Results 11 to 20 of about 718,149 (279)

Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase [PDF]

Journal of Medicinal Chemistry, 2023
Hedgehog signaling is involved in embryonic development and cancer growth. Functional activity of secreted Hedgehog signaling proteins is dependent on N-terminal palmitoylation, making the palmitoyl transferase Hedgehog acyltransferase (HHAT), a potential drug target and a series of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines have been identified as HHAT ...
Markus Ritzefeld, Leran Zhang, Zhangping Xiao, Sebastian A. Andrei, Olivia Boyd, Naoko Masumoto, Ursula R. Rodgers, Markus Artelsmair, Lea Sefer, Angela Hayes, Efthymios-Spyridon Gavriil, Florence I. Raynaud, Rosemary Burke, Julian Blagg, Henry S. Rzepa, Christian Siebold, Anthony I. Magee, Thomas Lanyon-Hogg, Edward W. Tate   +18 more
core   +7 more sources

Hedgehog signalling is involved in acquired resistance to KRASG12C inhibitors in lung cancer cells [PDF]

Cell Death and Disease
Although KRASG12C inhibitors have shown promising activity in lung adenocarcinomas harbouring KRASG12C, acquired resistance to these therapies eventually occurs in most patients.
Chaeyoung Lee, Jawoon Yi, Jihwan Park, Byungyong Ahn, Young-Wook Won, JiHeung Jeon, Byung Ju Lee, Wha Ja Cho, Jeong Woo Park   +8 more
doaj   +2 more sources

Endocannabinoids are conserved inhibitors of the Hedgehog pathway [PDF]

Proceedings of the National Academy of Sciences, 2015
Significance Hedgehog proteins regulate development and tissue homeostasis. They signal through activation of the transmembrane protein Smoothened. Smoothened hyperactivation underlies development of many tumors. Smoothened activity can be modulated by several synthetic small molecules, which have shown promise in the clinic. However,
Khaliullina, H., Bilgin, M., Sampaio, J., Shevchenko, A., Eaton, S.   +4 more
openaire   +4 more sources

Synthesis and characterisation of 5-acyl-6,7-dihydrothieno[3,2-c]pyridine inhibitors of Hedgehog acyltransferase [PDF]

Data in Brief, 2016
In this data article we describe synthetic and characterisation data for four members of the 5-acyl-6,7-dihydrothieno[3,2-c]pyridine (termed “RU-SKI”) class of inhibitors of Hedgehog acyltransferase, including associated NMR spectra for final compounds ...
Thomas Lanyon-Hogg, Naoko Masumoto, George Bodakh, Antonio D. Konitsiotis, Emmanuelle Thinon, Ursula R. Rodgers, Raymond J. Owens, Anthony I. Magee, Edward W. Tate   +8 more
doaj   +2 more sources

Hedgehog pathway inhibitors – current status and future prospects

Infectious Agents and Cancer, 2012
The Hedgehog (Hh) proteins comprise a group of secreted proteins that regulate cell growth, differentiation and survival. Inappropriate activation of the Hh signaling pathway has been implicated in the development of a variety of cancers.
Sheikh Asfandyar, Alvi Arsalan, Aslam Hafiz, Haseeb Abdul   +3 more
doaj   +2 more sources

Clinical implications of hedgehog signaling pathway inhibitors

Chinese Journal of Cancer, 2011
Hedgehog was first described in Drosophila melanogaster by the Nobel laureates Eric Wieschaus and Christiane Nüsslein-Volhard. The hedgehog (Hh) pathway is a major regulator of cell differentiation, proliferation, tissue polarity, stem cell maintenance, and carcinogenesis.
Liu, Hailan, Gu, Dongsheng, Xie, Jingwu
openaire   +4 more sources

The role of Sulf1 during Sonic hedgehog mediated neural patterning [PDF]

, 2011
Heparan sulphate proteoglycans (HSPGs) are large molecules distributed ubiquitously, both at the cell surface and within the extracellular matrix. These molecules are known to play essential roles in developmental cell signalling, and the differential ...
Ramsbottom, Simon.A
core   +5 more sources

Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling [PDF]

Nature Chemical Biology, 2013
Inhibition of Sonic hedgehog (Shh) signaling is of great clinical interest. Here we exploit Hedgehog acyltransferase (Hhat)-mediated Shh palmitoylation, a modification critical for Shh signaling, as a new target for Shh pathway inhibition. A target-oriented high-throughput screen was used to identify small-molecule inhibitors of Hhat.
Petrova, Elissaveta, Rios-Esteves, Jessica, Ouerfelli, Ouathek, Glickman, J. Fraser, Resh, Marilyn D.   +4 more
openaire   +2 more sources

The dawn of hedgehog inhibitors: Vismodegib. [PDF]

J Pharmacol Pharmacother, 2013
Cancer, one of the leading causes of death worldwide is estimated to increase to approximately 13.1 million by 2030. This has amplified the research in oncology towards the exploration of novel targets. Recently there has been lots of interest regarding the hedgehog (Hh) pathway, which plays a significant role in the development of organs and tissues ...
Sandhiya S, Melvin G, Kumar SS, Dkhar SA.   +3 more
europepmc   +4 more sources

gatoravi/hedgehog-variability:

, 2022
v1.0.0 of the notebooks used in the hedgehog variability ...
Avinash R
core   +2 more sources