6UYB
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6uyb by Molmil](/molmil-images/mine/6uyb) | Crystal structure of TEAD2 bound to Compound 1 | Descriptor: | (3R,4R)-1-{3-[(E)-2-(4-chlorophenyl)ethenyl]-4-methoxy-5-methylphenyl}-3,4-dihydroxypyrrolidin-2-one, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, GLYCEROL, ... | Authors: | Noland, C.L, Holden, J.K, Crawford, J.J, Zbieg, J.R, Cunningham, C.N. | Deposit date: | 2019-11-12 | Release date: | 2020-06-24 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.543 Å) | Cite: | Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling. Cell Rep, 31, 2020
|
|
7TYP
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7typ by Molmil](/molmil-images/mine/7typ) | TEAD2 bound to GNE-7883 | Descriptor: | (8S)-5-(4-cyclohexylphenyl)-3-[3-(fluoromethyl)azetidine-1-carbonyl]-2-(3-methylpyrazin-2-yl)pyrazolo[1,5-a]pyrimidin-7(4H)-one, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Transcriptional enhancer factor TEF-4 | Authors: | Noland, C.L, Fong, R. | Deposit date: | 2022-02-14 | Release date: | 2023-05-03 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.6 Å) | Cite: | Novel mechanism of YAP-TEAD inhibition results in targeted chromatin remodeling and reveals an
expanded Hippo dependent landscape in cancers To Be Published
|
|
6UYC
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6uyc by Molmil](/molmil-images/mine/6uyc) | Crystal structure of TEAD2 bound to Compound 2 | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, N-{5-[(E)-2-(4,4-difluorocyclohexyl)ethenyl]-6-methoxypyridin-3-yl}methanesulfonamide, Transcriptional enhancer factor TEF-4 | Authors: | Noland, C.L, Holden, J.K, Crawford, J.J, Zbieg, J.R, Cunningham, C.N. | Deposit date: | 2019-11-12 | Release date: | 2020-06-24 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.658 Å) | Cite: | Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling. Cell Rep, 31, 2020
|
|
7TYU
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7tyu by Molmil](/molmil-images/mine/7tyu) | TEAD2 bound to Compound 2 | Descriptor: | (3R)-1-[(8S)-5-(4-cyclohexylphenyl)-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonyl]pyrrolidine-3-carbonitrile, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Transcriptional enhancer factor TEF-4 | Authors: | Noland, C.L, Fong, R. | Deposit date: | 2022-02-14 | Release date: | 2023-05-03 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.78 Å) | Cite: | Novel mechanism of YAP-TEAD inhibition results in targeted chromatin remodeling and reveals an
expanded Hippo dependent landscape in cancers To Be Published
|
|
7TYQ
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7tyq by Molmil](/molmil-images/mine/7tyq) | TEAD2 bound to Compound 1 | Descriptor: | Transcriptional enhancer factor TEF-4, ethyl (8S)-7-oxo-5-[4-(trifluoromethyl)phenyl]-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxylate | Authors: | Noland, C.L, Fong, R. | Deposit date: | 2022-02-14 | Release date: | 2023-05-03 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.88 Å) | Cite: | Novel mechanism of YAP-TEAD inhibition results in targeted chromatin remodeling and reveals an
expanded Hippo dependent landscape in cancers To Be Published
|
|
7OYJ
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7oyj by Molmil](/molmil-images/mine/7oyj) | |
8POM
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8pom by Molmil](/molmil-images/mine/8pom) | TEAD2 in complex with an inhibitor | Descriptor: | 2-[[3-(2-phenylethoxy)phenyl]amino]pyridine-3-carboxylic acid, GLYCEROL, Transcriptional enhancer factor TEF-4 | Authors: | Guichou, J.F. | Deposit date: | 2023-07-05 | Release date: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings. Bioorg.Med.Chem.Lett., 95, 2023
|
|
3L15
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 3l15 by Molmil](/molmil-images/mine/3l15) | Human Tead2 transcriptional factor | Descriptor: | GLYCEROL, Transcriptional enhancer factor TEF-4 | Authors: | Tomchick, D.R, Luo, X, Tian, W. | Deposit date: | 2009-12-10 | Release date: | 2010-04-07 | Last modified: | 2017-11-01 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Structural and functional analysis of the YAP-binding domain of human TEAD2. Proc.Natl.Acad.Sci.USA, 107, 2010
|
|
6S60
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6s60 by Molmil](/molmil-images/mine/6s60) | Crystal structure of hTEAD2 in complex with a trisubstituted pyrazole inhibitor | Descriptor: | 4-[3-(3,4-dichlorophenyl)-4-[(phenylmethyl)carbamoyl]pyrazol-1-yl]butanoic acid, MYRISTIC ACID, Transcriptional enhancer factor TEF-4 | Authors: | Sturbaut, M, Allemand, F, Guichou, J.F. | Deposit date: | 2019-07-02 | Release date: | 2020-07-22 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Discovery of a cryptic site at the interface 2 of TEAD - Towards a new family of YAP/TAZ-TEAD inhibitors. Eur.J.Med.Chem., 226, 2021
