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Application of PEGylation in Recombinant Protein Drugs

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Seebio provides a wide variety of PEGs from phospholipid PEGs to fluorescent PEGs with a complete product portfolio. It also has the capability for contract development and manufacturing (CDMO/CRO) of recombinant protein drug intermediates.
PEG Modification of Proteins
PEG Modification of Proteins[1]
Recombinant proteins are obtained using recombinant DNA or RNA technology to connect gene fragments that can be translated into the desired protein to recombinant vectors. They are the core products in biologics and have significantly higher safety compared to small molecule drugs. Although the production conditions are harsh, the administration procedures are complex, and the prices are expensive, they have irreplaceable therapeutic effects on certain diseases and thus have relatively high approval rates. At the same time, the clinical trial period of recombinant protein drugs is shorter than that of small molecule drugs, with relatively extended patent protection, which gives pharmaceutical companies more exclusive profit time. These features have become an important motivator for the R&D of recombinant protein drugs.
Production Process of Recombinant Protein Drugs
Production Process of Recombinant Protein Drugs[1]
Using chemical modification and genetic engineering technologies to transform or modify recombinant protein drugs to address issues like short half-life in blood, single administration route, immunogenicity and side effects, thereby enhancing drug activity and improving efficacy, is one of the focuses in recombinant protein drug research. Long-acting protein biologics technology is also a core technology occupied by many large international companies.
Polyethylene glycol (PEG), due to its low immunogenicity, good water solubility and biocompatibility, is the most widely used polymer in biomedicine. Its "stealth" effect is the "gold standard" of biomaterials. The main PEG modification methods for protein drugs are amino modification (including N-terminal amino acylation modification, lysine side chain amino acylation modification, N-terminal amino alkylation modification), carboxyl modification, thiol modification, etc. Currently, research on PEG-modified protein drugs is mainly focused on adenosine deaminase, asparaginase, interferon, granulocyte colony stimulating factor, interleukin, etc.
CAS# N/A
TZ-Ste-SO2-nBu-AEEA-Glu(OH)-
Glu(OH)-AEEA-Lys(OH)-C
CAS# 1188328-37-1
OtBu-Ara-Glu(AEEA-AEEA-OH)-OtBu
CAS# N/A
HO-Ste-CYH-Glu(OH)-Glu(OH)-AEEEEA-Mal
After PEG covalent modification, the half-life of protein drugs is prolonged, immunogenicity is reduced, while maximally retaining its bioactivity, thus improving efficacy:
Molecular radius is increased, renal clearance rate is decreased.
PEG forms a shielding and steric hindrance effect on the protein surface, reducing the enzymatic degradation rate and increasing stability and half-life.
The shielding and steric hindrance effects can also mask antigenic sites on the protein surface, reducing the immunogenicity of the protein.
Increases the solubility of the drug in body fluids.
The chemical bond with the drug hydrolyzes over time in vivo, slowly releasing the drug[2].[2]
Various types of PEGylated proteins
Various types of PEGylated proteins[3]
Currently, R&D giants in recombinant protein drugs (Amgen, Biogen IDEC, Johnson & Johnson, Eli Lily, Novo Nordisk, Roche) are almost all from Europe and America[4], accounting for about 80% of the global market share. The sales of all European and American companies account for as high as 97% of the sales of global biotechnology companies. Since the approval of the first PEGylated protein drug, Adagen (PEG-ADA) for treatment of severe combined immunodeficiency syndrome by FDA in 1990, many other drugs have also been approved successively.
PEGs-modified protein approved FDA. Site-specific PEGylated proteins given in bold[3]

FDA Approved PEGylated Protein Drugs
Reference:

1.Y. Wei, Z.W. Zhang, et al. Chin j Biotech, 2018, 34(3): 360-368
2.K.J. Dozier, D.M. Distefano Int. J. Mol. Sci. 2015, 16(10), 25831-25864(扉页图片)
3.F.M. Veronese, G. Pasut. Drug Discov.Today, 2005, 10(21): 1451–1458

4.W.X. Wu, Y. Zhang, et al. Lett Biotechnol, 2006, 17(6): 929–934.



