α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).
α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).
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DOI：
10.1021/acs.jmedchem.6b01166
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发表时间：
2017-02-23
影响因子：
7.3
通讯作者：
Frédérick R
中科院分区：
文献类型：
--
作者：
Ravez S;Corbet C;Spillier Q;Dutu A;Robin AD;Mullarky E;Cantley LC;Feron O;Frédérick R
鉴于PHGDH在癌症中的假定作用，需要开发抑制剂来探索其功能。在这种情况下，我们建立并验证了一个简单的酶法适用于高通量筛选，我们确定了类似的化学支架的抑制剂。通过会聚药效团方法，我们合成了α-酮硫代酰胺，其表现出有趣的体外PHGDH抑制和令人鼓舞的细胞结果。这些新的探针可用于了解这种代谢靶点的新兴生物学。
Given the putative role of PHGDH in cancer, development of inhibitors is required to explore its function. In this context, we established and validated a straightforward enzymatic assay suitable for high-throughput screening and we identified inhibitors with similar chemical scaffolds. Through a convergent pharmacophore approach, we synthesized α-ketothioamides that exhibit interesting in vitro PHGDH inhibition and encouraging cellular results. These novel probes may be used to understand the emerging biology of this metabolic target.
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影响因子：
14.8
作者：
Pacold ME;Brimacombe KR;Chan SH;Rohde JM;Lewis CA;Swier LJ;Possemato R;Chen WW;Sullivan LB;Fiske BP;Cho S;Freinkman E;Birsoy K;Abu-Remaileh M;Shaul YD;Liu CM;Zhou M;Koh MJ;Chung H;Davidson SM;Luengo A;Wang AQ;Xu X;Yasgar A;Liu L;Rai G;Westover KD;Vander Heiden MG;Shen M;Gray NS;Boxer MB;Sabatini DM
通讯作者：
Sabatini DM
PHGDH表达的增加和结直肠癌的预后意义。
影响因子：
5
作者：
Jia XQ;Zhang S;Zhu HJ;Wang W;Zhu JH;Wang XD;Qiang JF
通讯作者：
Qiang JF
影响因子：
64.8
作者：
Possemato, Richard;Marks, Kevin M.;Shaul, Yoav D.;Pacold, Michael E.;Kim, Dohoon;Birsoy, Kivanc;Sethumadhavan, Shalini;Woo, Hin-Koon;Jang, Hyun G.;Jha, Abhishek K.;Chen, Walter W.;Barrett, Francesca G.;Stransky, Nicolas;Tsun, Zhi-Yang;Cowley, Glenn S.;Barretina, Jordi;Kalaany, Nada Y.;Hsu, Peggy P.;Ottina, Kathleen;Chan, Albert M.;Yuan, Bingbing;Garraway, Levi A.;Root, David E.;Mino-Kenudson, Mari;Brachtel, Elena F.;Driggers, Edward M.;Sabatini, David M.
通讯作者：
Sabatini, David M.
影响因子：
4.1
作者：
Bolton, JL;Trush, MA;Monks, TJ
通讯作者：
Monks, TJ
磷酸甘油酸脱氢酶通过稳定叉头盒M1诱导胶质瘤细胞增殖和侵袭
影响因子：
3.9
作者：
Liu, Jinlong;Guo, Shaolei;Li, Qingzhi;Yang, Lixuan;Xia, Zhibai;Zhang, Longjuan;Huang, Zhengsong;Zhang, Nu
通讯作者：
Zhang, Nu