Join Us at TIDES Europe 2025 in Congress Center Basel! Mark your calendars!TIDES Europe2025—the premier event for oligonucleotide and peptide therapeutics—is coming to Basel, Switzerland, on 11-13 November 2025. Visit SINOPEG at Booth #333 to explore cutting-edge solutions in: Custom PEG Derivatives (mPEG, heterobifunctional PEGs, branched PEGs) Lipid Nanoparticles (LNPs) & Lipidoids for nucleic acid delivery Innovative Linker Technologies & ADC Payloads Why Stop By? Discuss your formulation challenges with our PEGylation experts Discover high-purity excipients for mRNA, siRNA, and peptide therapies Learn how our GMP-grade materials accelerate preclinical-to-commercial transitions Spotlight Case Study: Ask us about our role in developing temperature-stable LNP formulations for a global COVID-19 vaccine partner! Schedule a 1:1 Meeting: Avoid the crowds—reserve your private session today: sales@sinopeg.com Can't attend? Explore our solutions online: http://www.sinopeg.com Let's shape the future of oligonucleotide and peptide therapeutics together! See you at #333. #TIDES2025 DrugDiscovery #LNPs #mRNA #PeptideTherapeutics #BiotechInnovation

Molecules. 2017 Jul 15;22(7):1190. doi: 10.3390/molecules22071190. Antiviral Lipopeptide-Cell Membrane Interaction Is Influenced by PEG Linker Length Abstract A set of lipopeptides was recently reported for their broad-spectrum antiviral activity against viruses belonging to the Paramyxoviridae family, including human parainfluenza virus type 3 and Nipah virus. Among them, the peptide with a 24-unit PEG linker connecting it to a cholesterol moiety (VG-PEG24-Chol) was found to be the best membrane fusion inhibitory peptide. Here, we evaluated the interaction of the same set of peptides with biomembrane model systems and isolated human peripheral blood mononuclear cells (PBMC). VG-PEG24-Chol showed the highest insertion rate and it was among the peptides that induced a larger change on the surface pressure of cholesterol rich membranes. This peptide also displayed a high affinity towards PBMC membranes. These data provide new information about the dynamics of peptide-membrane interactions of a specific group of antiviral peptides, known for their potential as multipotent paramyxovirus antivirals. Keywords: antiviral; cholesterol; membranes; paramyxoviruses; peptides. PEG Linker: Various Kingds And Grades Of Such Monodispersed Are Readily Avaliable| SINOPEG

Join Us at 2025 CPHI Worldwide Europe! SINOPEG's booth no. 8.0T48 Exciting news! 2025 CPHI Worldwide Europe is just around the corner, taking place October 28–30 at Messe Frankfurt. SINOPEG will be showcasing cutting-edge drug delivery system (DDS) solutions at Booth 8.0T48.    As your trusted partner in specialty chemicals and advanced drug delivery systems, we’re eager to share innovations that drive industry progress. Why visit us? Explore our latest portfolio of PEG derivatives, lipids, and custom synthesis services Discuss tailored solutions for your R&D and manufacturing challenges Connect face-to-face with our technical experts We warmly welcome friends, partners, and industry peers from around the globe to drop by!    Let’s collaborate to shape the future of pharma. Dates: October 28–30, 2025 Venue: Messe Frankfurt Our Booth: T48 (Hall 8.0) Ready to meet? Simply stop by!

