Drug discovery and development is a complex and resource-intensive process that plays a crucial role in bringing innovative therapies. One of the key stages in this process is hit-to-lead, where the identification of small-molecule modulators of protein function is transformed into high-content lead series. At Alfa Cytology, we offer a comprehensive hit-to-lead service that combines our expertise and a commitment to scientific excellence.
Fig.1 Hit-identification strategies. (Bleicher, K. H., et al., 2003)
Introduction to Hit-to-lead
A Hit is a compound that displays desired biological activity towards a drug target and reproduces this activity when retested. There are several methods for Hit finding such as High-Throughput Screening (HTS), virtual screening (VS), or fragment-based drug discovery (FBDD).
A lead is a chemical compound within a defined chemical series having demonstrated a robust pharmacological and biological activity on a specific therapeutic target. This chemical structure is used as a starting point but require further optimization through chemical modifications or structural changes.
Hit-To-Lead Process aims to refine the large number of hits down into a small number of highly potent and selective lead compounds for optimization. The process usually begins with hit molecules being grouped together based on structural similarity and ranked based on potency, target affinity and ligand efficiency.
Our Services
At Alfa Cytology, we understand the critical need for effective small molecule in the battle against cancer. As a trusted preclinical CRO, we offer a specialized hit-to-lead service tailored specifically for small molecule development. Our services include, but are not limited to:
Target Identification and Evaluation
The first step in the hit-to-lead process is the identification and evaluation of potential drug targets. Our experts utilize the latest advancements in functional genomics and proteomics to identify key proteins and pathways involved in cancer development and progression.
Hit Expansion and Lead Identification
Our team conducts hit expansion studies to explore structure-activity relationships (SAR) and optimize the hit compounds for potency, selectivity, and drug-like properties. We also leverage computer-aided drug design (CADD) techniques to generate binding hypotheses and guide lead optimization efforts.
ADME/PK Assessment and Optimization
Alfa Cytology conducts ADME/PK (absorption, distribution, metabolism, excretion/pharmacokinetics) assessments to evaluate the drug-like properties of lead compounds. Our robust ADME/PK assays provide critical insights into compound stability, solubility, bioavailability, and metabolic fate.
Target Engagement Biomarker Assay Development
To further support lead identification and optimization, we develop target engagement biomarker assays. These assays enable the assessment of compound binding to the target protein and provide valuable information on target engagement and downstream signaling pathways.
Our Advantages
Professional and well-trained technical team
Advanced experimental equipment
Empowering success through cooperation
Strict quality control system
At Alfa Cytology, we understand the complexities involved in the hit-to-lead process. Our team of highly skilled scientists works closely with clients to define the desired compound profile required for their specific anti-cancer drug development program. With customized solutions, we are committed to supporting our clients' drug discovery programs and contributing to the fight against cancer. If you are interested in our service, please contact us for more details.
Reference
- Bleicher, K. H., et al.; (2003). Hit and lead generation: beyond high-throughput screening. Nature reviews Drug discovery, 2(5), 369-378.
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