Seebio PEGylation Product List
Product NO. CAS Product Name Size 1 Size 2 Purity
AAU0205A 876345-13-0 Boc-NH-PEG4-CH2COOH 250mg 500mg 97%
AAU0206A 951671-87-7 DNP-PEG3-azide 100mg 200mg 98%
AAU0207A 112-35-6 m-PEG3-OH 100g 200g 97%
AAU0208A 756525-95-8 NH2-PEG2-C2-Boc 1g 2g 95%
AAU0209A 581065-95-4 Amino-PEG4-Boc 1g 2g 97%
AAU0210A 1393330-38-5 Bromo-PEG4-acid 1g 2g 97%
AAU0211A 139115-90-5 Azido-PEG2-alcohol 1g 2g 97%
AAU0212A 86520-52-7 Azido-PEG3-alcohol 5g 10g 98%
AAU0213A 305372-39-8 Biotin-PEG2-Mal 100mg 200mg 98%
AAU0214A 1453117-42-4 Tos-PEG4-acid 1g 2g 97%
AAU0215A 86259-87-2 BnO-PEG4-OH 25g 50g 97%
AAU0216A 1312309-63-9 Azido-PEG2-C2-acid 1g 2g 97%
AAU0217A 1446282-18-3 Amino-PEG5-Boc 2g 4g 98%
AAU0218A 252881-74-6 NH2-PEG3-C2-Boc 2g 4g 97%
AAU0219A 1393330-36-3 Bromo-PEG1-C2-Boc 1g 2g 97%
AAU0220A 928292-69-7 Amino-PEG10-amine 1g 2g 97%
AAU0221A 890091-43-7 Boc-amido-PEG9-amine 1g 2g 97%
AAU0222A 1859379-85-3 Propargyl-PEG2-acid 5g 10g 98%
AAU0223A 906099-89-6 Biotin-PEG6-alcohol 1g 2g 97%
AAU0224A 1800414-71-4 Azido-PEG11-amine 1g 2g 97%
AAU0225A 31127-85-2 Bis-PEG4-acid 1g 2g 98%
AAU0226A 518044-37-6 Mal-PEG6-Boc 250mg 500mg 97%
AAU0227A 437655-95-3 Fmoc-NH-PEG4-CH2COOH 5g 10g 98%
AAU0228A 1122484-77-8 NH2-PEG2-C1-Boc 1g 2g 97%
AAU0229A 144942-89-2 Amino-PEG1-C2-acid 5g 10g 98%
AAU0230A 127828-22-2 Amino-PEG2-NH-Boc 1g 2g 98%
AAU0231A 166388-57-4 Azido-PEG2-C2-amine 250mg 500mg 97%
AAU0232A 149299-82-1 Hydroxy-PEG2-CH2-Boc 1g 2g 97%
AAU0233A 1233234-77-9 Boc-NH-PEG11-NH2 100mg 200mg 97%
AAU0234A 208827-90-1 Propargyl-PEG3-alcohol 5g 10g 97%
AAU0235A 287174-32-7 Hydroxy-PEG1-CH2-Boc 1g 2g 97%
AAU0236A 756525-93-6 Mal-amido-PEG8-NHS ester 250mg 500mg 98%
AAU0237A 1008402-79-6 Bis-PEG9-NHS ester 25mg 50mg 98%
AAU0238A 756526-04-2 NH2-PEG9-acid 3g 6g 98%
AAU0239A 1191079-83-0 Amino-PEG9-acid 1g 2g 97%
AAU0240A 872679-70-4 Fmoc-NH-PEG2-CH2CH2COOH 10g 20g 98%
AAU0241A 882847-13-4 Boc-NH-PEG6-CH2CH2COOH 100mg 200mg 97%
AAU0242A 1334169-93-5 Boc-NH-PEG8-CH2CH2COOH 100mg 200mg 97%
AAU0243A 756525-91-4 Boc-NH-PEG4-CH2CH2COOH 100mg 200mg 97%
AAU0244A 1347750-78-0 Boc-NH-PEG5-CH2CH2COOH 100mg 200mg 97%
