8PVR
 
 | | Cryo-EM structure of horse Nhe9 bound to PI(3,5)P2 | | Descriptor: | (2R)-3-{[(S)-hydroxy{[(1S,2R,3R,4S,5S,6R)-2,4,6-trihydroxy-3,5-bis(phosphonooxy)cyclohexyl]oxy}phosphoryl]oxy}propane-1,2-diyl dioctanoate, Sodium/hydrogen exchanger 9 | | Authors: | Kokane, S, Meier, P, Gulati, A, Delemotte, L, Drew, D. | | Deposit date: | 2023-07-18 | | Release date: | 2024-07-24 | | Method: | ELECTRON MICROSCOPY (3.06 Å) | | Cite: | PIP2 mediated oligomerization of the endosomal sodium/proton exchanger NHE9
To Be Published
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5FM2
 | | Crystal structure of hyper-phosphorylated RET kinase domain with (proximal) juxtamembrane segment | | Descriptor: | 1-TER-BUTYL-3-P-TOLYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET | | Authors: | Plaza-Menacho, I, Barnouin, K, Barry, R, Borg, A, Orme, M, Mouilleron, S, Martinez-Torres, R.J, Meier, P, McDonald, N.Q. | | Deposit date: | 2015-10-30 | | Release date: | 2016-12-28 | | Last modified: | 2019-04-24 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | RET Functions as a Dual-Specificity Kinase that Requires Allosteric Inputs from Juxtamembrane Elements.
Cell Rep, 17, 2016
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5FM3
 | | Crystal structure of hyper-phosphorylated RET kinase domain with (proximal) juxtamembrane segment | | Descriptor: | 1-TER-BUTYL-3-P-TOLYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET | | Authors: | Plaza-Menacho, I, Barnouin, K, Barry, R, Borg, A, Orme, M, Mouilleron, S, Martinez-Torres, R.J, Meier, P, McDonald, N.Q. | | Deposit date: | 2015-10-30 | | Release date: | 2016-12-28 | | Last modified: | 2019-04-24 | | Method: | X-RAY DIFFRACTION (2.95 Å) | | Cite: | RET Functions as a Dual-Specificity Kinase that Requires Allosteric Inputs from Juxtamembrane Elements.
Cell Rep, 17, 2016
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8PS0
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6Z3Y
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6Z3Z
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6DCG
 | | Discovery of MK-8353: An Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology | | Descriptor: | (3S)-3-(methylsulfanyl)-1-(2-{4-[4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]-3,6-dihydropyridin-1(2H)-yl}-2-oxoethyl)-N-(3-{6-[(propan-2-yl)oxy]pyridin-3-yl}-1H-indazol-5-yl)pyrrolidine-3-carboxamide, Mitogen-activated protein kinase 1, SULFATE ION | | Authors: | Boga, S.B, Deng, Y, Zhu, L, Nan, Y, Cooper, A, Shipps Jr, G.W, Doll, R, Shih, N, Zhu, H, Sun, R, Wang, T, Paliwal, S, Tsui, H, Gao, X, Yao, X, Desai, J, Wang, J, Alhassan, A.B, Kelly, J, Patel, M, Muppalla, K, Gudipati, S, Zhang, L, Buevich, A, Hesk, D, Carr, D, Dayananth, P, Mei, H, Cox, K, Sherborne, B, Hruza, A.W, Xiao, L, Jin, W, Long, B, Liu, G, Taylor, S.A, Kirschmeier, P, Windsor, W.T, Bishop, R, Samatar, A.A. | | Deposit date: | 2018-05-06 | | Release date: | 2018-08-08 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
ACS Med Chem Lett, 9, 2018
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4QYY
 | | Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase State | | Descriptor: | (3R)-1-{2-[4-(4-acetylphenyl)piperazin-1-yl]-2-oxoethyl}-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamide, Mitogen-activated protein kinase 1, SULFATE ION | | Authors: | Deng, Y, Shipps, G.W, Cooper, A, English, J.M, Annis, D.A, Carr, D, Nan, Y, Wang, T, Zhu, Y.H, Chuang, C, Dayananth, P, Hruza, A.W, Xiao, L, Jin, W, Kirschmeier, P, Windsor, W.T, Samatar, A.A. | | Deposit date: | 2014-07-26 | | Release date: | 2014-11-12 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase.
J.Med.Chem., 57, 2014
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3KSQ
 | | Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors | | Descriptor: | FARNESYL DIPHOSPHATE, Farnesyltransferase, CAAX box, ... | | Authors: | Zhu, H.Y, Cooper, A.B, Njoroge, G, Kirschmeier, P, Strickland, C, Hruza, A, Girijavallabhan, V.M. | | Deposit date: | 2009-11-23 | | Release date: | 2010-01-26 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Discovery of C-imidazole azaheptapyridine FPT inhibitors.
Bioorg.Med.Chem.Lett., 20, 2010
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7G1I
 | | Crystal Structure of human FABP4 in complex with 5-(4-chlorophenyl)-6-(2,2,2-trifluoroethoxy)-2-(trifluoromethyl)pyridine-3-carboxylic acid | | Descriptor: | 5-(4-chlorophenyl)-6-(2,2,2-trifluoroethoxy)-2-(trifluoromethyl)pyridine-3-carboxylic acid, Fatty acid-binding protein, adipocyte, ... | | Authors: | Ehler, A, Benz, J, Obst, U, Waldmeier, P, Rudolph, M.G. | | Deposit date: | 2023-04-27 | | Release date: | 2023-06-14 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.53 Å) | | Cite: | Crystal Structure of a human FABP4 complex
To be published
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