼冨湇锛屼娇寰楃瀛稿鍊戣兘澶犺ō瑷堝嚭鍏锋湁鐗规畩鎬ц唱鐨勮泲鐧借唱鎴栧垎瀛愩€�
闈炲ぉ鐒舵皑鍩洪吀鐨勬噳鐢ㄥ拰鐮旂┒
闈炲ぉ鐒舵皑鍩洪吀鍦ㄧ敓鐗╁鐮旂┒鍜岀敓鐗╁伐绋嬩腑鐨勬噳鐢ㄦ棩鐩婂唬娉涖€傞€氶亷灏囬潪澶╃劧姘ㄥ熀閰稿紩鍏ュ埌铔嬬櫧璩腑锛岀爺绌朵汉鍝¤兘澶犺肠浜堣泲鐧借唱鏂扮殑鍔熻兘锛屾垨鏄爺绌剁壒瀹氬姛鑳藉熀鍦樺皪铔嬬櫧璩椿鎬х殑褰遍熆銆備緥濡傦紝鍦ㄧ敓鐗╂浜ゅ寲瀛稿弽鎳変腑锛屽埄鐢ㄩ潪澶╃劧姘ㄥ熀閰稿彲浠ュ紩鍏ョ壒瀹氱殑妯欒鎴栨帰閲濓紝瀵︾従灏嶈泲鐧借唱鐨勫鏅傝拷韫ゅ拰瀹氫綅銆�
鍦�1 闈炲ぉ鐒舵皑鍩洪吀鐨勭窗鑳炴懟鍏ヨ垏铔嬬櫧璩殑鐢熺墿姝ｄ氦妯欒[1]
姝ゅ锛岄潪澶╃劧姘ㄥ熀閰稿湪钘ョ墿闁嬬櫦涓篃灞曠従鍑虹崹鐗圭殑鍎嫝銆傞€氶亷鏀硅畩姘ㄥ熀閰稿伌閺堢殑绲愭锛屽彲浠ヨō瑷堝嚭鏇村叿绌╁畾鎬у拰鐗圭暟鎬х殑钘ョ墿鍒嗗瓙銆傞€欑ó鎶€琛撳凡缍撹鐢ㄤ簬闁嬬櫦鏂板瀷鐨勮泲鐧借唱钘ョ墿锛屽鎶楅珨鍜岄叾椤炶棩鐗╋紝閫蹭竴姝ユ帹鍕曚簡绮炬簴閱鐨勭櫦灞曘€�
鍦�2 涓€绋湪楂斿収灏囬潪澶╃劧姘ㄥ熀閰哥壒鐣版€у紩鍏ヨ泲鐧借唱鐨勯€氱敤鏂规硶銆侾Pi = 鐒︾７閰搁菇[2]
淇濊姘ㄥ熀閰稿湪鍖栧鍚堟垚涓殑閲嶈鎬�
鍦ㄦ皑鍩洪吀鐨勫寲瀛稿悎鎴愬拰澶氳偨鍚堟垚閬庣▼涓紝淇濊鍩哄湗鐨勪娇鐢ㄨ嚦闂滈噸瑕併€備繚璀锋皑鍩洪吀鏄寚鍦ㄦ皑鍩洪吀鐨勫悎鎴愰亷绋嬩腑锛岄棞閸电殑娲绘€у熀鍦樿鏆檪淇濊璧蜂締锛屼互閬垮厤涓嶅繀瑕佺殑鍓弽鎳夈€備緥濡傦紝鍦ㄥ浐鐩稿鑲藉悎鎴愪腑锛屼娇鐢ㄤ繚璀峰熀鍦樺彲浠ョ⒑淇濇皑鍩洪吀鐨勬皑鍩哄拰缇у熀鍦ㄧ壒瀹氭椹熶腑淇濇寔涓嶆椿韬嶏紝鍙湁鍦ㄩ渶瑕佹檪鎵嶈閲嬫斁閫茶鍙嶆噳銆傞€欑ó绛栫暐妤靛ぇ鍦版彁楂樹簡鍚堟垚寰╅洔澶氳偨鍜岃泲鐧借唱鐨勬晥鐜囪垏绮惧害銆傚湪鐝句唬鍚堟垚鍖栧涓紝淇濊姘ㄥ熀閰哥殑鎶€琛撹寤ｆ硾鎳夌敤浜庨枊鐧兼柊鍨嬭棩鐗╁拰鍔熻兘鎬х敓鐗╂潗鏂欙紝鐐哄寲瀛稿悎鎴愮殑鍙潬鎬у拰鍙帶鎬ф彁渚涗簡淇濋殰銆�
鍦�3 鍥虹浉鑲藉悎鎴愶紙SPPS锛夌殑閬庣▼[3]
姘ㄥ熀閰哥殑鎳夌敤
闅ㄨ憲绉戝鎶€琛撶殑閫叉锛屾皑鍩洪吀鍦ㄥ鍊嬮牁鍩熺殑鎳夌敤寰楀埌浜嗗唬娉涚櫦灞曘€傚湪鐕熼瀛搁牁鍩燂紝姘ㄥ熀閰歌鍏呭姂宸茶寤ｆ硾鐢ㄤ簬閬嬪嫊鍝°€佽€佸勾浜哄拰鐗规畩浜虹兢鐨勮喅椋熻鍏咃紝浠ユ敼鍠勮韩楂旀鑳藉拰鎻愰珮鍏嶇柅鍔涖€�
鍦ㄩ啱钘ラ牁鍩燂紝姘ㄥ熀閰镐綔鐐鸿棩鐗╅枊鐧肩殑鍩虹鏉愭枡锛屽叿鏈夐噸瑕佺殑鎳夌敤鍓嶆櫙銆備緥濡傦紝L-绮炬皑閰稿湪蹇冭绠＄柧鐥呯殑娌荤檪涓捣鍒伴噸瑕佷綔鐢紝鍏堕€氶亷涓€姘у寲姘悎鎴愰€斿緫鏀瑰杽琛€绠″姛鑳姐€傝胺姘ㄩ叞鑳哄墖琚唬娉涚敤浜庨噸鐧ユ偅鑰呯殑鐕熼鏀寔娌荤檪锛岀壒鍒ユ槸鍦ㄦ噳婵€鐙€鎱嬩笅锛屾湁鍔╀簬鍏嶇柅鍔熻兘鐨勭董鎸併€�
姘ㄥ熀閰搁倓鍦ㄥ悎鎴愮敓鐗╁鍜岀敓鐗╁伐绋嬮牁鍩熶腑寰楀埌鎳夌敤銆傞€氶亷鍩哄洜宸ョ▼鎵嬫锛屽彲浠ュ悎鎴愬叿鏈夌壒瀹氬姛鑳界殑闈炲ぉ鐒舵皑鍩洪吀锛屽緸鑰岃ō瑷堝嚭鏂板瀷铔嬬櫧璩垨閰躲€傞€欑偤钘ョ墿闁嬬櫦銆佹潗鏂欑瀛稿拰宸ユキ閰剁殑鐢熺敘鎻愪緵浜嗘柊鐨勯€斿緫銆�
楹ュ厠鏋楁皑鍩洪吀瑭﹀姂鍙婅鐢熺敘鍝佷粙绱�
楹ュ厠鏋楁皑鍩洪吀瑭﹀姂鐢㈠搧鍎嫝锛�
1.绲愭鏂扮⿴銆佸搧绋箒澶�
2.绱斿害绛夌礆楂�
3.鐢熺敘宸ヨ棟鍏堥€�
4.鎺ュ彈鐮旂櫦瀹氬埗
澶╃劧姘ㄥ熀閰�
L-澶╁啲姘ㄩ吀
瓒呯磾鐢熺墿瑭﹀姂绱�, ≥99.5%(T)
L-璋锋皑閰�
Ultra pure,≥99.5%(NT)
L-铔嬫皑閰革紙鐢茬～姘ㄩ吀锛�
99%鐢熺墿鎶€琛撶礆
闈炲ぉ鐒舵皑鍩洪吀
淇濊姘ㄥ熀閰�
N-鐢查叞鍩�-DL-鑻笝姘ㄩ吀
≥99%(T)
N-姘ㄥ熀鐢查叞鍩�-DL-澶╁啲姘ㄩ吀
≥98%