AAU0245A 1312309-64-0 N3-PEG2-C2-NHS ester 100mg 200mg 97%
AAU0246A 439114-13-3 Bis-PEG5-acid 1g 2g 97%
AAU0247A 875770-34-6 Biotin-PEG3-azide 1g 2g 97%
AAU0248A 31576-51-9 m-PEG2-Amine 1g 2g 98%
AAU0249A 1383814-00-3 Amino-PEG12-Boc 1g 2g 98%
AAU0250A 929-75-9 Amino-PEG3-C2-Amine 1g 2g 95%
AAU0251A 142929-49-5 Boc-NH-PEG1-CH2COOH 1g 2g 97%
AAU0252A 937188-59-5 Hydroxy-PEG4-acid 100mg 200mg 97%
AAU0253A 663171-32-2 Biotin-PEG4-amine 250mg 500mg 98%
AAU0254A 169751-72-8 Hydroxy-PEG4-CH2-Boc 1g 2g 97%
AAU0255A 2100306-71-4 Bromo-PEG3-CH2-Boc 1g 2g 98%
AAU0256A 459426-22-3 Biotin-PEG4-NHS ester 250mg 500mg 97%
AAU0257A 2055042-66-3 Hydroxy-PEG9-Boc 250mg 500mg 98%
AAU0258A 108466-89-3 Boc-NH-PEG2-CH2COOH 1g 2g 97%
AAU0259A 215181-61-6 m-PEG2-azide 5g 10g 97%
AAU0260A 86770-67-4 Azido-PEG4-alcohol 1g 2g 97%
AAU0261A 1895922-74-3 Boc-NH-PEG2-propargyl 250mg 500mg 97%
AAU0262A 87450-10-0 Propargyl-PEG4-alcohol 100mg 200mg 95%
AAU0263A 9004-74-4 m-PEG-OH (MW 2000) 25g 50g 97%
AAU0264A 57641-66-4 Bromo-PEG2-alcohol 5G 10G 97%
AAU0265A 54149-17-6 m-PEG2-Br 5g 10g 97%
AAU0266A 27425-92-9 m-PEG10-alcohol 1g 2g 97%
AAU0267A 2101563-45-3 Fmoc-NH-PEG10-acid 1g 2g 97%
AAU0268A 1257063-35-6 Azido-PEG4-C2-acid 250mg 500mg 97%
AAU0269A 462100-06-7 Boc-NH-PEG3-CH2COOH 1g 2g 97%
AAU0270A 869310-84-9 Propargyl-PEG2-NHBoc 250mg 500mg 97%
AAU0271A 858126-78-0 DNP-PEG4-NHS ester 500mg 1g 97%
AAU0272A 518044-31-0 Hydroxy-PEG3-CH2-Boc 1g 2g 97%
AAU0273A 297162-47-1 Hydroxy-PEG6-CH2-Boc 1g 2g 97%
AAU0274A 955094-26-5 Mal-amido-PEG2-NHS ester 250mg 500mg 97%
AAU0275A 1404111-67-6 N-Boc-PEG5-alcohol 1g 2g 97%
AAU0276A 186020-66-6 Hydroxy-PEG3-(CH2)2-Boc 10g 20g 97%
AAU0277A 791028-27-8 Amino-PEG2-C2-acid 20g 40g 97%
AAU0278A 165963-71-3 N-Boc-PEG3-bromide 1g 2g 97%
AAU0279A 1334177-79-5 Mal-amido-PEG6-acid 1g 2g 97%
AAU0280A 2241669-16-7 NH2-PEG5-C6-Cl (hydrochloride) 1g 2g 97%
AAU0281A 557756-85-1 Fmoc-NH-PEG4-CH2CH2COOH 5g 10g 98%
AAU0282A 474082-35-4 Amino-PEG9-amine 1g 2g 98%
AAU0283A 119189-70-7 Bis-PEG6-acid 250mg 500mg 97%
AAU0284A 2388521-20-6 Hydroxy-PEG12-Boc 250mg 500mg 98%
