Chemically derived peptide libraries: a new resin and methodology for lead identification.

Int J Pept Protein Res

Bayer Corporation, Clayton, North Carolina, USA.

Published: March 1997

We have developed a new resin for peptide synthesis that can be used to synthesize and evaluate directly combinatorial peptide libraries for binding target proteins. Fidelity of the peptide synthesis using this hydrophilic resin is comparable to polystyrene-based resins. Peptide libraries synthesized on this resin were probed by a two color PEptide Library Immunostaining Chromatographic ANalysis (PELICAN) technique for sequences binding the serine protease Factor IX zymogen. This PELICAN technique readily distinguishes between beads interacting with the reagents for target detection (blue beads) from those beads specific for the target protein itself (red beads). Validation of the PELICAN technique, as well as purification of Factor IX from plasma, is demonstrated utilizing this resin.

Download full-text PDF

Source
http://dx.doi.org/10.1111/j.1399-3011.1996.tb00812.xDOI Listing

Publication Analysis

Top Keywords

peptide libraries
12
pelican technique
12
peptide synthesis
8
peptide
6
resin
5
chemically derived
4
derived peptide
4
libraries resin
4
resin methodology
4
methodology lead
4

Similar Publications

Antimicrobial and plant defence elicitor peptides have received attention on last decades as novel tools to combat bacterial plant diseases. We previously reported a library of peptide conjugates resulting from the combination of an antimicrobial peptide (, , or ) and a plant defence elicitor sequence (, , or ). From this library, we selected a set of 14 peptide conjugates including both highly and poorly active sequences and we performed a structure-activity relationship study by NMR and MD simulations.

View Article and Find Full Text PDF

Triazination/IEDDA Cascade Modular Strategy Installing Pyridines/Pyrimidines onto Tyrosine Enables Peptide Screening and Optimization.

J Am Chem Soc

January 2025

State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, P. R. China.

Modular chemical postmodification of peptides is a promising strategy that supports the optimization and innovation of hit peptide therapeutics by enabling rapid derivatization. However, current methods are primarily limited to traditional bio-orthogonal strategies and chemical ligation techniques, which require the preintroduction of non-natural amino acids and impose fixed methods that limit peptide diversity. Here, we developed the Tyrosine-1,2,3-Triazine Ligation (YTL) strategy, which constructs novel linkages (pyridine and pyrimidine) through a "one-pot, two-step" process combining SAr and IEDDA reactions, promoting modular post modification of Tyr-containing peptides.

View Article and Find Full Text PDF

Introduction: The neuron-specific K-Cl cotransporter KCC2 maintains low intracellular chloride levels, which are crucial for fast GABAergic and glycinergic neurotransmission. KCC2 also plays a pivotal role in the development of excitatory glutamatergic neurotransmission by promoting dendritic spine maturation. The cytoplasmic C-terminal domain (KCC2-CTD) plays a critical regulatory role in the molecular mechanisms controlling the cotransporter activity through dimerization, phosphorylation, and protein interaction.

View Article and Find Full Text PDF

This study compared the efficacy and safety of glucogan-like peptide-1 receptor agonists (GLP1RAs) combined with metformin versus metformin alone in women with polycystic ovary syndrome (PCOS). A systematic search of "PubMed", "EMBASE", "Cochrane Library", and "Web of Science", "Google Scholar" was conducted up to September 2024. Studies were included if they were RCTs investigating the combination of GLP1RAs and metformin in women diagnosed with PCOS.

View Article and Find Full Text PDF

Objective: This network meta-analysis was to compare the efficacy of different drugs on cardiac function, renal function, and clinical outcomes in patients with acute heart failure (AHF) accompanied by renal dysfunction.

Methods: PubMed, EMBASE, Cochrane Library, and Web of Science were searched to screen all clinical trials of AHF between January 1st 2001 and March 31th 2024. The primary outcome measures were N-terminal pro-B type natriuretic peptide (NT-proBNP), B-type natriuretic peptide (BNP), glomerular filtration rate (GFR), blood urea nitrogen, serum creatinine, all-cause mortality within 60 days, and cardiovascular mortality.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!