The σ subunit is the key regulator of bacterial transcription. Proteolysis of Thermus aquaticus
σ A , which occurred in situ during crystallization, reveals three domains, σ 2 , σ 3 , and σ 4 , …

A method is described for the elucidation of protein−protein interactions using novel cross-linking
reagents and mass spectrometry. The method incorporates (1) a modular solid-phase …

Differences in the ability of opioid drugs to promote regulated endocytosis of μ-opioid receptors
are related to their tendency to produce drug tolerance and dependence. Here we show …

In comparison to endogenous ligands of seven-transmembrane receptors, which typically act
as full agonists, many drugs act as partial agonists. Partial agonism is best described as a “…

Posttranslational modifications (PTMs) of the β-2 adrenoceptor (B2AR) play a fundamental
role in receptor regulation by agonists. We have examined the effects of several agonists on …

Endosomal signaling downstream of G-protein-coupled receptors (GPCRs) has emerged as
a novel paradigm with important pharmacological and physiological implications. However, …

Semisynthesis of an active tetraphosphorylated analogue of the Type I TGFβ receptor is
reported. An efficient native chemical ligation protocol was developed to link a …

The ability of chemically distinct ligands to produce different effects on the same G protein–coupled
receptor (GPCR) has interesting therapeutic implications, but, if excessively …

An integrated approach is described that allows the domain-specific incorporation of optical
probes into large recombinant proteins. The strategy is the combination of two existing …

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