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澶氳偨淇グ: Linkers, spacers and PEGylation
鑱氫箼浜岄唶鍖栨槸鑱氫箼浜岄唶錛圥EG錛夎仛鍚堢墿閾鵑氳繃鍏變環(huán)閿繛緇撲簬澶氳偨鎴栬泲鐧借川銆傞氳繃澧炲姞铔嬬櫧璐ㄥ拰鑲界殑鍒嗗瓙璐ㄩ噺騫朵繚鎶や粬浠笉鍙楄泲鐧介叾姘磋В錛岃仛涔欎簩閱囧寲鍙彁楂樿嵂鐗╁姩鍔涘銆傝仛涔欎簩閱囧寲鍙檷浣庤偩娓呴櫎鐜囷紝浠庤屼嬌寰楀湪鐨笅緇欒嵂鍜屽垎鏁ｅ彈闄愭儏鍐典笅浠嶈兘鎸佷箙鍚告敹銆?/p>
鑽悊浼樺娍錛?/p>
- 鏀瑰杽鑽墿婧惰В搴﹀拰淇濇姢鍏朵笉琚泲鐧介叾闄嶈В銆侾EG鑱氬悎鐗╁強鍏剁浉鍏蟲按鍒嗗瓙灝卞儚涓涓繚鎶ょ僵錛屼繚鎶よ嵂鐗╁厤鍙楅叾鐨勯檷瑙ｏ紝浠庤岄檷浣庝簡涓嶈壇鍏嶇柅鍙嶅簲銆備笌鏈繘琛岃仛涔欎簩閱囧寲鐨勮嵂鐗╃浉姣旓紝鍦╬H鍊煎拰娓╁害鍙樺寲鐨勫緢澶ц寖鍥村唴錛岃仛涔欎簩閱囪嵂鐗╅兘鏇寸ǔ瀹氥?/li>
- 鍥犲噺灝戜簡緇欒嵂鍓傞噺銆侀鐜囷紝浠庤岄檷浣庝簡娼滃湪姣掓с侾EG鍑犱箮娌℃湁姣掓э紝鍏跺彲琚偩 (PEGs< 30 kDa)鎴栫勃渚?PEGs> 20 kDa)瀹屽叏娓呴櫎銆?/li>
- 澧炲姞鑽墿鐨勭ǔ瀹氭у茍寤墮暱鑽墿鐨勫驚鐜鍛姐侾EG娌℃湁鍏嶇柅鍘熸э紝濡傛灉PEG涓庨珮鍏嶇柅鍘熸ц泲鐧界粨鍚堬紝閽堝PEG鐨勬姉浣撳彧浼氬湪鍏斿瓙浣撳唴浜х敓銆?/li>
娉芥邯婧愬彲浠ュ澶氳偨榪涜mini-PEGs淇グ銆備互涓嬪垪鍑哄皯璁鎬緥瀛愶細
- {Gly}, 2 Carbons
- {Beta-Ala}, 3 Carbons
- {GABA}, 4 Carbons
- {Ava}, 5 Carbons
- {AEA}, Aminoethoxyacetic Acid
- {ANP Linker}
- {Ahx}, 6 Carbons:
- Fmoc-蔚-Ahx-OH錛屾垨N-蔚-Fmoc-蔚-aminocaproic acid錛屾垨 Fmoc-6-aminohexanoic acid錛汣AS鍙? 88574-06-5錛涘垎瀛愰噺錛?53.42 g/mol銆?/li>
- 鐮旂┒鏄劇ず錛屼笌Lys(Ahx)涓璧峰悎鎴愶紝鍙互鏈夋洿濂界殑鏀剁泭鐜囥傚彲鑳界敱浜庡湪鍚堟垚榪囩▼涓伒媧葷殑Ahx鏈夊姪浜庝嬌澶氳偨閾懼憟閫傚綋鐨勬憾鍓傚寲鐗╋紝閬垮厤浜嗚仛闆嗭紝浠庤屽鍔犱簡澶氳偨搴忓垪寤墮暱鐨勫彲鑳姐?/li>
- 鍦ㄥ埗澶嘑ITC鏍囪澶氳偨鏃訛紝Ahx鎴朾-Ala鍧囧彲鎴愬姛鍦頒綔涓簂inker浣跨敤銆傝繖浼氳鑽у厜鏍囩鏇寸ǔ瀹氥傞氳繃涓庡崐鑳辨皚閰哥殑宸熀鎴栬禆姘ㄩ吀鐨勬皚鍩虹粨鍚堬紝FITC鍙鏍囪鍦ㄥ鑲界殑浠諱綍浣嶇疆銆?/li>
- {Mini-PEG}, 9 Carbons, CAS number: 166108-71-0; Fmoc-NH-(PEG)-COOH, or Fmoc-8-amino-3,6-dioxaoctanoic acid; Molecular weight: 385.42 g/mol; C21H23NO6
- {Mini-PEG2}, 13 Carbons, CAS number: 867062-95-1; Fmoc-NH-(PEG)2-COOH, or Fmoc-12-amino-4,7,10-trioxadodecanoic acid; Molecular weight: 443.5 g/mol; C24H29NO7
- {Mini-PEG3}, 16 Carbons, CAS number: 557756-85-1; Fmoc-NH-(PEG)3-COOH, or Fmoc-15-amino-4,7,10,13-tetraoxapentadecanoic acid; Molecular weight: 489.57 g/mol; C26H35NO8
澶氳偨鍚堟垚鍦ㄧ嚎鎶ヤ環(huán)錛?/p>
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