Viewpoints:

Dispatches from the Frontlines of Research - edited by John W. Nelson

Neil Osheroff

Unraveling the Structure of the Variola Topoisomerase IB-DNA Complex: A Possible New Twist on Smallpox Therapy
Mol. Interv. 2006 6: 245-248. [Summary] [Full Text] [PDF]  

Molly J. Carlson and David E. Cummings

Prospects for an Anti-Ghrelin Vaccine to Treat Obesity
Mol. Interv. 2006 6: 249-252. [Summary] [Full Text] [PDF]  

Helen P. Carroll, Benjamin B.A. McNaull, and Massimo Gadina

Immunodeficiency Is A Tough Nut to CRAC: The Importance of Calcium Flux in T Cell Activation
Mol. Interv. 2006 6: 253-256. [Summary] [Full Text] [PDF]  

R E V I E W S:

Timothy A. Vortherms and Bryan L. Roth

Salvinorin A: From Natural Product to Human Therapeutics
Mol. Interv. 2006 6: 257-265. [Summary] [Full Text] [PDF]  

The hallucinogenic plant Salvia divinorum, a member of the mint family, has traditionally been used by the Mazatec natives of southern Mexico to induce ritual visions and is increasingly used in the US for recreational purposes. The main active ingredient in the plant is the diterpene salvinorin A, which is structurally distinct from other chemical classes of hallucinogens. In recent high-throughput screening experiments, salvinorin A was found to bind to the -opioid receptor (KOR) with high specificity. Chemical analogs of the compound are now under study, in concert with functional characterization of KOR, to determine whether modulation of KOR activity could provide a basis for new psychotropic medications. Indeed, there are indications that salvinorin A or its congeners may prove useful in both psychiatric and non-psychiatric diseases.

Philip J. Hajduk

SAR by NMR: Putting the Pieces Together
Mol. Interv. 2006 6: 266-272. [Summary] [Full Text] [PDF]  

Constructing novel drug leads from small molecular building blocks is a powerful new approach to drug discovery. This field, called fragment-based drug design, relies on the experimental detection and structural characterization of very weakly binding, low molecular–weight ligands that can be rapidly increased in potency using structure-based drug design. Numerous examples of fragment-based drug design now exist in the literature, and several compounds derived using this approach have made it into the clinic. This review will describe the concept of fragment-based drug design, discuss why it works, and use two case studies to illustrate the power of the approach.

Jack Bergman and Carol A. Paronis

Measuring the Reinforcing Strength of Abused Drugs
Mol. Interv. 2006 6: 273-283. [Summary] [Full Text] [PDF]  

The abuse liability of a drug is closely related to its ability to maintain self-administration behavior in laboratory subjects. But how do researchers gauge the reinforcing value of a self-administered drug in the preclinical laboratory? One approach is to determine the "preference" for that drug, that is, the allocation of behavior to drug taking, when alternative reinforcers are concurrently available. Careful analyses of such "choice" behavior in laboratory subjects can lead to a scientific understanding of the pharmacological and behavioral determinants of the reinforcing strength of a drug and, ultimately, to a more useful preclinical evaluation of abuse liability.

D E P A R T M E N T S:

Speaking of Pharmacology:

John S. Lazo

Roadmap or Roadkill: A Pharmacologist’s Analysis of the NIH Molecular Libraries Initiative
Mol. Interv. 2006 6: 240-243. [Full Text] [PDF]  

Nascent Transcripts:

Emerging concepts from the recent literature
Mol. Interv. 2006 6: 244. [Full Text] [PDF]  

Beyond the Bench:

Representations of pharmacology and science in the media

Dayle Houston

Trouble In Mind: Poisonous Roots
Mol. Interv. 2006 6: 284-285. [Full Text] [PDF]  

Net Results:

Sites of interest on the World Wide Web

Sites of interest on the World Wide Web—edited by David Roman
Mol. Interv. 2006 6: 286. [Full Text] [PDF]  

Outliers:

Cartoon

Outliers
Mol. Interv. 2006 6: 292. [Full Text] [PDF]  

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