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Akademický článek

A functional genetic screen for metabolic proteins unveils GART and the de novo purine biosynthetic pathway as novel targets for the treatment of luminal A ERα expressing primary and metastatic invasive ductal carcinoma

Autor: Manuela Cipolletti, Stefano Leone, Stefania Bartoloni, Filippo Acconcia

Publikováno v: Frontiers in Endocrinology, Vol 14 (2023)

Targeting tumor cell metabolism is a new frontier in cancer management. Thus, metabolic pathway inhibitors could be used as anti-estrogen receptor α (ERα) breast cancer (BC) drugs. Here, the interplay among metabolic enzyme(s), the ERα levels and

Externí odkaz: https://doaj.org/article/6fbaa480676e46818e890cb7a3b8aa3f

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Molecular mechanism of c‐Myc and PRPS1/2 against thiopurine resistance in Burkitt's lymphoma

Autor: Yali Han, Yingwen Zhang, Yanxin Li, Lili Song, Yang Li, Zhou Xv, Shanshan Li, Yi Yang, Liang Zheng, Ting Li, Zhiyan Zhan, Yuejia Tang, Yijin Gao, Siqi wang

Publikováno v: Journal of Cellular and Molecular Medicine

Patients with relapsed/refractory Burkitt's lymphoma (BL) have a dismal prognosis. Current research efforts aim to increase cure rates by identifying high‐risk patients in need of more intensive or novel therapy. The 8q24 chromosomal translocation

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4af100e0e599d7362584aa2780be06f2
http://europepmc.org/articles/PMC7299692

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Akademický článek

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Akademický článek

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Structural basis of inhibition of the human serine hydroxymethyltransferase SHMT2 by antifolate drugs

Autor: Thomas Helleday, Ann-Sofie Jemth, Emma Rose Scaletti, Pål Stenmark

Publikováno v: FEBS letters. 593(14)

Serine hydroxymethyltransferase (SHMT) is the major source of 1-carbon units required for nucleotide synthesis. Humans have cytosolic (SHMT1) and mitochondrial (SHMT2) isoforms, which are upregulated in numerous cancers, making the enzyme an attracti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81d3b50cc2f43423dec7431314d1f0ad
https://pubmed.ncbi.nlm.nih.gov/31127856

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10-(2-Benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid

Autor: Kevin Capps, Michael P. Hedrick, Stephen J. Benkovic, Ali Tavassoli, Dale L. Boger, Ian A. Wilson, Yan Zhang, Joel Desharnais, Thomas H. Marsilje

Publikováno v: Bioorganic & Medicinal Chemistry. 11:4503-4509

The design and synthesis of 10-(2-benzoxazolcarbonyl)-DDACTHF (1) as an inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. Ketone 1 and the corresponding alcoho

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::eb1b1c7bafda71862c1f28c06ed5ba2c
https://doi.org/10.1016/s0968-0896(03)00457-7

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Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway

Autor: Justin Baboval, Inkyu Hwang, Dale L. Boger, Joel Desharnais, Ian A. Wilson, Stephen J. Benkovic, Yan Zhang, Ali Tavassoli

Publikováno v: Bioorganic & Medicinal Chemistry. 11:4511-4521

The synthesis and evaluation of analogues and key derivatives of 10-CF 3 CO-DDACTHF as inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. Polyglutamate analogu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b9fed467b4cf7b4ab05df1985b94513
https://doi.org/10.1016/s0968-0896(03)00458-9

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Design, synthesis, and biological evaluation of simplified α-Keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase

Autor: Yan Zhang, Ali Tavassoli, Thomas H. Marsilje, Michael P. Hedrick, Ian A. Wilson, Stephen J. Benkovic, Joel Desharnais, Dale L. Boger

Publikováno v: Bioorganic & Medicinal Chemistry. 11:4487-4501

A series of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues lacking the benzoylglutamate subunit were prepared and examined as potential inhibitors of glycinamide ribonucleotide transformylase (GAR T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1e631196a9af7128711f15b006dbacf
https://doi.org/10.1016/s0968-0896(03)00456-5

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Novel antifolate drugs

Autor: David S. Ettinger, W. Thomas Purcell

Publikováno v: Current Oncology Reports. 5:114-125

Antimetabolites are active chemotherapeutic agents for many solid tumor and hematologic malignancies. Folate antagonists, purine analogues, and pyrimidine analogues are the three main categories of antimetabolites. Methotrexate, the most studied fola

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13fc06c203bb377f3155a21e768bb37a
https://doi.org/10.1007/s11912-003-0098-3

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