Modern Drug Discovery ACS Publications
May 2003 From Concept to Development
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Volume 6, Issue 5
Article Indexes
Author Indexes



Focus on phosphate (326 KB)
by Mark S. Lesney
Developing effective drugs targeted to specific physiological processes is the ultimate goal of medicinal chemistry. The G-protein coupled receptors (GPCRs) are specific metabolic receptors for the majority of target-directed drug discovery. But like the GPCRs, kinases are involved in the all-critical function of signal transduction. In cancer or autoimmune disease, the inappropriate or badly timed signal leads to damaging responses (e.g., tumor growth, inappropriate angiogenesis, erroneous apoptosis). Drugs that inhibit the inappropriate expression of a kinase in a patient can stop the signaling cascade in its tracks and mean the difference between life and death. Biochemists have speculated for years about the potential value of kinases as drug targets, and these phosphate-transferring enzymes have become today’s hot topic of drug research.

Focus on phosphate

SPRing screening (172 KB)
by Stefan Löfås
Surface plasmon resonance (SPR) technology can provide detailed functional characterization of biomolecular interactions across the drug discovery and development spectrum—serving not only to identify novel drug targets, but also to give researchers the opportunity to make yes/no decisions on a drug candidate much earlier in the drug discovery process. The unique functional data provided by SPR is being used for a wide variety of life science and drug discovery applications, from proteomics to neurobiology and cancer research. With its application in pre-clinical, clinical, and quality assurance/quality control (QA/QC), SPR can offer advantages in quality, reliability, and throughput of data from the earliest stages of research to the strict regulatory environment of drug manufacturing.

SPRing screening


Content in Context
SARS wars
(35 KB)
by James F. Ryan

News in Brief (206 KB)
Combi-extensionsProtein chipEggs, not butterFDA looks forwardPox pill penetrationInterfering with HCVThiamine to tumorAspirin toxicity—NO wayGoing with the flowChemical matchmaker

Caffeine chroniclesFor Your Health
Caffeine chronicles
(131 KB)
by Mark S. Lesney
This natural high may be the most widely used “herbal remedy”; as purified drug it is in a host of medications.

Applications NoteBook
The tablet’s coat du jour
(83 KB)
by John T. Thornton
Atomic force microscopy has found a place in characterizing pharmaceutical process development.

Sites and Software
E pluribus unum
(89 KB)
by Ludwig Franzisket
A chemical information system for a global R&D organization bridges disparate cultures, synthetic processes, and informatics systems.


The Business Page
Patents and property
(55 KB)
By Joseph G. Contrera and Belinda M. Lew
A primer on legal rights for start-up companies

The Tool Box
From gene to protein
(87 KB)
by Burkhard Ziebolz
Cell-free translation systems are steadily changing the face of biochemistry.

Desperately seeking quinineThe Time Line
Desperately seeking quinine
(83 KB)
by Vassiliki Betty Smocovitis
The malaria threat drove the Allies’ WWII “Cinchona Mission”.

Clinical Trials Track
Kinase inhibitors
(89 KB)
by Mark S. Lesney
Researchers eye compounds that prevent or compete with phosphorylation, hoping to find another Glivec.

Product Info Now (153 KB)

On the Calendar (71 KB)
HPLC 2003

Diseases and Disorders
Fragile X syndrome
(89 KB)
by Randall C. Willis