N-[1-(S)-涔欐哀缇板熀-3-鑻笝鍩篯-L-涓欐皑閰�
98%
N-(2,4-浜岀鍩鸿嫰鍩�)-DL-铇囨皑閰�
99%
S-鐑笝鍩�-L-鍗婅儽姘ㄩ吀
≥98.0%(T)
鍙冭€冩枃鐛�
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[3] Wang, L., Wang, N., Zhang, W. et al. Therapeutic peptides: current applications and future directions. Sig Transduct Target Ther 7, 48 (2022).
[4] Wu, G. (2009). Amino acids: metabolism, functions, and nutrition. Amino acids, 37(1), 1-17.
Brosnan, J. T. (2003). Interorgan amino acid transport and its regulation. Journal of Nutrition, 133(6), 2068S-2072S.
[5] Li, P., et al. (2007). Amino acids and immune function. British Journal of Nutrition, 98(2), 237-252.
[6] Li, X., et al. (2021). Branched-chain amino acids and insulin resistance: From molecular aspects to clinical solutions. Journal of Molecular Medicine, 99(5), 689-703.
[7] Chin, J. W. (2014). Expanding and reprogramming the genetic code of cells and animals. Annual Review of Biochemistry, 83, 379-408.
[8] Dawson, P. E., & Kent, S. B. (2000). Synthesis of native proteins by chemical ligation. Annual Review of Biochemistry, 69(1), 923-960.
[9] Merrifield, R. B. (1963). Solid phase peptide synthesis. I. The synthesis of a tetrapeptide. Journal of the American Chemical Society, 85(14), 2149-2154.
[10] Lang, K., & Chin, J. W. (2014). Cellular incorporation of unnatural amino acids and bioorthogonal labeling of proteins. Chemical Reviews, 114(9), 4764-4806.
[11] Muir, T. W., Sondhi, D., & Cole, P. A. (1998). Expressed protein ligation: A general method for protein engineering. Proceedings of the National Academy of Sciences, 95(12), 6705-6710.