Enzymes are the workhorses of biology, and when they go wrong, they often form the basis of disease. Therefore, the ability to fine-tune their function with inhibitors is a key strategy in drug discovery. At Creative Biolabs, our core competency is the isolation of new molecules based on biological activity, which forms the foundation of our Functional Target Screening by Phage Display Services. Building on this powerful technology, we will take you on a journey into the world of enzyme inhibitor discovery. Functional screening's flagship application, we'll show you why it is so crucial and how our cutting-edge phage display platform is a game-changer in terms of speed, efficiency, and success rate. We'll explore how this powerful technique can be utilized to identify novel peptide-based inhibitors targeting a diverse range of enzyme targets, thereby accelerating research and development efforts within the biopharmaceutical industry.
Before we know "how," let's solidify the "why." Enzymes are biological macromolecules, typically proteins, that act as catalysts to speed up virtually all the chemical reactions that take place within cells. They are the workhorses of biology, essential for everything from digestion and metabolism to DNA replication and cellular signaling. Enzymes are often compared to a lock and a key. The lock is the enzyme, which has an active site (catalytic site) with a specific shape. The key is the substrate. Only the key (substrate) that is the correct size and shape can bind to the enzyme (lock). The binding of the substrate to the enzyme allows the chemical reaction to take place (conversion of the substrate into a product).
Because enzymes are so fundamental to biological processes, their dysregulation—being overactive, underactive, or active at the anachronistic time or place—is a standard driver of human disease.
By developing molecules that can selectively block the action of a specific enzyme implicated in a disease, we can effectively intervene in the pathological process. This precise enzyme targeting is the foundation of a significant portion of the modern pharmacopeia.
We provide a seamless, end-to-end solution built on a transparent and robust workflow to guarantee the highest quality results.
| Active-Site Competitive Screening | By introducing a known substrate or competitive inhibitor during the elution step, we can specifically enrich for clones that bind directly to the enzyme's active site. |
| Allosteric Inhibitor Screening | We utilize specialized panning conditions designed to capture binders that target allosteric sites, enabling the discovery of molecules with novel mechanisms of action. |
| Covalent Inhibitor Screening | By using libraries that display peptides containing reactive residues (e.g., cysteine), we can effectively screen for irreversible inhibitors that form a covalent bond with the target enzyme. |
The decision of whether to build capabilities in-house or to collaborate with a specialist is critical. By outsourcing enzyme inhibitor discovery to Creative Biolabs, you leverage focused expertise and a purpose-built platform designed for success. Here are some reasons why you can partner with us:
Discovery of new, potent, and safe drugs has never been more important. Enzyme inhibitors will continue to be a large class of therapeutics, and the technologies that we use to discover them need to be highly robust, accurate, and efficient. Phage display is an outstanding technology that has been repeatedly proven to deliver high-quality lead molecules, even against the most challenging targets. Creative Biolabs has fully utilized the technology's capabilities. Our in-house Enzyme Inhibitor Discovery platform, supported by our team's extensive experience and expertise, offers a direct and faster route to the next-generation therapeutics candidates. Are you looking to move your research forward and identify novel inhibitors for your enzyme of interest? today, and let's talk about your project and see how we can help.
How are enzyme inhibitors discovered?
Teams discover enzyme inhibitors by combining scale, selectivity, and mechanism. After target validation and assay development, we run high-throughput campaigns—DNA-encoded libraries, fragment-based screens, or phage-displayed peptides/antibodies—to surface tractable chemotypes. Hits proceed through orthogonal biophysics (SPR/BLI, DSF), detailed enzyme kinetics to assign competitive or allosteric modes, and cell-based counterscreens to de-risk off-targets. Medicinal chemistry then optimizes potency, selectivity, and ADME. At Creative Biolabs, diverse libraries and mechanistic selection schemes help convert binders into robust, mechanism-defined inhibitors.
When was phage display invented?
Phage display originated in 1985, when George P. Smith fused foreign peptides to the pIII coat protein of filamentous phage M13, linking genotype to displayed phenotype; antibody display followed soon after. Its transformative impact—through the iterative selection of high-affinity ligands and antibodies—was recognized by the 2018 Nobel Prize in Chemistry, awarded to Smith and Sir Gregory Winter. Creative Biolabs leverages this platform routinely to isolate enzyme-targeted peptides and antibody fragments.
What are the 4 types of enzyme inhibitors?
The four canonical inhibitor classes are competitive (active-site binders that raise apparent Km without changing Vmax), uncompetitive (bind the ES complex, lowering both Km and Vmax), noncompetitive/mixed (bind allosteric sites on E and ES, reducing Vmax with little Km shift), and irreversible (often covalent, permanently inactivating the enzyme). Proper classification relies on global kinetic modeling with mechanism-aware controls, rather than a single-timepoint IC50.
What materials do I need to provide?
You will typically need to provide your target enzyme at high purity and with confirmed biological activity. Our team will consult with you to determine the specific requirements and optimal amount of protein for the project.
What is the typical project timeline?
A standard project, from sample receipt to the delivery of initial validated hits, usually takes 1-3 months. The exact timeline may vary depending on project complexity and the scope of services selected.
Can you guarantee that an inhibitor will be found?
Several factors, including the druggability of the target and the inherent diversity of the library, significantly influence the outcomes of discovery research. While we cannot guarantee a specific outcome, we leverage our extensive experience to design a strategy that maximizes the probability of success and maintains transparent communication throughout the process.
Please kindly note that our services can only be used to support research purposes (Not for clinical use).
Creative Biolabs is a globally recognized phage company. Creative Biolabs is committed to providing researchers with the most reliable service and the most competitive price.