AAU0285A 361189-64-2 Hydroxy-PEG6-Boc 250mg 500mg 97%
AAU0286A 164332-88-1 N-Boc-PEG2-bromide 1g 2g 97%
AAU0287A 929-59-9 Bis-NH2-PEG2 25g 50g 95%
AAU0288A 1818294-42-6 Amino-PEG10-Boc 100mg 200mg 97%
AAU0289A 1334177-80-8 Cbz-NH-PEG6-C2-acid 250mg 500mg 97%
AAU0290A 957486-82-7 Azido-PEG6-amine 250mg 500mg 97%
AAU0291A 1334177-87-5 Cbz-NH-PEG8-C2-acid 100mg 200mg 95%
AAU0292A 361189-66-4 Azido-PEG6-acid 500mg 1g 98%
AAU0293A 1670249-37-2 Azido-PEG9-acid 500mg 1g 98%
AAU0294A 39160-70-8 Amino-PEG6-alcohol 250mg 500mg 97%
AAU0295A 2093153-98-9 Propargyl-PEG9-amine 100mg 200mg 97%
AAU0296A 882518-90-3 Azido-PEG2-CH2COOH 250mg 500mg 97%
AAU0297A 756526-00-8 Cbz-NH-PEG4-C2-acid 250mg 500mg 97%
AAU0298A 1245823-51-1 Propargyl-PEG5-acid 1g 2g 98%
AAU0299A 1425973-14-3 NH2-PEG7 500mg 1g 98%
AAU0300A 1347760-82-0 Propargyl-PEG3-acid 250mg 500mg 97%
AAU0301A 1951438-84-8 Propargyl-PEG6-acid 250mg 500mg 97%
AAU0302A 932741-19-0 Propargyl-PEG3-amine 1g 2g 97%
AAU0303A 34188-11-9 NH2-PEG5-OH 250mg 500mg 98%
AAU0304A 581065-94-3 Tos-PEG5-Boc 1g 2g 97%
AAU0305A 86770-68-5 Azido-PEG5-alcohol 250mg 500mg 97%
AAU0306A 880129-82-8 Azido-PEG6-CH2COOH 500mg 1g 98%
AAU0307A 1214319-92-2 Azido-PEG8-acid 100mg 200mg 98%
AAU0308A 217180-81-9 Azido-PEG5-CH2CO2H 250mg 500mg 98%
AAU0309A 857891-82-8 Azido-PEG8-amine 250mg 500mg 97%
AAU0310A 5961-83-1 Bis-PEG1-acid 250mg 500mg 98%
AAU0311A 19364-66-0 Bis-PEG2-acid 250mg 500mg 97%
AAU0312A 2411681-88-2 Thalidomide-O-PEG4-NHS ester 250mg 500mg 97%
AAU0313A 82209-36-7 Amino-PEG8-amine 100mg 200mg 98%
AAU0314A 1263045-16-4 Mal-amido-PEG4-acid 500mg 1g 97%
AAU0315A 756525-99-2 Mal-amido-PEG4-NHS ester 100mg 200mg 98%
AAU0316A 139338-72-0 Fmoc-amino-PEG3-CH2COOH 2g 4g 97%
AAU0317A 252881-76-8 Biotin-PEG3-acid 1g 2g 95%
AAU0318A 1381861-91-1 Bromo-PEG2-C2-Boc 1g 2g 97%
AAU0319A 1292268-13-3 N-Boc-PEG7-alcohol 5g 10g 97%
AAU0320A 1334286-77-9 Hydroxy-PEG2-acid 250mg 500mg 97%
AAU0321A 1036204-60-0 Propargyl-PEG5-OH 250mg 500mg 95%
AAU0322A 2250216-93-2 Boc-NH-PEG3-NHS ester 1g 2g 97%
AAU0323A 1314378-14-7 Fmoc-PEG4-NHS ester 1g 2g 98%
AAU0324A 1431618-70-0 Biotin-PEG3-Mal 100mg 200mg 97%
