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Hit-To-Lead Optimization in Pancreatic Cancer
Alfa Cytology is a full-scale preclinical research service provider with extensive experience. We are committed to providing a range of pancreatic cancer (PC) research and drug development services to our global clients ranging from pharmaceutical, biotechnology, and research institutions. Importantly, we can provide our services in a modular and integrated manner during the development of small molecule drugs according to our customers' requirements.
Introduction to Hit-To-Lead Optimization
Following the lead compound identification phase, several of the most promising lead compound structures will be selected for optimization. Pharmaceutical chemistry and efficacy testing are central to the lead compound optimization process.
- Modifying the lead compound's chemical structure can improve its potency, selectivity, pharmacokinetics, and safety.
- Maintain good molecular properties while addressing structural issues related to toxicity or side effects.
- Any structural molecular changes must be extensively tested by in vitro and in vivo bioassays. In addition to the obvious drug properties, other properties can be investigated, such as genotoxicity, metabolic stability, and in vivo behavior.
- Determine the optimal dose range, including consideration of the preferred route of administration (oral, intravenous, etc.) and the development of drug formulations that ensure long-term stability and reliable drug delivery.
Fig. 1 Target-based drug discovery steps. (Li Q.; 2020)
Our Services
During the compound design and compound synthesis, a range of parameters must be fully understood and considered, including potency, stability, bioavailability, efficacy, selectivity, pharmacokinetics, pharmacodynamics, and so on. The optimization of a lead structure is mainly through iterative rounds of medicinal chemistry design, synthesis, and testing. Our small molecule drug discovery project team has years of experience in pancreatic cancer therapy and compound optimization, and we are well equipped to drive your program forward.
- Medicinal Chemistry Platform
Through an in-depth understanding of the factors that influence the pharmacokinetics and the extensive use of structural biology and computational tools, Alfa Cytology is able to help our clients optimize the properties of their compounds in a comprehensive and rational manner. On our medicinal chemistry platform, a hypothesis-driven optimization is a powerful tool for driving compound optimization, including developing hypotheses to overcome problems and then interrogating those hypotheses in a cycle of design, synthesis, testing, and analysis.
- Structure-Based Assessment Platform
Size exclusion chromatography, X-ray crystallography, surface plasmon resonance (SPR), and nuclear magnetic resonance (NMR) are accessible to perform biophysical assays to find compound binding to candidate target proteins.
Several popular pancreatic cancer models are available at our company, including pancreatic cancer cell models, pancreatic cancer organoids, genetically engineered mouse models, and transplantation models. These models can be used to assist lead optimization.
- Computer-Aided Drug Design Platform
Using advanced modeling techniques and data analysis methods, we can support small molecule inhibitor discovery for pancreatic cancer therapy from hit identification to lead optimization. In addition to supporting the design and optimization process, our computational chemistry team has years of experience deploying a suite of computer tools to assist in the interpretation of in vitro and in vivo data.
- Synthetic Chemistry Platform
Our chemistry team consists of talented chemists who are able to ensure high compound productivity and maximum efficiency by using the latest synthetic chemistry methods and techniques with innovative synthetic route designs. Our synthetic chemistry capabilities include, but are not limited to, validation of synthetic routes, automated mass-oriented purification, multi-stage syntheses, and scale-up production.
Why Choose Us?
Scientific Excellence
Customized Solutions
Collaborative Approach
Worldwide Service
DataSecurity
Our services are based on in-depth scientific expertise, proven discovery platforms, and years of experience, supporting the optimization and translation of optimal solutions into single compounds to be delivered to our client partners. Thanks for your interest in our hit-to-lead optimization service, which is part of our integrated small molecule drug development for pancreatic cancer. In order to get more details about our services, please contact us. We've got everything covered for your needs.
References
- Hoelder, Swen, Paul A. Clarke, and Paul Workman. "Discovery of small molecule cancer drugs: successes, challenges and opportunities." Molecular oncology 6.2 (2012): 155-176.
- Li Q. Application of Fragment-Based Drug Discovery to Versatile Targets. Front Mol Biosci. 2020;7:180. Published 2020 Aug 5. doi:10.3389/fmolb.2020.00180
