Reports of increasing antibiotic resistance and sagging drug discovery rates are appearing with increasing frequency, and many warn that we are living on the wrong side of an antibiotic peak—a period in which everfewer new antibiotics are being discovered at ever-increasing costs (1). In response, efforts to discover new antibiotics and other drugs have taken many forms, including looking at fo...

Chemogenomics is a new strategy in drug discovery which, in principle, searches for all molecules that are capable of interacting with any biological target. Because of the almost infinite number of drug-like organic molecules, this is an impossible task. Therefore chemogenomics has been defined as the investigation of classes of compounds (libraries) against families of functionally related pr...

The National Cancer Institute's (NCI's) human tumor cell line panel for screening potential new anticancer drugs is now operational (/). Its implementation and the demonstration of its feasibility represent a technical and organizational tour de force. The rationale for the change in the primary screen from leukemias in mice to the array of 60 human cancer cell lines was earlier debated in cont...

In the past two decades, the identification of commonly mutated oncogenes and tumour suppressor genes has driven an unprecedented growth in our understanding of the genetic basis of human cancer. Although oncogenes can clearly serve as classically defined drug targets whose inactivation by small molecules could place a brake on cancer cell proliferation, the restoration of mutated tumour suppre...

Chemokines and Drug Discovery was a one-day meeting organized by the Society for Medicines Research, held at the Novartis Horsham Research Centre in Horsham, United Kingdom, on March 11, 2004. More than 100 scientists, mostly from industry, attended this meeting.

Current drug discovery is dominated by label-dependent molecular approaches, which screen drugs in the context of a predefined and target-based hypothesis in vitro. Given that target-based discovery has not transformed the industry, phenotypic screen that identifies drugs based on a specific phenotype of cells, tissues, or animals has gained renewed interest. However, owing to the intrinsic com...

Fragment-based drug discovery (FBDD), while still a relatively new approach, has been so successful for identifying ligands for protein targets that it is alreadywidely regarded as representing a sea-change in drug discovery techniques. The strategy involves identifying small (typically ,300Da), low-affinity ligands (‘fragments’) and combining or expanding these to produce larger, higher-affini...

Components from venoms have stimulated many drug discovery projects, with some notable successes. These are briefly reviewed, from captopril to ziconotide. However, there have been many more disappointments on the road from toxin discovery to approval of a new medicine. Drug discovery and development is an inherently risky business, and the main causes of failure during development programmes a...

OPINION article Front. Drug. Discov., 24 August 2022Sec. Technologies and Strategies to Enable Drug Discovery https://doi.org/10.3389/fddsv.2022.983030

The development of therapies for the treatment of neurological cancer faces a number of major challenges including the synthesis of small molecule agents that can penetrate the blood-brain barrier (BBB). Given the likelihood that in many cases drug exposure will be lower in the CNS than in systemic circulation, it follows that strategies should be employed that can sustain target engagement at ...