AAU0325A 912849-73-1 Azido-PEG10-amine 1g 2g 97%
AAU0326A 157759-50-7 Bromo-PEG1-CH2-Boc 1g 2g 97%
AAU0327A 134179-38-7 Amino-PEG3-C2-Azido 100mg 200mg 97%
AAU0328A 778596-26-2 Hydroxy-PEG10-Boc 1g 2g 97%
AAU0329A 57641-67-5 Br-PEG3-OH 250mg 500mg 98%
AAU0330A 189808-70-6 NH2-PEG3-C1-Boc 1g 2g 98%
AAU0331A 7218-43-1 Propargyl-PEG2-OH 250mg 500mg 95%
AAU0332A 1056024-94-2 N3-PEG3-CH2CH2COOH 5g 10g 98%
AAU0333A 359860-27-8 Amine-PEG3-Biotin 100mg 200mg 97%
AAU0334A 1537892-36-6 Mal-PEG3-NHS ester 500mg 1g 98%
AAU0335A 1260092-44-1 Boc-NH-PEG1-CH2CH2COOH 5g 10g 97%
AAU0336A 85141-94-2 Br-PEG4-OH 1g 2g 97%
AAU0337A 352439-37-3 NH2-PEG8-OH 1g 2g 97%
AAU0338A 141282-35-1 Amino-PEG5-CH2COOH 0.1g 0.2g 98%
AAU0339A 635287-26-2 Fmoc-NH-PEG5-CH2COOH 0.25g 0.5g 97%
AAU0340A 867062-95-1 Fmoc-NH-PEG3-CH2CH2COOH 100mg 200mg 98%
AAU0341A 1052207-59-6 Boc-NH-PEG8-CH2CH2NH2 1g 2g 98%
AAU0342A 31255-26-2 Bromo-PEG3-bromide 1g 2g 98%
AAU0343A 24345-74-2 Azido-PEG1-azide 100mg 200mg 98%
AAU0344A 1325208-25-0 Mal-PEG4-NHS ester 250mg 500mg 97%
AAU0345A 516493-93-9 Azido-PEG5-amine 1g 2g 97%
AAU0346A 1374666-32-6 Mal-PEG2-acid 100mg 200mg 97%
AAU0347A 1013921-36-2 Propargyl-PEG4-amine 250mg 500mg 97%
AAU0348A 1347750-75-7 Boc-N-amido-PEG3-acid 1g 2g 97%
AAU0349A 72236-26-1 Amino-PEG5-amine 0.25g 0.5g 97%
AAU0350A 332941-25-0 Amino-PEG7-amine 0.25g 0.5g 98%
AAU0351A 1517-05-1 Azido-PEG1 5g 10g 97%
AAU0352A 945633-30-7 Biotin-PEG2-CH2CH2N3 50mg 100mg 97%
AAU0353A 65869-63-8 Bis-PEG2-NHS ester 100mg 200mg 97%
AAU0354A 206265-98-7 Boc-NH-PEG7-NH2 100mg 200mg 97%
AAU0355A 721431-18-1 Biotin-PEG4-acid 50mg 100mg 97%
AAU0356A 1027371-75-0 m-PEG1-NHS ester 1g 2g 97%
AAU0357A 110429-45-3 m-PEG4-Br 5g 10g 97%
AAU0358A 782475-37-0 Br-PEG3-C2-Boc 1g 2g 97%
AAU0359A 784105-33-5 Amino-PEG3-C2-acid 1g 2g 97%
AAU0360A 530151-56-5 Bromo-PEG2-C2-azide 1g 2g 97%
AAU0361A 905954-28-1 NH2-PEG6-CH2CH2COOH 1g 2g 97%
AAU0362A 195071-49-9 Amino-PEG4-CH2COOH 2g 4g 97%
AAU0363A 2365309-92-6 Cl-PEG6-acid 100mg 200mg 98%
AAU0364A 1137109-21-7 Mal-amido-PEG6-NHS ester 100g 200g 97%
AAU0365A 936917-36-1 Iodo-PEG4-N3 500mg 1g 97%
