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PROTAC Linkers

PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules composed of two ligands; an “anchor” that binds to an E3 ubiquitin ligase and a “warhead” that binds to a protein of interest, connected by a chemical linker.

Figure 1: Schematic of typical PROTAC structure and an example (ARV-110).
Figure 1: Schematic of typical PROTAC structure and an example (ARV-110).

PROTAC linker plays a vital role in efficient ubiquitination of the target protein and its ultimate degradation. To date, several kinds of linkers have been reported and applied in PROTAC ternary complexes formation, such as PEG linker, Alkyl linker, alkyne linkers, and click chemistry linker, etc. 

PEG linkers are the most common motifs incorporated into PROTAC linker structures. According to statistics, 54% of the reported PROTAC molecules used PEG as a linker.
▶ The introduction of PEG can increase the water solubility of PROTAC molecules and affect cell permeability, thus affecting oral absorption.
▶ Systematic changes in linker length can be easily achieved by using PEGs of different chain lengths, affecting the degradation efficiency of PROTAC molecules.
​▶ The use of various bifunctionalized PEG linkers enables the simple and rapid assembly of molecules with different linker groups and accelerates the screening of efficient degradation structures.

Biopharma PEG is dedicated to the R&D of PROTAC Linker, providing high purity PEG linkers with various reactive groups to continuously assist your project development.

References:
[1] Sun X, Gao H, Yang Y, et al. PROTACs: great opportunities for academia and industry.Signal Transduct Target Ther. 2019;4:64.
​[2]Troup RI, Fallan C, Baud MGJ. Current strategies for the design of PROTAC linkers: a critical review. Explor Target Antitumor Ther. 2020;1:273-312. https://doi.org/10.37349/etat.2020.00018

Catalog No. Name Structure M.W. Purity
NE12458 NH2-Ph-C4-acid-NH2-Me NH2-Ph-C4-acid-NH2-Me 222.28 ≥95%
NE12454 Boc-NH-C6-amido-C4-acid Boc-NH-C6-amido-C4-acid 344.45 ≥95%
MD005002 NH2-PEG3-OH NH2-PEG3-OH 149.18 ≥95%
MD005005 NH2-PEG2-NH2 NH2-PEG2-NH2 148.2 ≥95%
MD005121 NH2-PEG2-CH2COOH NH2-PEG2-CH2COOH 163.2 ≥95%
MD005128 NH2-PEG3-CH2COOtBu NH2-PEG3-CH2COOtBu 263.33 ≥95%
MD005286 Thalidomide-O-amido-PEG3-NH2 Thalidomide-O-amido-PEG3-NH2 506.509 ≥95%
MD006005 N3-PEG4-NH2 N3-PEG4-NH2 262.31 ≥95%
MD006121 N3-PEG3-CH2COOH N3-PEG3-CH2COOH 233.22 ≥95%
MD006121 N3-PEG4-CH2COOH N3-PEG4-CH2COOH 277.27 ≥95%
MD016016 COOH-PEG3-COOH COOH-PEG3-COOH 294.298 ≥95%
MD038038 Tos-PEG4-Tos Tos-PEG4-Tos 502.6 ≥95%