Hedgehog signaling: from basic biology to cancer therapy

F Wu, Y Zhang, B Sun, AP McMahon, Y Wang - Cell chemical biology, 2017 - cell.com
The Hedgehog (HH) signaling pathway was discovered originally as a key pathway in
embryonic patterning and development. Since its discovery, it has become increasingly …

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 for Smoothened receptor modulation and chemoresistance to anticancer drugs

C Wang, H Wu, T Evron, E Vardy, GW Han… - Nature …, 2014 - nature.com
The Smoothened receptor (SMO) mediates signal transduction in the hedgehog pathway,
which is implicated in normal development and carcinogenesis. SMO antagonists can …

Sterols in an intramolecular channel of Smoothened mediate Hedgehog signaling

X Qi, L Friedberg, R De Bose-Boyd, T Long… - Nature chemical …, 2020 - nature.com
Smoothened (SMO), a class Frizzled G protein-coupled receptor (class F GPCR), transduces
the Hedgehog signal across the cell membrane. Sterols can bind to its extracellular cysteine …

Sonic Hedgehog dependent phosphorylation by CK1α and GRK2 is required for ciliary accumulation and activation of smoothened

Y Chen, N Sasai, G Ma, T Yue, J Jia, J Briscoe… - PLoS …, 2011 - journals.plos.org
Hedgehog (Hh) signaling regulates embryonic development and adult tissue homeostasis
through the GPCR-like protein Smoothened (Smo), but how vertebrate Smo is activated …

Small‐molecule inhibitors of the hedgehog signaling pathway as cancer therapeutics

S Peukert, K Miller‐Moslin - … : Chemistry Enabling Drug …, 2010 - Wiley Online Library
Abstract Inhibitors of the Hedgehog (Hh) molecular signaling pathway have emerged in
recent years as a promising new class of potential therapeutics for cancer treatment …

Strategies to target the Hedgehog signaling pathway for cancer therapy

M Xin, X Ji, LK De La Cruz, S Thareja… - Medicinal Research …, 2018 - Wiley Online Library
Hedgehog (Hh) signaling is an essential pathway in the human body, and plays a major role
in embryo development and tissue patterning. Constitutive activation of the Hh signaling …

Modulators of the hedgehog signaling pathway

P Heretsch, L Tzagkaroulaki, A Giannis - Bioorganic & medicinal chemistry, 2010 - Elsevier
Since its discovery by C. Nüsslein-Volhard and EF Wieschaus, hedgehog (hh) signaling has
come a long way. Today it is regarded as a key regulator in embryogenesis where it governs …

Targeting of Smoothened for therapeutic gain

M Ruat, L Hoch, H Faure, D Rognan - Trends in Pharmacological Sciences, 2014 - cell.com
The Smoothened (Smo) receptor is a key transducer of the Hedgehog (Hh) signaling
pathway, which plays a critical role in tissue maintenance and repair. Recent studies have …

Cooperative integration between HEDGEHOG-GLI signalling and other oncogenic pathways: implications for cancer therapy

S Pandolfi, B Stecca - Expert reviews in molecular medicine, 2015 - cambridge.org
The HEDGEHOG-GLI (HH-GLI) signalling is a key pathway critical in embryonic
development, stem cell biology and tissue homeostasis. In recent years, aberrant activation …