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[BroadPharm] Two classes of PEG Linkers & Applications From BroadPharm

관리자 2021.09.30 10:50 조회 1105 추천 35
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PEG Linkers & Applications Highlight

 

 

Figure 1. Azido-PEG12-NHS ester is a bifunctional, monodisperse PEG linker.

 

 

In the last two decades, PEG linkers have become widely used in pharmacological and biotechnological R&D such as antibody drug conjugates (ADC), Drug discovery & drug delivery because of their water solubility, lack of toxicity, low immunogenicity. A few Applications are highlighted as below:

PEG Linker in Antibody Drug Conjugate (ADC)

ADC drug, Zynlonta incorporated several interesting linker components (Figure 2). The linker includes the maleimide - PEG8, and  enzymatically cleavable dipeptide (Val-Ala), to connect the antibody with the payload.

 

Figure 2. Zynlonta has several unique features including a maleimide group for attachment to the mAbs, a PEG8 liner for solubility, and a cleavable Val-Ala section bound to the drug SG3199.

 

PEG Lipid in Nanoparticle Drug Delivery

Stable nucleic acid lipid particles (SNALPs) were first developed in 2001. They have now become famous with the development of Moderna and Pfizer COVID-19 vaccines (Figure 3). Typically, SNALPS are composed of a high transition temperature phospholipid, a PEG lipid, and an ionizable phospholipid. One specific example is DSPE-mPEG 2000, which is essential to producing the Pfizer COVID-19 vaccine. Another well-known PEGylated lipid is DMG-PEG 2000, is used in the Moderna COVID-19 vaccine.

 

Figure 3.  PEG Lipids used in COVID-19 vaccines, Pfizer’s DSPE-PEG 2000 shown on top and Moderna’s DMG-PEG 2000 shown on bottom.

 

PEG in Small Molecule Drug Development

Introduction of PEG linkers to small molecule drugs increases the drug's solubility and molecular weight. This may allow for an extended drug half-life in the body. Naloxegol (Movantik) is one example of a small molecule drug that incorporates PEG to improve the drug’s efficiency by reducing its transport across the blood-brain barrier (Figure 4).

 

Figure 4. Movantik, shown above, is a pegylated derivative of α-naloxol.

 

As a worldwide leader of PEG linkers & Bioconjugation reagent, BroadPharm offers a wide array of PEG Linkers to empower our customer’s advanced research. These compounds feature great aqueous solubility, smart choice of PEG length, and a broad selection of functional groups to choose from. Please email to sales@broadpharm.com, or call, +1-858-677-6760, with any questions you may have.

 




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