ArticleScientific reports2015
Variant fatty acid-like molecules Conjugation, novel approaches for extending the stability of therapeutic peptides.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 44 citations in OpenAlex.
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- Understanding peptide hormones: from precursor proteins to bioactive molecules.Trends in biochemical sciences · 2025Review
- Lipopeptide-mediated Cas9 RNP delivery: A promising broad therapeutic strategy for safely removing deep-intronic variants inMolecular therapy. Nucleic acids · 2024Article
- Comparison of Protocols to Test Peptide Stability in Blood Plasma and Cell Culture Supernatants.ACS pharmacology & translational science · 2024Article
- Diversity of Antimicrobial Peptides in Silkworm.Life (Basel, Switzerland) · 2023Review
- A Factor XIa Inhibitor Engineered from Banded Krait Venom Toxin: Efficacy and Safety in Rodent Models of Arterial and Venous Thrombosis.Biomedicines · 2022Article
- Designing a Dual GLP-1R/GIPR Agonist from Tirzepatide: Comparing Residues Between Tirzepatide, GLP-1, and GIP.Drug design, development and therapy · 2022Review
- The Therapeutic Effect and In Vivo Assessment of Palmitoyl-GDPH on the Wound Healing Process.Pharmaceutics · 2021Article
- Impact of non-proteinogenic amino acids in the discovery and development of peptide therapeutics.Amino acids · 2020Review
- Structure-tuned membrane active Ir-complexed oligoarginine overcomes cancer cell drug resistance and triggers immune responses in mice.Chemical science · 2020Article
- Effects of 2 Novel PYY(1-36) Analogues, (PClinical medicine insights. Endocrinology and diabetes · 2019Article
- Glycation of human serum albumin impairs binding to the glucagon-like peptide-1 analogue liraglutide.The Journal of biological chemistry · 2018Article
- Factors affecting the physical stability (aggregation) of peptide therapeutics.Interface focus · 2017Review
- Controlling the bioactivity of a peptide hormone in vivo by reversible self-assembly.Nature communications · 2017Article
- The polysialic acid mimetics idarubicin and irinotecan stimulate neuronal survival and neurite outgrowth and signal via protein kinase C.Journal of neurochemistry · 2017Article
- Tumor-targeted delivery of siRNA using fatty acyl-CGKRK peptide conjugates.Scientific reports · 2017Article
- Necrosis-inducing peptide has the beneficial effect on killing tumor cells through neuropilin (NRP-1) targeting.Oncotarget · 2016Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The multiple physiological properties of glucagon-like peptide-1 (GLP-1) make it a promising drug candidate for the treatment of type 2 diabetes. However, the in vivo half-life of GLP-1 is short due to rapid degradation by dipeptidyl peptidase-IV (DPP-IV) and renal clearance. The poor stability of GLP-1 has significantly limited its clinical utility; however, many studies are focused on extending its stability. Fatty acid conjugation is a traditional approach for extending the stability of therapeutic peptides because of the high binding affinity of human serum albumin for fatty acids. However, the conjugate requires a complex synthetic approach, usually involving Lys and occasionally involving a linker. In the current study, we conjugated the GLP-1 molecule with fatty acid derivatives to simplify the synthesis steps. Human serum albumin binding assays indicated that the retained carboxyl groups of the fatty acids helped maintain a tight affinity to HSA. The conjugation of fatty acid-like molecules improved the stability and increased the binding affinity of GLP-1 to HSA. The use of fatty acid-like molecules as conjugating components allowed variant conjugation positions and freed carboxyl groups for other potential uses. This may be a novel, long-acting strategy for the development of therapeutic peptides.
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