跳至主要内容

Inventory of Several Sources of Peptide Drugs

 

Polypeptide is a chemically active substance ubiquitous in organisms. It is a type of compound composed of amino acids connected by peptide bonds. Compared with other chemical drugs and biotechnology drugs, peptide drugs have significant activity, strong specificity, and receptors. The affinity is good, the toxicity is weak, and it is generally not easy to accumulate in the body; the immunogenicity is weak or even non-existent relative to the protein, and the structure is easy to modify, easy to produce, and can even be solved by synthetic methods. Peptide drug research and development is a hot spot in the current pharmaceutical market. Today, let’s briefly understand what are the main sources of peptide drugs?

Medicilon relies on its strong drug innovation technology strength, integrates the company's internal superior resources, and joins forces among departments to build a platform for Medicilon's peptide drug conjugate (PDC) research and development into a technologically with advanced platform, complete supporting facilities and functions and standardized operation. It can form a comprehensive innovative drug research and development platform with integrated innovation capabilities, develop and provide key technologies, and can provide services such as the research and innovative peptide drugs, new peptide dosage forms, and peptide generic drugs.

            Peptide Synthesis

The Medicilon peptide synthesis research team closely focuses on the theme of peptide drug research and is committed to solving the core issues that limit the development and application of peptide drugs. Currently, it has established the synthesis of upstream non-natural amino acid structural units, peptide drug modification, and large-scale synthesis, to a complete system for research on downstream peptide drug signal transduction pathways and mechanisms of action. Through multi-disciplinary cooperation and crossover in chemistry, biology, medicine, pharmacy, etc., the team has achieved outstanding achievements in both basic and applied research.

Naturally extracted peptides

Such as osteopeptide. There are active components in some natural products, which can be extracted from simple mixtures by solvent extraction. If the natural products have complex components and very few active components, it is necessary to use enzymatic hydrolysis or microwave-assisted digestion to make the protein The precursor is degraded, and the active fragments are separated and detected by the detection equipment, and the active small peptides are quickly and effectively found from the mixture.

Chemical synthesis of peptides

The biological activity of peptides is extensive and important, and can be widely used in the endocrine system, immune system, digestive system, cardiovascular system, blood system, musculoskeletal system, etc., and with the maturity of peptide synthesis technology and the improvement of pharmaceutical preparation technology, peptide drugs Research and development has become the focus of attention of domestic and foreign drug research and development companies. The chemical synthesis of peptides includes solid-phase synthesis, liquid-phase synthesis, and solid-phase and liquid-phase combined fragment synthesis.

The liquid-phase method is the first peptide synthesis method developed, and the solid-phase peptide synthesis method is currently the commonly used method for peptide synthesis. After years of research and development, the solid-phase peptide synthesis method not only overcomes the time-consuming and cumbersome liquid phase synthesis, but also reduces the loss caused by the operation. The biggest advantage is that all the purification steps in the synthesis are simply washed and filtered. Complete, greatly reduce the difficulty of purification, has the advantages of convenience and quickness, simple operation and high yield. Its superiority is also expressed in the ease of automation. In the research and development of peptide drugs, the many characteristics of peptides have caused difficulties and challenges in the analysis process. In the analysis of peptide biotechnology drugs, Medicilon Biotechnology Drug Analysis Department flexibly uses ELISA, ECL, TRFIA, CLIA, IF, IP, CoIP, qPCR, FACS, ELISpot, enzymology and other methods to support cutting-edge biology Drugs such as proteins, antibodies (monoclonal antibodies, bi- or multispecific antibodies, antibody fragments), ADCs, peptides, nucleic acids, vaccines and cell gene therapy and other drugs in the early development, preclinical and clinical stages of PK/TK/Immunogenicity (Total ADA& Nab)/Biomarker&Cytokine and other research evaluation.

Gene recombination

Recombinant gene polypeptides, such as laglutide, insulin, etc. As a new biological method that has only started to develop rapidly in recent decades, gene recombination technology has received widespread attention since its inception and has been widely used in the field of medicine. With the progress of modern biotechnology, especially the introduction of genetic engineering technology, people can synthesize more peptide drugs in a short period of time and make it possible to produce peptide drugs on a large scale.

