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21 hits

Bibliografisk träff 2023-09-28

Targeting the Subpocket Enables the Discovery of Thiadiazole-Pyridazine Derivatives as Glutaminase C Inhibitors.

Sun H, Du T, Yang M, Liu X, Xue X, Chen K, Lang X, Chen X, Wang B, Wang X.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.3c00375

Bibliografisk träff 2023-05-03

Diselenide Covalent Allosteric Inhibitors of Glutaminase with Strong <i>In Vivo</i> Anticancer Activity.

Hou W, Chen Z, Pan C, Ni M, Ruan H, Song J, Lu S, Bhasin A, Ruan BH.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.2c00470

Bibliografisk träff 2023-03-23

Targeting glutaminase 1 (GLS1) by small molecules for anticancer therapeutics.

Chen Y, Tan L, Gao J, Lin C, Wu F, Li Y, Zhang J.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2023.115306

Bibliografisk träff 2022-12-22

Synthesis of Novel Kidney-Type Glutaminase Allosteric Inhibitors Targeting the Critical Lys-320 Residue.

Song J, Pan C, Li J, Bai R, Zeng Z, Han Y, Chen Z, Hou W, Li Y, Ruan BH.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.2c00302

Bibliografisk träff 2022-12-12

Design, synthesis, and biological evaluation of novel glutaminase 1 allosteric inhibitors with an alkane chain tail group.

Chang X, Wang M, Zhang D, Zhang Y, Wang J, Li Z, Bian J, Xu X.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.115014

Bibliografisk träff 2022-08-28

Novel allosteric glutaminase 1 inhibitors with macrocyclic structure activity relationship analysis.

Lee EJ, Duggirala KB, Lee Y, Yun MR, Jang J, Cyriac R, Jung ME, Choi G, Chae CH, Cho BC, Lee K.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2022.128956

Bibliografisk träff 2022-04-06

Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles.

Xu X, Chang X, Huang J, Zhang D, Wang M, Jing T, Zhuang Y, Kou J, Qiu Z, Wang J, Li Z, Bian J.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114337

Bibliografisk träff 2022-03-06

Metabolomics-assisted discovery of a new anticancer GLS-1 inhibitor chemotype from a nortopsentin-inspired library: From phenotype screening to target identification.

Carbone D, Vestuto V, Ferraro MR, Ciaglia T, Pecoraro C, Sommella E, Cascioferro S, Salviati E, Novi S, Tecce MF, Amodio G, Iraci N, Cirrincione G, Campiglia P, Diana P, Bertamino A, Parrino B, Ostacolo C.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114233

Bibliografisk träff 2021-04-01

Structure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site.

Xu X, Wang J, Wang M, Yuan X, Li L, Zhang C, Huang H, Jing T, Wang C, Tong C, Zhou L, Meng Y, Xu P, Kou J, Qiu Z, Li Z, Bian J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c02044

Bibliografisk träff 2021-03-02

Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.

Liao M, Zhang J, Wang G, Wang L, Liu J, Ouyang L, Liu B.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.0c01180

Bibliografisk träff 2020-10-29

Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.

Soth MJ, Le K, Di Francesco ME, Hamilton MM, Liu G, Burke JP, Carroll CL, Kovacs JJ, Bardenhagen JP, Bristow CA, Cardozo M, Czako B, de Stanchina E, Feng N, Garvey JR, Gay JP, Do MKG, Greer J, Han M, Harris A, Herrera Z, Huang S, Giuliani V, Jiang Y, Johnson SB, Johnson TA, Kang Z, Leonard PG, Liu Z, McAfoos T, Miller M, Morlacchi P, Mullinax RA, Palmer WS, Pang J, Rogers N, Rudin CM, Shepard HE, Spencer ND, Theroff J, Wu Q, Xu A, Yau JA, Draetta G, Toniatti C, Heffernan TP, Jones P.

J Med Chem · research-article; journal article · DOI 10.1021/acs.jmedchem.0c01398

Bibliografisk träff 2020-08-06

Allosteric kidney-type glutaminase (GLS) inhibitors with a mercaptoethyl linker.

Duvall B, Zimmermann SC, Gao RD, Thomas AG, Kalčic F, Veeravalli V, Elgogary A, Rais R, Rojas C, Le A, Slusher BS, Tsukamoto T.

Bioorg Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2020.115698

Bibliografisk träff 2019-10-24

Development and Characterization of a Fluorescent Probe for GLS1 and the Application for High-Throughput Screening of Allosteric Inhibitors.

Xu X, Kuang Z, Han J, Meng Y, Li L, Luan H, Xu P, Wang J, Luo C, Ding H, Li Z, Bian J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.9b01035

Bibliografisk träff 2019-07-16

Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.

Finlay MRV, Anderton M, Bailey A, Boyd S, Brookfield J, Cairnduff C, Charles M, Cheasty A, Critchlow SE, Culshaw J, Ekwuru T, Hollingsworth I, Jones N, Leroux F, Littleson M, McCarron H, McKelvie J, Mooney L, Nissink JWM, Perkins D, Powell S, Quesada MJ, Raubo P, Sabin V, Smith J, Smith PD, Stark A, Ting A, Wang P, Wilson Z, Winter-Holt JJ, Wood JM, Wrigley GL, Yu G, Zhang P.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.9b00260

Bibliografisk träff 2018-12-31

Novel 1,3,4-Selenadiazole-Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity.

Chen Z, Li D, Xu N, Fang J, Yu Y, Hou W, Ruan H, Zhu P, Ma R, Lu S, Cao D, Wu R, Ni M, Zhang W, Su W, Ruan BH.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b01198

Bibliografisk träff 2018-11-28

Discovery and development of small molecule modulators targeting glutamine metabolism.

Li L, Meng Y, Li Z, Dai W, Xu X, Bi X, Bian J.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2018.11.066

Bibliografisk träff 2018-09-07

Overview of the Development of Glutaminase Inhibitors: Achievements and Future Directions.

Xu X, Meng Y, Li L, Xu P, Wang J, Li Z, Bian J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b00961

Bibliografisk träff 2018-07-03

Recent Progress in the Discovery of Allosteric Inhibitors of Kidney-Type Glutaminase.

Zimmermann SC, Duvall B, Tsukamoto T.

J Med Chem · research support, non-u.s. gov't; research-article; review; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.8b00327

Bibliografisk träff 2017-01-21

Physapubescin, a natural withanolide as a kidney-type glutaminase (KGA) inhibitor.

Cheng L, Wu CR, Zhu LH, Li H, Chen LX.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2017.01.057

Bibliografisk träff 2016-03-13

Allosteric Glutaminase Inhibitors Based on a 1,4-Di(5-amino-1,3,4-thiadiazol-2-yl)butane Scaffold.

Zimmermann SC, Wolf EF, Luu A, Thomas AG, Stathis M, Poore B, Nguyen C, Le A, Rojas C, Slusher BS, Tsukamoto T.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.6b00060

Bibliografisk träff 2016-03-07

Design and evaluation of novel glutaminase inhibitors.

McDermott LA, Iyer P, Vernetti L, Rimer S, Sun J, Boby M, Yang T, Fioravanti M, O'Neill J, Wang L, Drakes D, Katt W, Huang Q, Cerione R.

Bioorg Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2016.03.009