PEG Linkers
PEG linkers provide covalent spacing and hydrophilicity in drug conjugates, rather than receptor-level agonism or inhibition[1]. Mechanistically, PEGylation links one or more polyethylene glycol chains to protein, peptide, or non-peptide molecules and improves delivery-relevant physicochemical behavior[1]. Releasable PEGylation uses customized linkers that reversibly tether therapeutic moieties to polyethylene glycol polymers, enabling regeneration of authentic and fully active drug[2]. In antibody-drug conjugates, hydrophilic PEG-containing linkers mask or reduce payload hydrophobicity and improve physical stability and in vivo performance[3]. Disease-model studies in cancer ADC research show that hydrophilic linker design supports antibody-maytansinoid conjugates and PEGylated glucuronide-MMAE conjugates[4][5]. Compared with alkyl linkers in PROTACs, ethylene glycol linkers can reduce cell permeability, showing that linker polarity and folding must be optimized for intracellular degrader design[6]. Compared with other hydrophilic linker classes, PEG linkers act as monodisperse hydrophilicity reservoirs for highly loaded lysine-conjugated ADCs[3]. For experimental applications, PEG linker selection should prioritize spacer length, cleavable release chemistry, hydrophilicity, aggregation control, and payload exposure in ADC, PEGylation, and PROTAC projects[2][3][6][7].
Verweise:
- [1]. Veronese FM, et al. PEGylation, successful approach to drug delivery. Drug Discov Today. 2005 Nov 1;10(21):1451-8. [Content Brief]
- [2]. Filpula D, et al. Releasable PEGylation of proteins with customized linkers. Adv Drug Deliv Rev. 2008 Jan 3;60(1):29-49. [Content Brief]
- [3]. Tedeschini T, et al. Polyethylene glycol-based linkers as hydrophilicity reservoir for antibody-drug conjugates. J Control Release. 2021 Sep 10;337:431-447. [Content Brief]
- [4]. Zhao RY, et al. Synthesis and evaluation of hydrophilic linkers for antibody-maytansinoid conjugates. J Med Chem. 2011 May 26;54(10):3606-23. [Content Brief]
- [5]. Burke PJ, et al. Optimization of a PEGylated Glucuronide-Monomethylauristatin E Linker for Antibody-Drug Conjugates. Mol Cancer Ther. 2017 Jan;16(1):116-123. [Content Brief]
- [6]. Poongavanam V, et al. Linker-Dependent Folding Rationalizes PROTAC Cell Permeability. J Med Chem. 2022 Oct 13;65(19):13029-13040. [Content Brief]
- [7]. Su Z, et al. Antibody-drug conjugates: Recent advances in linker chemistry. Acta Pharm Sin B. 2021 Dec;11(12):3889-3907. [Content Brief]
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PEG Linkers Verwandte Produkte (2357)
Verwandte Produkte (2357)
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Biotin-PEG3-azide
0 ImagesArt. -Nr.: HY-130143CAS. Nr.: 875770-34-6Biotin-PEG3-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Biotin-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Azido-PEG2-C2-amine
0 ImagesArt. -Nr.: HY-140213CAS. Nr.: 166388-57-4Synonyms: N3-PEG2-CH2CH2NH2Azido-PEG2-C2-amine (N3-PEG2-CH2CH2NH2) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG2-C2-amine is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG2-C2-amine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Biotin-PEG4-azide
0 ImagesBiotin-PEG4-azide is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin-PEG4-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Azido-PEG4-NHS-ester
0 ImagesAzido-PEG4-NHS-ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG4-NHS-ester is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Azido-PEG1
0 ImagesAzido-PEG1 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG1 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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N3-PEG4-C2-NH2
0 ImagesSynonyms: PROTAC Linker 20N3-PEG4-C2-NH2 (PROTAC Linker 20) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. N3-PEG4-C2-NH2 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Fmoc-NH-PEG4-CH2CH2COOH
0 ImagesSynonyms: Fmoc-15-amino-4,7,10,13-tetraoxapentadecanoic acidFmoc-NH-PEG4-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-NH-PEG4-CH2CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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Azido-PEG2-C2-acid
0 ImagesAzido-PEG2-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG2-C2-acid is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Azido-PEG5-amine
0 ImagesAzido-PEG5-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG5-amine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Fmoc-8-amino-3,6-dioxaoctanoic acid
0 ImagesSynonyms: Fmoc-NH-PEG2-CH2COOHFmoc-8-amino-3,6-dioxaoctanoic acid (Fmoc-NH-PEG2-CH2COOH) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-8-amino-3,6-dioxaoctanoic acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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Azido-PEG4-alcohol
0 ImagesAzido-PEG4-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Azido-PEG4-alcohol is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