J Pharm Sci. 2020 Feb;109(2):981-991.  doi: 10.1016/j.xphs.2019.10.052.  Epub 2019 Nov 2. Conjugation of Amine-Functionalized Polyesters With Dimethylcasein Using Microbial Transglutaminase Abstract Protein-polymer conjugates have been used as therapeutics because they exhibit frequently higher stability, prolonged in vivo half-life, and lower immunogenicity compared with native proteins.  The first part of this report describes the enzymatic synthesis of poly(glycerol adipate) (PGA(M)) by transesterification between glycerol and dimethyl adipate using lipase B from Candida antarctica.  PGA(M) is a hydrophilic, biodegradable but water insoluble polyester.  By acylation, PGA(M) is modified with 6-(Fmoc-amino)hexanoic acid and with hydrophilic poly(ethylene glycol) side chains (mPEG12) rendering the polymer highly water soluble.  This is followed by the removal of protecting groups, fluorenylmethyloxycarbonyl, to generate polyester with primary amine groups, namely PGA(M)-g-NH2-g-mPEG12.  1H NMR spectroscopy, FTIR spectroscopy, and gel permeation chromatography have been used to determine the chemical structure and polydispersity index of PGA(M) before and after modification.  In the second part, we discuss the microbial transglutaminase-mediated conjugation of the model protein dimethylcasein with PGA(M)-g-NH2-g-mPEG12 under mild reaction conditions.  SDS-PAGE proves the protein-polyester conjugation. Keywords: CAL-B;  amine-functionalized polyester;  enzymatic polymerization;  microbial transglutaminase (mTGase);  poly(glycerol adipate) (M);  protein-polymer conjugate.

Bioconjug Chem. 2025 Feb 19;36(2):179-189.  doi: 10.1021/acs.bioconjchem.4c00392.  Epub 2025 Jan 20. PEGylation of Dipeptide Linker Improves Therapeutic Index and Pharmacokinetics of Antibody-Drug Conjugates Abstract Hydrophobic payloads incorporated into antibody-drug conjugates (ADCs) typically are superior to hydrophilic ones in tumor penetration and "bystander killing" upon release from ADCs.  However, they are prone to aggregation and accelerated plasma clearance, which lead to reduced efficacies and increased toxicities of ADC molecules.  Shielding the hydrophobicity of payloads by incorporating polyethylene glycol (PEG) elements or sugar groups into the ADC linkers has emerged as a viable alternative to directly adopting hydrophilic payloads.  In this study, ADC linkers incorporating PEG or sugar groups were synthesized by modifying dipeptide linkers, with hydrophobic monomethyl auristatin E (MMAE) serving as an exemplary hydrophobic payload.  All drug-linkers (DLs) were conjugated to RS7, a humanized antibody targeting Trop-2, with drug-to-antibody ratio (DAR) values set at 4 or 8.  Among these, the ADC molecule RS7-DL 11, featuring a methyl-PEG24 (mPEG24) moiety as a side chain to the Valine-Lysine-PAB (VK) linker, demonstrated maximum hydrophilicity, biophysical stability, and tumor suppression, along with prolonged half-life and enhanced animal tolerability.  In conclusion, through PEGylation of the traditional dipeptide linker, we have demonstrated an optimized ADC conjugation technology that can be employed for conjugating ultrahydrophobic payloads, thus enhancing both the therapeutic index and pharmacokinetics profile.

Langmuir. 2014 Jul 1;30(25):7465-74. doi: 10.1021/la500403v. Epub 2014 Jun 17. Effect of polyethylene glycol, alkyl, and oligonucleotide spacers on the binding, secondary structure, and self-assembly of fractalkine binding FKN-S2 aptamer-amphiphiles Abstract Previously we identified an aptamer, named FKN-S2, which binds the cell surface protein fractalkine with high affinity and specificity. In this paper a hydrophobic dialkyl C16 tail was added to the aptamer to create an aptamer-amphiphile. We investigated how the tail and a spacer molecule of varying length and hydrophobicity, inserted between the tail and the aptamer headgroup, affect the binding, structure, and self-assembly properties of the aptamer-amphiphile. We synthesized aptamer-amphiphiles with no spacer (NoSPR), polyethylene glycol (PEG4, PEG8, PEG24), alkyl (C12 and C24), or oligonucleotide (T10 and T5: 10 and 5 thymine, and A10: 10 adenine) spacers. The addition of the tail reduced the binding affinity of the aptamer-amphiphile over 7.5-fold compared to the free aptamer. The hydrophobic alkyl spacers resulted in the greatest loss of affinity, and the hydrophilic PEG spacers improved amphiphile affinity but did not restore it to that of the free aptamer. Interestingly, oligonucleotide spacers produced the highest affinity amphiphiles. Nucleotide composition did not affect affinity, however, as the T10 and A10 spacers had equal affinity. The oligonucleotide spacer amphiphiles had the highest affinity because the oligonucleotide spacer increased the affinity of free aptamer; the FKN-S2 aptamer plus the oligonucleotide spacer had a higher affinity than the free FKN-S2 aptamer. Circular dichroism (CD) spectroscopy and thermal melting studies indicated the aptamer forms a stem-loop and intramolecular G-quadruplex, and the tail strongly stabilized the formation of the G-quadruplex in a buffer. Cryogenic transmission electron microscopy (cryo-TEM) imaging showed the aptamer-amphiphiles, independent of the spacer used, self-assembled into micelles and nanotapes, flat bilayer structures that were often twisted. Finally, liposomes functionalized with the FKN-S2 amphiphile were incubated with fractalkine expressing cells, and the amount of binding was dependent on the concentration of the amphiphile on the liposome surface.

