Viewpoints:

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

Dzung H. Nguyen and Dennis D. Taub

Targeting Lipids to Prevent HIV Infection
Mol. Interv. 2004 4: 318-320. [Summary] [Full Text] [PDF]  

Chris Hague, Randy A. Hall, and Kenneth P. Minneman

Olfactory Receptor Localization and Function: An Emerging Role for GPCR Heterodimerization
Mol. Interv. 2004 4: 321-322. [Summary] [Full Text] [PDF]  

Gergely Szakács and Michael M. Gottesman

Comparing Solid Tumors with Cell Lines: Implications for Identifying Drug Resistance Genes in Cancer
Mol. Interv. 2004 4: 323-325. [Summary] [Full Text] [PDF]  

R E V I E W S:

Lee E. Limbird

The Receptor Concept: A Continuing Evolution
Mol. Interv. 2004 4: 326-336. [Summary] [Full Text] [PDF] Correction to doi  

It might not be too much of a stretch to sum up the Dark Ages of receptor biology by invoking Sidney Harris's famous cartoon of two scientists standing at the blackboard where, in the middle of a written mathematical proof, one scientist has written, "Then a miracle occurs." The meticulous research of Paul Ehrlich branded the beginnings of this research field, as we know it, with no small degree of sophistication, and one wonders what he would have accomplished with modern-day technology. Moving from concepts of selectivity and preferential distribution, other researchers demonstrated the concept of concentration-dependent antagonism. More modern analyses engendered the concepts of affinity, relative potency, radioligand binding, culminating in the contemporary study of signal transduction and molecular mechanisms of disease.

Kenneth A. Jacobson, Soo-Kyung Kim, Stefano Costanzi, and Zhan-Guo Gao

PURINE RECEPTORS: GPCR STRUCTURE AND AGONIST DESIGN
Mol. Interv. 2004 4: 337-347. [Summary] [Full Text] [PDF]  

G protein–coupled receptors constitute the most common protein class to be targeted by modern drugs-and by modern drug developers. Nevertheless, the crystal structure of only one GPCR (i.e., Rhodopsin) has been solved, and with at least 700 GPCRs in the human genome, the design of specific GPCR-targeting drugs poses a formidable challenge. Computer modeling and ligand docking are enabling researchers to determine the consequences of structurally altering both GPCRs and their ligands, offering important insights into GPCR function and routes to drug design. Purine receptors are exemplary GPCRs in a number of contexts, and ongoing investigations suggest that ligand design may be—literally—only half of the battle in the future of certain GPCR-based therapies.

Tammy M. Seasholtz and Joan Heller Brown

RHO SIGNALING in Vascular Diseases
Mol. Interv. 2004 4: 348-357. [Summary] [Full Text] [PDF]  

Small monomeric G proteins of the Rho family interact with a variety of effector and regulatory proteins to regulate signaling cascades that involve protein phosphorylation and dephosphorylation. The contraction of vascular smooth muscle is becoming increasingly recognized as a context in which Rho has clinical implications. Rat models of hypertension, along with an increasing variety of pharmacological tools, have established that at least one Rho protein (i.e., RhoA) can contribute to vascular disease. Indeed, the finding that the widely prescribed statins inhibit the isoprenyl modification and Rho may suggest that therapeutic modulation of Rho is already in practice. Cellular responses that emanate from Rho signaling in vascular disease likely engage the regulation of nitric oxide synthase activity and culminate in smooth muscle cell migration, contraction, and DNA synthesis.

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

Reflections:

Science in the cultural context

Stanley Scheindlin

Transdermal Drug Delivery: PAST, PRESENT, FUTURE
Mol. Interv. 2004 4: 308-312. [Full Text] [PDF]  

CrossTalk:

Interviews with people in the world of pharmacology

ROBERT TEMPLE: An eye for data
Mol. Interv. 2004 4: 313-317. [Summary] [Full Text] [PDF]  

Beyond the Bench:

Representations of pharmacology and science in the media

Dan Collinge

Frankenstein’s Castle (On Long Island)
Mol. Interv. 2004 4: 358-359. [Full Text] [PDF]  

Net Results:

Sites of interest on the World Wide Web

Sites of interest on the World Wide Web–edited by Rick Neubig and David Roman
Mol. Interv. 2004 4: 360. [Full Text] [PDF]  

Outliers:

Cartoon

Mol. Interv. 2004 4: 364. [Full Text] [PDF]  

To see an article, click its [Full Text] link. To review many summaries, check the boxes to the left of the titles you want, and click the 'Get All Checked Summary(s)' button. To see one summary at a time, click its [Summary] link.