Related Experiment Video
Updated: Jun 21, 2026
06:01
Extracellular Protein Microarray Technology for High Throughput Detection of Low Affinity Receptor-Ligand Interactions
Published on: January 7, 2019
7.3K
Small-Molecule Lead-Finding Trends across the Roche and Genentech Research Organizations
Peter S Dragovich1, Wolfgang Haap2, Melinda M Mulvihill1
1Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
Journal of Medicinal Chemistry
|February 9, 2022
Summary
This study analyzes the sources of small-molecule drug leads at Roche and Genentech from 2009-2020. It reveals trends in lead discovery methods and their translation into clinical development, highlighting organizational similarities and differences.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Pharmaceutical Research
Background:
- Analysis of small-molecule lead origins at Roche and Genentech (2009-2020).
- Covers diverse lead-finding methodologies employed by two independent research organizations.
Purpose of the Study:
- To describe the origin of small-molecule leads.
- To discuss the translation of leads into in vivo tool compounds and development candidates.
- To identify trends in lead-finding approaches and their future impact.
Main Methods:
- Review of lead series from various sources: public data, high-throughput screening (HTS), fragment-based design (FBD), DNA-encoded libraries (DEL), internal data, in-licensing, and de novo design.
- Analysis of biological target classes and therapeutic areas.
- Comparison of commonalities and differences between Roche and Genentech.
Main Results:
- Identified diverse origins of small-molecule leads across multiple discovery platforms.
- Detailed the progression of lead series to tool compounds and development candidates.
- Highlighted key trends and variations in lead generation strategies between the two organizations.
Conclusions:
- Lead-finding trends identified are expected to influence future research applications at Roche and Genentech.
- Understanding commonalities and differences aids in optimizing drug discovery pipelines.
- Caveats in data collection and analysis are noted for improved interpretation.
Related Concept Videos
02:40Ligand Binding Sites
Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
01:26Drug Discovery: Overview
Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...