Biosens Bioelectron. 2019 Sep 15:141:111477. doi: 10.1016/j.bios.2019.111477. Epub 2019 Jun 25. Novel thiolated-PEG linker molecule for biosensor development on gold surfaces Abstract The surface modifying linker molecules can directly influence the performance and longevity of biosensors. They must allow the attachment of biological recognition layer on the sensor surface, as well as the protection of the surface from fouling effects. Recent advances in this field identified several key factors that can increase the efficiency, stability and the anti-fouling effect of a layer formed by surface modifying linker molecules. Herein, this work presents a simple synthetic procedure, characterization, and application of a novel thiolated-PEG surface modifying molecule (DSPEG2) that could act as a multi-purpose linker for gold surfaces. The analyses of the molecular spatial distribution of DSPEG2 on gold surfaces were performed using time-of-flight secondary ion mass spectrometry (TOF-SIMS) imaging and X-ray photoelectric spectroscopy (XPS). The immobilization of DSPEG2 on gold surfaces was examined using cyclic voltammetry (CV), electrochemical impedance spectroscopy (EIS) and surface plasmon resonance (SPR). Our preliminary results demonstrated that DSPEG2 is a promising novel linker molecule that can be applied in a wide range of biosensors based on gold surfaces. Keywords: Anti-fouling; Biosensor; Cyclic voltammetry; Electrochemical impedance spectroscopy; Non-specific adsorption; PEG; Surface plasmon resonance; Synthetic linker.

Br J Haematol. 2020 May;189(3):442-451. doi: 10.1111/bjh.16254. Epub 2019 Dec 27. Acute lymphoblastic leukaemia patients treated with PEGasparaginase develop antibodies to PEG and the succinate linker Abstract Polyethylene glycol (PEG) conjugated asparaginase (PEGasparaginase) is essential for treatment of paediatric acute lymphoblastic leukaemia. We developed an assay identifying antibodies against the PEG-moiety, the linker and the drug itself in patients experiencing hypersensitivity reactions to PEGasparaginase. Eighteen patients treated according to the DCOG ALL-11 protocol, with a neutralizing hypersensitivity reaction to PEGasparaginase to the first PEGasparaginase doses in induction (12 patients) or during intensification after interruption of several months (6 patients) were included. ELISA was used to measure antibodies, coating with the succinimidyl succinate linker conjugated to BSA, PEGfilgrastim and Escherichia coli asparaginase, and using hydrolysed PEGasparaginase and mPEG5,000 for competition. Anti-PEG antibodies were detected in all patients (IgG 100%; IgM 67%) of whom 39% had anti-PEG antibodies exclusively. Pre-existing anti-PEG antibodies were also detected in patients who not previously received a PEGylated therapeutic (58% IgG; 21% IgM). Antibodies against the SS-linker were predominantly detected during induction (50% IgG; 42% IgM). Anti-asparaginase antibodies were detected in only 11% during induction but 94% during intensification. In conclusion, anti-PEG and anti-SS-linker antibodies predominantly play a role in the immunogenic response to PEGasparaginase during induction. Thus, switching to native E. coli asparaginase would be an option for adequate asparaginase treatment. Keywords: PEGasparaginase; acute lymphoblastic leukemia; antibodies.