Tag: dPEG®ylation

Graph showing the relationship of dPEG® linker length in relation to potency and specificity in extracellular drug conjugates.

Extracellular Drug Conjugates Therapeutically Exploit Protein Proximity

Pharmaceutical company Centrose, founded by James R. Prudent, Ph.D., developed a new class of antibody drug conjugates called extracellular drug conjugates. Nature Publishing Group published the research as a open access paper in its Molecular Therapy journal.1 Apart from the interesting and important development of a new class of antibody drug conjugate (ADC), the research also showed how important linker length 2 is to the potency and specificity of the EDC. Continue reading

Amphotericin B conjugated to a discrete PEG (dPEG®) linker with a free amine have higher water solubility and lower toxicity than the parent compound.

Amphotericin B+dPEG®: Water-Soluble, Less Toxic, Potent

Amphotericin B conjugated to a discrete PEG (dPEG®) linker with a free amine have higher water solubility and lower toxicity than the parent compound.
Amphotericin B conjugated to a discrete PEG (dPEG®) linker with a free amine has  higher water solubility and lower toxicity than the parent compound. Image used by permission from J. Med. Chem. (2016), 59, 1197-1206, copyright 2016, American Chemical Society.

About Amphotericin B

Structure of Amphotericin B. Used with permission from J. Med. Chem. (2016), 59, 1197-1206, copyright 2016, American Chemical Society.
Figure 1: Structure of Amphotericin B. Image used by permission from J. Med. Chem. (2016), 59, 1197-1206, copyright 2016, American Chemical Society.

Amphotericin B (Figure 1) is the “gold standard” treatment for systemic fungal infections and diseases caused by the parasite Leishmania. Sometimes it is the only effective treatment because drug resistance renders other treatments useless. Systemic fungal infections are an increasingly serious, widespread problem in medicine. Patients with weakened or suppressed immune systems (caused by HIV/AIDS, diabetes, organ transplants, some cancer treatments) are especially at risk. An estimated 1.5-2 million people die each year from systemic fungal infections (1). Despite its “gold standard” label, there are several difficulties with Amphotericin B. Continue reading

Chart showing the analgesic activities of various galanin analogues used in a formalin pain assay.

PEGylated Galanin Shows Enhanced Analgesic Effects in PNS

Galanin is a naturally occurring neuropeptide in the human body that facilitates communication between cells to balance a myriad of physiological functions. Neuropeptides are biosynthesized molecules used by the human body for everything from neurogenesis to cell communication.  Galanin’s main receptor sites reside in the central nervous system (CNS), and it normally crosses the blood brain barrier; however, the peripheral nervous system (PNS) also reacts directly to galanin and its receptors in sites of pain mediation.1  Continue reading

dPEG®-Modified Diabodies Improve Tumor Imaging

Researchers in Australia and the United States have shown that dPEG®-modified diabodies improve positron emission tomography (PET) imaging of tumors by reducing kidney uptake of diabody and extending diabody half-life in the bloodstream, which thus allows more diabody to be taken up by the tumor.1 These findings suggest that better tumor imaging can be achieved using less material, because more of the diabody that targets the tumor gets to the tumor and less of it is excreted by the kidney. Continue reading

A dPEG®ylated Avibody provides an example of the discrete nature of Quanta BioDesign's dPEG® reagents..

Noise control and removal through dPEG®ylation

Noise control and removal is important in any discipline where clean, clear signals are critical in measurement and data collection. For this reason, whilst the saying ‘Beauty is in the eyes of the beholder’ may be true in many instances, scientific research cannot permit subjective, qualitative thinking to trump objective data. Continue reading