Peptide molecules to specifically bind targets such as aptamer, avimer and kunitz domain have been intensively studied and developed as alternatives to antibodies. The peptides with high affinity to targets can be used as drugs or diagnostic agents, particularly where whole antibodies may be unsuitable. Given applicability and market potential of peptide molecules as drugs or diagnostic agents, a multitude of companies and laboratories are researching to seek peptide molecules with a novel structure.
By conjugation to a set of sixteen polypeptides, a small binding molecule can evolve into a polypeptide binder with increased affinity and selectivity.
CRP is a well-known biomarker of inflammation in humans and binders recognizing it are therefore of large interest as medical diagnostics. Until now, phosphocholine (PCh) and derivatives are the only known small molecule binders for CRP, but they have low μM affinity and bind CRP in a Ca2+ dependent manner. The small molecule DQ was designed as a CRP binder that is structurally unrelated to PCh. Its polypeptide conjugate, 4-C25l22-DQ, was demonstrated as a strong, Ca2+ independent binder for CRP, and had an affinity approximately three orders of magnitude higher than DQ itself.
HCA IX is a protein that is interesting for diagnosis of cancer. AZM is a small molecule inhibitor of HCAs with a dissociation constant of 38 nM for HCA II and 3 nM for HCA IX. Interestingly, polypeptide conjugate 4-C10L17-AZM displayed stronger binding to both HCA II (KD 4 nM) and HCA IX (KD 90 pM). This result provided evidence that the binder concept can be applied also for small molecules which already have high affinity for their protein receptors.
LSD1 is an enzyme that regulates the methylation of Lys 4 of histone 3 via a PPI-like interaction and which is of therapeutic interest in certain cancers. Based on the structures of two peptidic ligands bound to LSD1, we sequentially prepared truncated, mono-substituted and macrocyclic peptides in order to develop reversible inhibitors of LSD1. Some stapled cyclic peptides bound to LSD1 with 10-fold higher affinity than the corresponding linear parent peptide. Changing the staple into a lactam further improved the binding potency and the best lactams inhibited the enzymatic activity of LSD1 at low μM Ki values.
In conclusion, it is important for the selection of peptide binders suitable for multiple purposes in biology, biotechnology, and medical science. Creative Peptides has extensively synthetic peptides binders which have potential as molecular target drugs comparable to that of monoclonal antibodies. It is the company of choice to manufacture your stapled peptide requirements, providing a confidential and efficient service at competitive prices. Every step of peptide synthesis is subject to Creative Peptides' stringent quality control. Typical delivery specifications include:
A peptide target binder is a small molecule or peptide that specifically binds to a target protein or molecule, enabling high affinity and specificity. These peptides are developed for applications in research, diagnostics, and therapeutic investigations. They offer a unique structural scaffold and are an alternative to traditional antibodies, providing advantages such as smaller molecular weight and cost-effective production.
Peptide target binders offer several benefits, including lower molecular weight, ease of synthesis, and cost-effectiveness. They also exhibit high affinity to target molecules, can be customized for specific applications, and have versatile uses across research and industrial applications.
Peptide target binders can be designed to target a wide variety of proteins and molecules, including biomarkers like C-reactive protein (CRP), enzymes such as carbonic anhydrases (HCA), and regulatory proteins involved in cancer. The versatility of peptide binders makes them applicable across multiple fields, from diagnostics to proteomics research.
Peptide target binders are developed using various strategies, including chemical modifications to improve protease resistance and metabolic stability. Structural information is used to optimize binding modes, and theoretical simulations predict their dynamic actions. These strategies ensure that the binders have high specificity and efficacy.
Peptide target binders are critical in biomarker discovery as they provide high specificity for targeting proteins associated with diseases. By binding selectively to biomarkers, these peptides can facilitate the identification and quantification of proteins, offering insights into disease mechanisms and enabling early detection strategies.
Yes, peptide target binders are well-suited for high-throughput screening due to their small size, ease of production, and customizable binding properties. They can be applied in automated systems to rapidly evaluate interactions with a wide range of target molecules, making them ideal for large-scale research projects.
Developing peptide target binders can be challenging due to issues like binding specificity, stability, and affinity. However, these challenges are addressed through optimization of peptide sequences, conjugation with polypeptides to enhance affinity, and using advanced techniques like stapled peptides to improve binding potency and stability.
Peptide target binders offer a distinct advantage over other molecular tools such as monoclonal antibodies. Their small size and customizable nature allow for easier synthesis and more precise targeting. Additionally, peptide binders can be more versatile in complex biological environments, providing a practical solution for a variety of research applications.
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