Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase
Steffi Koerner
1
,
Sha Bai
1
,
Finith E Jernigan
1
,
Miwa Oki
2
,
Chieko Komaba
2
,
Emi Shuto
2
,
Vikas P. Sukhatme
3
,
Lijun Sun
1
1
2
Publication type: Journal Article
Publication date: 2017-01-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
27997879
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
Aberrant cellular metabolism drives cancer proliferation and metastasis. ATP citrate lyase (ACL) plays a critical role in generating cytosolic acetyl CoA, a key building block for de novo fatty acid and cholesterol biosynthesis. ACL is overexpressed in cancer cells, and siRNA knockdown of ACL limits cancer cell proliferation and reduces cancer stemness. We characterized a new class of ACL inhibitors bearing the key structural feature of the natural product emodin. Structure-activity relationship (SAR) study led to the identification of 1d as a potent lead that demonstrated dose-dependent inhibition of proliferation and cancer stemness of the A549 lung cancer cell line. Computational modeling indicates this class of inhibitors occupies an allosteric binding site and blocks the entrance of the substrate citrate to its binding site.
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75
Total citations:
75
Citations from 2024:
19
(25.34%)
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GOST
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Koerner S. et al. Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase // European Journal of Medicinal Chemistry. 2017. Vol. 126. pp. 920-928.
GOST all authors (up to 50)
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Koerner S., Bai S., Jernigan F. E., Oki M., Komaba C., Shuto E., Sukhatme V. P., Sun L. Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase // European Journal of Medicinal Chemistry. 2017. Vol. 126. pp. 920-928.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.ejmech.2016.12.018
UR - https://doi.org/10.1016/j.ejmech.2016.12.018
TI - Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase
T2 - European Journal of Medicinal Chemistry
AU - Koerner, Steffi
AU - Bai, Sha
AU - Jernigan, Finith E
AU - Oki, Miwa
AU - Komaba, Chieko
AU - Shuto, Emi
AU - Sukhatme, Vikas P.
AU - Sun, Lijun
PY - 2017
DA - 2017/01/01
PB - Elsevier
SP - 920-928
VL - 126
PMID - 27997879
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2017_Koerner,
author = {Steffi Koerner and Sha Bai and Finith E Jernigan and Miwa Oki and Chieko Komaba and Emi Shuto and Vikas P. Sukhatme and Lijun Sun},
title = {Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase},
journal = {European Journal of Medicinal Chemistry},
year = {2017},
volume = {126},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/j.ejmech.2016.12.018},
pages = {920--928},
doi = {10.1016/j.ejmech.2016.12.018}
}