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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
MD329025 Thalidomide-O-PEG4-SPA Thalidomide-O-PEG4-SPA 619.57 ≥95%
MD329007 Thalidomide-O-PEG2-Propargyl Thalidomide-O-PEG2-Propargyl 400.38 ≥95%
MD329007 Thalidomide-O-PEG4-Propargyl Thalidomide-O-PEG4-Propargyl 488.49 ≥95%
MD329005 Thalidomide-O-PEG4-NH2 Thalidomide-O-PEG4-NH2 493.51 ≥95%
MD329006 Thalidomide-O-PEG4-N3 Thalidomide-O-PEG4-N3 519.51 ≥95%
MD329067 Thalidomide-O-PEG4-t-butyl ester Thalidomide-O-PEG4-t-butyl ester 578.61 ≥95%
MD329038 Thalidomide-O-PEG5-Tosyl Thalidomide-O-PEG5-Tosyl 648.68 ≥95%
MD038005 Tos-PEG2-NH2 Tos-PEG2-NH2 259.32 ≥95%
MD068038 Boc-NH-PEG2-Tos Boc-NH-PEG2-Tos 403.49 ≥95%
MD038330 Tos-PEG3-O-C1-CH3COO Tos-PEG3-O-C1-CH3COO 376.42 ≥95%
MD068006 Boc-NH-PEG11-N3 Boc-NH-PEG11-N3 670.79 ≥89%