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pro vyhledávání: '"M. Kyle Hadden"'
Autor:
Jiachen Wen, M. Kyle Hadden
Publikováno v:
European journal of medicinal chemistry. 228
Vitamin D3 (VD3) is a seco-steroid that inhibits the Hedgehog (Hh) signaling pathway. Initial studies suggested its anti-Hh activity results from direct inhibition of Smoothened, a seven-transmembrane cell surface receptor that is a key regulator of
Publikováno v:
European Journal of Medicinal Chemistry. 162:495-506
The Hedgehog (Hh) pathway is a developmental pathway with therapeutic potential as a target for a variety of cancers. In recent years, several vitamin D-based compounds have been identified as potent inhibitors of Hh signaling. These analogues contai
Publikováno v:
Molecular and Cellular Biochemistry. 450:75-85
Calcitriol, vitamin D3 (VD3), and structurally related VD3 analogues are inhibitors of Hh signaling in multiple contexts and are promising anti-cancer agents in Hh-dependent forms of cancer; however, the cellular mechanisms through which these compou
Autor:
M. Kyle Hadden, Jiachen Wen
Publikováno v:
ChemMedChem. 13:748-753
The Hedgehog (Hh) signaling pathway is critical for embryonic patterning and postembryonic tissue regeneration. Constitutive pathway activation has also been linked to human malignancies such as basal cell carcinoma (BCC) and medulloblastoma; therefo
Autor:
Upasana Banerjee, Daniel J. Madden, Vibhavari Sail, M. Kyle Hadden, Daniel De Carlo, Adam Meares, Steven Lemieux, Albert M. DeBerardinis, Daniel S. Raccuia
Publikováno v:
Journal of Medicinal Chemistry. 57:3724-3736
A structure-activity relationship study for a series of vitamin D3-based (VD3) analogues that incorporate aromatic A-ring mimics with varying functionality has provided key insight into scaffold features that result in potent, selective Hedgehog (Hh)
Autor:
M. Kyle Hadden
The classic physiological activity associated with the vitamin D scaffold is the maintenance of calcium and phosphorous homeostasis in the bone. This activity is commonly attributed to direct binding of 1α,25-dihydroxyvitamin D3 [1α,25(OH)2D3, calc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1cdf43e2c2bd97a856a92a6e0ff0a649
https://doi.org/10.1016/bs.vh.2015.10.006
https://doi.org/10.1016/bs.vh.2015.10.006
Publikováno v:
Bioorganicmedicinal chemistry. 23(3)
Vitamin D3 (VD3) is a moderately potent and non-selective inhibitor of the Hedgehog (Hh) signaling cascade. Previous studies have established that the CD-ring region of VD3 serves as the Hh inhibitory pharmacophore. Subsequently, compound 3, an ester
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(19)
The anti-proliferative activity of a series of ester- and amide-linked Inhoffen–Lythgoe side chain analogues is reported. Whereas the Inhoffen–Lythgoe diol was inactive in these studies, a number of aromatic and aliphatic ester-linked side chains
Publikováno v:
ACS medicinal chemistry letters. 4(7)
Previous structure-activity relationship studies for vitamin D3 (VD3) inhibition of Hedgehog (Hh) signaling directed the design, synthesis, and evaluation of a series of VD3-based analogues that contain an aromatic A-ring mimic. Characterization of t
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(3)
A structure-activity relationship study focusing on the A-ring of vitamin D3 (VD3) was undertaken to elucidate its role in inhibiting the Hedgehog pathway and in mediating anti-cancer effects. Analogues resulting from simple functional group substitu