Thermo stability is a property that the molecule retains its three-dimensional (3D) structure intact in high ambient temperature. It represents a critical parameter during pharmaceutical research and development. A drug doesn’t have to be highly thermostable, but the formulation of a drug needs to give a suitable bioavailability which means sufficiently reproducible to make a drug efficient and safe. As a famous expert in physical stability assessment, Creative Biolabs has investigated two approaches for protein thermostability, including experimental methods and computational analyses, to study the relationship between thermostability and conformational characteristics of potential drug proteins.
Thermo stability is the quality of a substance to resist irreversible change in its physical or chemical structure, normally by resisting decomposition or polymerization at a relatively high temperature. The adaptations of proteins towards an enhanced thermostability have been observed in natural environments (e.g. marine hydrothermal vents). Then, basic principles behind an enhanced thermostability can be applied in the biotech industry in order to design or engineer proteins with high stability. The demand for increased heat stability has to be balanced by the dynamic required for maintaining the catalytic activity of the enzyme. The hyper-thermophilic proteins consist of the common 20 amino acids. Hence, the optimization of interactions between amino acids in the peptide chain is a key feature for increased thermostability.
Owing to their structural complexity, assessment of peptide and protein drugs ask for extensive analysis, often by a variety of test ways. An essential part of pharmaceutical drug development is the evaluation of thermo stability of an active ingredient of the formulated compound. At Creative Biolabs, we offer a suite of fast, simple, and high-throughput thermostability-based assays to identify protein stabilizing factors, which facilitate the handling and characterization of drug molecules by subsequent structural analysis and functional studies, as well as ensure the development phase as short as possible. Here, there’s a summary of our robust thermo stability assays, including but not limited to:
This method simplifies the identification of thermostabilizing conditions and can be used to study the thermal stability of membrane proteins, without either purification or radioligands. And many parameters, such as additive lipids, detergents, ligands, and receptor variants, can also be assessed for their impacts on membrane protein thermostability.
The method allows determining a melting temperature (Tm), in which the protein is gradually heated. The Tm value is the temperature, at which a half-maximal fluorescence (maximal fluorescence at the highest temperature) is observed. And the higher Tm temperature, the more stable it is a protein.
This method can perform quantities of thermostability measurement of protein samples (particularly enzymes) at the same time, and also collects other parameters like catalytic activity, substrate specificity, etc.
The pharmaceutical development of protein drugs shows new challenges in the field of stability assessment, including thermo stability. These products require more analytical effort than classic drugs, which may even dictate the speed of progress in certain development phases. As a well-recognized supplier in the bioassay market, Creative Biolabs pays attention to the initial stage of the pharmaceutical development of pre-formulation studies and provides a series of high-throughput approaches to determine the thermostability of desired compounds. If you’re interested in any physical assessment, please directly contact us or consult our experts online.
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