Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021

Q Wu, W Qian, X Sun, S Jiang - Journal of hematology & oncology, 2022 - Springer
Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …

Cellular and molecular mechanisms of Hedgehog signalling

Y Zhang, PA Beachy - Nature Reviews Molecular Cell Biology, 2023 - nature.com
The Hedgehog signalling pathway has crucial roles in embryonic tissue patterning,
postembryonic tissue regeneration, and cancer, yet aspects of Hedgehog signal …

GPCRdb in 2021: integrating GPCR sequence, structure and function

AJ Kooistra, S Mordalski… - Nucleic Acids …, 2021 - academic.oup.com
G protein-coupled receptors (GPCRs) form both the largest family of membrane proteins and
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …

An insight into GPCR and G-proteins as cancer drivers

PK Chaudhary, S Kim - Cells, 2021 - mdpi.com
G-protein-coupled receptors (GPCRs) are the largest family of cell surface signaling
receptors known to play a crucial role in various physiological functions, including tumor …

Structural basis for strychnine activation of human bitter taste receptor TAS2R46

W Xu, L Wu, S Liu, X Liu, X Cao, C Zhou, J Zhang, Y Fu… - Science, 2022 - science.org
Taste sensing is a sophisticated chemosensory process, and bitter taste perception is
mediated by type 2 taste receptors (TAS2Rs), or class TG protein–coupled receptors …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …

Smoothened stimulation by membrane sterols drives Hedgehog pathway activity

I Deshpande, J Liang, D Hedeen, KJ Roberts, Y Zhang… - Nature, 2019 - nature.com
Hedgehog signalling is fundamental to embryonic development and postnatal tissue
regeneration. Aberrant postnatal Hedgehog signalling leads to several malignancies …

Structural basis of Smoothened regulation by its extracellular domains

EFX Byrne, R Sircar, PS Miller, G Hedger, G Luchetti… - Nature, 2016 - nature.com
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 GPCR residue numbers–aligning topology maps while minding the gaps

V Isberg, C De Graaf, A Bortolato, V Cherezov… - Trends in …, 2015 - cell.com
Generic residue numbers facilitate comparisons of, for example, mutational effects, ligand
interactions, and structural motifs. The numbering scheme by Ballesteros and Weinstein for …

Cholesterol access in cellular membranes controls Hedgehog signaling

A Radhakrishnan, R Rohatgi, C Siebold - Nature chemical biology, 2020 - nature.com
Abstract The Hedgehog (Hh) signaling pathway coordinates cell–cell communication in
development and regeneration. Defects in this pathway underlie diseases ranging from birth …