As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …

Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …

The sonic hedgehog (Shh) signaling pathway is a major regulator of cell differentiation, cell
proliferation, and tissue polarity. Aberrant activation of the Shh pathway has been shown in …

The hedgehog (HH) signaling pathway regulates normal cell growth and differentiation. As a
consequence of improper control, aberrant HH signaling results in tumorigenesis and …

In vertebrates, sterols are necessary for Hedgehog signaling, a pathway critical in
embryogenesis and cancer. Sterols activate the membrane protein Smoothened by binding …

Developmental signals of the Hedgehog (Hh) and Wnt families are transduced across the
membrane by Frizzled-class G-protein-coupled receptors (GPCRs) composed of both a …

Generic residue numbers facilitate comparisons of, for example, mutational effects, ligand
interactions, and structural motifs. The numbering scheme by Ballesteros and Weinstein for …

Abstract The Hedgehog (Hh) signaling pathway coordinates cell–cell communication in
development and regeneration. Defects in this pathway underlie diseases ranging from birth …

Advanced basal cell carcinomas (BCCs) frequently acquire resistance to Smoothened
(SMO) inhibitors through unknown mechanisms. Here we identify SMO mutations in 50%(22 …