AAU0366A 85030-56-4 m-PEG4-Amine 250mg 500mg 97%
AAU0367A 869718-81-0 m-PEG8-Amine 1g 2g 97%
AAU0368A 1702356-19-1 ENdo-BCN-PEG4-NHS ester 25mg 50mg 97%
AAU0369A 1058691-77-2 m-PEG6-CH2CH2CHO 100mg 200mg 97%


Seebio supplies G-Kg grade protein drug intermediates

Protein Drug Intermediates Seebio Code CAS No. Name Packsize
growth hormone side chain AAU0178A N/A TZ-Ste-SO2-nBu-AEEA-Glu(OH)-Glu(OH)-AEEA-Lys(OH)-C 1g, 5g; 1kg
AAU0179A N/A HO-Ste-CYH-Glu(OH)-Glu(OH)-AEEEEA-Mal 1g, 5g; 1kg
Tirzepatide Side Chain AAU0180A 1188328-37-1 OtBu-Ara-Glu(AEEA-AEEA-OH)-OtBu 1g, 5g; 1kg
Semaglutide Side Chain AAU0181A 1169630-40-3 (S)-22-(carboxy)-1-((2,5-dioxocyclopentyl)oxy)-1,10,19,24-tetraoxo-3,6,12,15-tetraxa Oxa-9,18,23-azatetradecane-41-acid 1g, 5g; 1kg
AAU0182A 1118767-16-0 tBuO-Ste-Glu(AEEA-AEEA-OH)-OtBu 1g, 5g; 1kg
AAU0183A 1118767-15-9 tBuO-Ste-Glu(AEEA-AEEA-OSu)-OtBu 1g, 5g; 1kg
AAU0184A N/A tBuO-Ste-Glu(AEEA-AEEA-ONa)-OtBu 1g, 5g; 1kg
AAU0185A 4871-70-5 Octadecanedioic acid 1g, 5g; 1kg
AAU0186A 843666-40-0 Octadecanedioic acid Mono-tert-butyl ester 1g, 5g; 1kg
AAU0187A 134978-97-5 AEEA 1g, 5g; 1kg
AAU0188A 1143516-05-5 AEEA-AEEA 1g, 5g; 1kg
AAU0189A 166108-71-0 Fmoc-AEEA 1g, 5g; 1kg
AAU0190A N/A Fmoc-PEG3-acetic acid 1g, 5g; 1kg
AAU0191A 2061897-68-3 Boc-His(Trt)-Aib-OH 1g, 5g; 1kg
AAU0192A N/A Boc-His(Trt)-Aib-Glu(OtBu)-Gly-OH 1g, 5g; 1kg
AAU0193A 1662688-20-1 Fmoc-Lys(tBuO-Ste-Glu(AEEA-AEEA)-OtBu)-OH 1g, 5g; 1kg
AAU0194A N/A tBuO-Ste-Glu(AEEA-AEEA-Glu)-OtBu 1g, 5g; 1kg
Liraglutide Side Chain AAU0195A 204521-63-1 Pal-Glu(OSu)-OtBu 1g, 5g; 1kg
AAU0196A 57078-98-5 D-Pal-Glu(OSu)-OtBu 1g, 5g; 1kg
AAU0197A N/A L-HO-Pal-Lys(OSu)-OH 1g, 5g; 1kg
AAU0198A 294855-91-7 L-Pal-Glu(OSu)-OH 1g, 5g; 1kg
AAU0199A N/A L-Pal-Glu(OH)-OtBu 1g, 5g; 1kg
AAU0200A N/A 2L-HO-Pal-Glu(OSu)-OtBu 1g, 5g; 1kg
Insulin degludec Side Chain AAU0201A N/A L-HO-Pal-Glu(OSu)-OH 1g, 5g; 1kg
AAU0202A N/A L-tBuO-Pal-Glu(OSu)-OtBu 1g, 5g; 1kg
AAU0203A N/A L-tBuO-Pal-Glu(OSu)-OH 1g, 5g; 1kg
Insulin detemir Side Chain AAU0204A 69888-86-4 N-succinimidyl myristic acid 1g, 5g; 1kg
 
 
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