Synthetic biology

Synthetic biology is an emerging field formed by the intersection of biology, engineering, chemistry and information technology. It is the design and construction of new biological accessories, equipment and systems, and the redesign of surviving natural biology for application purposes. system. Its application fields are extremely wide, including medicine, chemicals, food, industrial enzymes, personal care, energy, agriculture, etc., among which medicine, chemical industry and energy are the key areas of synthetic biology product development.

According to reports, Li Jian’s research group from the School of Material Science and Technology of Shanghai University of Science and Technology has made important progress in the in vitro biosynthesis of complex natural products. It is the first to use cell-free synthetic biology to achieve the in vitro biosynthesis of the non-ribosomal polypeptide antibiotic valinomycin. . In view of the advantages of the cell-free system with controllable reaction conditions, fast reaction rate, high product yield, and no cytotoxic effects, cell-free synthetic biology will provide a new way for the discovery and synthesis of natural product drugs. This method has the characteristics of high throughput, and will greatly simplify the research and identification process of unknown (new) natural product synthetic gene clusters.

At present, people have been able to use high-tech methods to isolate a variety of biologically active peptides from animals, plants and microorganisms. Their physiological functions are mainly immune regulation, growth promotion, anti-thrombosis, anti-hypertension, lowering cholesterol, and inhibiting bacteria. , Virus, anti-cancer, anti-oxidation and free radical scavenging effects, improve element absorption and mineral transportation. Although the development of peptide drugs still faces huge challenges, with the development of science and technology in the future, people will overcome the shortcomings of peptide drugs, and new peptide technologies will be applied to pharmaceuticals.

评论

此博客中的热门博文

What is preclinical testing?

In the process of  preclinical testing  of a compound or biological agent into a drug, the compound involved must go through the testing phase. First, we need to identify potential targets that can treat the disease. Then, a variety of compounds or preparations are screened out. Any compound that has shown potential as a drug for the treatment of this disease needs to be tested for toxicity before clinical testing to reduce the possibility of injury. preclinical testing What is the basis of preclinical testing? According to US Food and Drug Administration (FDA) regulations, a series of tests are required before a new drug is approved for use. In the first stage, basic research determines a hypothetical target for the treatment of a certain disease, and then screens small molecules or biological compounds to discover any substance with the potential to treat the disease. Then, a  preclinical research  phase followed, before which, as described above, the potential toxicity of the compou

Inventory of the three major in vitro pharmacokinetic research methods

  The metabolic properties of a compound are an essential factor in whether or not it can be used as a drug in the clinical setting, so pharmacokinetic studies of newly synthesized compounds are required in drug development. In vitro incubation with liver microsomes, recombinant CYP450 enzyme lines, and in vitro incubation with hepatocytes are some of the more common in vitro drug metabolism methods. 1. In vitro incubation method with liver microsomes The metabolic stability and metabolic phenotypes of candidate compounds in different species of liver microsomes are good predictors of the metabolic properties of compounds in vivo. They are practical tools for evaluating candidate compounds in the pre-development phase of drug development. Liver microsomes include rat liver microsomes, human liver microsomes, canine liver microsomes, monkey liver microsomes, and mouse liver microsomes. In in vitro incubation of the liver, microsomes are the "gold standard" for in vitro d

Novel Parkinson’s Therapies Possible with New Mouse Model

Parkinson's disease (PD) is a neurodegenerative disorder that is marked by the accumulation of the protein, α-synuclein (αS), into clumps known as Lewy bodies, which diminish neural health. Now, researchers from Brigham and Women's Hospital (BWH) report the development of a mouse model to induce PD-like αS aggregation, leading to resting tremor and abnormal movement control. The mouse responds to L-DOPA, similarly to patients with PD. The team's study (“Abrogating Native α-Synuclein Tetramers in Mice Causes a L-DOPA-Responsive Motor Syndrome Closely Resembling Parkinson’s Disease”) on the use of this transgenic mouse model appears in  Neuron . “α-Synuclein (αS) regulates vesicle exocytosis but forms insoluble deposits in PD. Developing disease-modifying therapies requires animal models that reproduce cardinal features of PD. We recently described a previously unrecognized physiological form of αS, α-helical tetramers, and showed that familial PD-causing missense mutati