|
|
5EMV
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5emv by Molmil](/molmil-images/mine/5emv) | Crystal structure of the palmitoylated human TEAD2 transcription factor | Descriptor: | Transcriptional enhancer factor TEF-4 | Authors: | Noland, C.L, Gierke, S, Schnier, P.D, Murray, J, Sandoval, W.N, Sagolla, M, Dey, A, Hannoush, R.N, Fairbrother, W.J, Cunningham, C.N. | Deposit date: | 2015-11-06 | Release date: | 2015-12-23 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Palmitoylation of TEAD Transcription Factors Is Required for Their Stability and Function in Hippo Pathway Signaling. Structure, 24, 2016
|
|
5HGU
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5hgu by Molmil](/molmil-images/mine/5hgu) | |
8PUX
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8pux by Molmil](/molmil-images/mine/8pux) | TEAD2 with a covalent inhibitor | Descriptor: | MYRISTIC ACID, Transcriptional enhancer factor TEF-4, ~{N}-[2-[(3-pentoxyphenyl)amino]phenyl]propanamide | Authors: | Guichou, J.F, Gelin, M, Allemand, F. | Deposit date: | 2023-07-17 | Release date: | 2023-12-13 | Last modified: | 2024-01-03 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Development of HC-258, a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. Acs Med.Chem.Lett., 14, 2023
|
|
8P29
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8p29 by Molmil](/molmil-images/mine/8p29) | TEAD2 in complex with an inhibitor | Descriptor: | 5-methyl-2-[(3-phenylmethoxyphenyl)amino]benzoic acid, GLYCEROL, MYRISTIC ACID, ... | Authors: | Guichou, J.F, Gelin, M, Allemand, F. | Deposit date: | 2023-05-15 | Release date: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.06 Å) | Cite: | Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings. Bioorg.Med.Chem.Lett., 95, 2023
|
|
6S6J
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6s6j by Molmil](/molmil-images/mine/6s6j) | Crystal structure of hTEAD2 in complex with a trisubstituted pyrazole inhibitor | Descriptor: | MYRISTIC ACID, Transcriptional enhancer factor TEF-4, ethyl 1-(4-azanylbutyl)-3-(3,4-dichlorophenyl)pyrazole-4-carboxylate | Authors: | Sturbaut, M, Allemand, F, Guichou, J.F. | Deposit date: | 2019-07-03 | Release date: | 2020-07-22 | Last modified: | 2022-02-02 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Discovery of a cryptic site at the interface 2 of TEAD - Towards a new family of YAP/TAZ-TEAD inhibitors. Eur.J.Med.Chem., 226, 2021
|
|
6VAH
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6vah by Molmil](/molmil-images/mine/6vah) | Crystal structure of human TEAD2 transcription factor in complex with Flufenamic acid derivative | Descriptor: | 2-fluoro-6-[(3-hexylphenyl)amino]benzoic acid, Transcriptional enhancer factor TEF-4, UNKNOWN ATOM OR ION | Authors: | Halabelian, L, Zeng, H, Dong, A, Li, Y, Melin, L, Gagnon, A, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Santhakumar, V, Structural Genomics Consortium (SGC) | Deposit date: | 2019-12-17 | Release date: | 2020-04-15 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.11 Å) | Cite: | Crystal structure of human TEAD2 transcription factor in complex with Flufenamic acid derivative to be published
|
|
7T2L
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7t2l by Molmil](/molmil-images/mine/7t2l) | Crystal Structure of TEAD2 in a covalent complex with TED-662 | Descriptor: | (3aR,4R,7aS)-4-[3-(trifluoromethyl)anilino]octahydro-2H-isoindole-2-carbonitrile, Transcriptional enhancer factor TEF-4 | Authors: | Bum-Erdene, K, Gonzalez-Gutierrez, G, Meroueh, S.O. | Deposit date: | 2021-12-05 | Release date: | 2023-06-14 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (2.15 Å) | Cite: | Small-Molecule Cyanamide Pan-TEAD·YAP1 Covalent Antagonists. J.Med.Chem., 66, 2023
|
|
6S69
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6s69 by Molmil](/molmil-images/mine/6s69) | Crystal structure of hTEAD2 in complex with a trisubstituted pyrazole inhibitor | Descriptor: | 3-[3-(3,4-dichlorophenyl)-4-(2-phenylethylcarbamoyl)pyrazol-1-yl]propanoic acid, MYRISTIC ACID, Transcriptional enhancer factor TEF-4 | Authors: | Sturbaut, M, Allemand, F, Guichou, J.F. | Deposit date: | 2019-07-02 | Release date: | 2020-07-22 | Last modified: | 2022-02-02 | Method: | X-RAY DIFFRACTION (2.15 Å) | Cite: | Discovery of a cryptic site at the interface 2 of TEAD - Towards a new family of YAP/TAZ-TEAD inhibitors. Eur.J.Med.Chem., 226, 2021
|
|
5DQE
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5dqe by Molmil](/molmil-images/mine/5dqe) | |
8PUY
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8puy by Molmil](/molmil-images/mine/8puy) | TEAD2 with a covalent inhibitor | Descriptor: | MYRISTIC ACID, Transcriptional enhancer factor TEF-4, ~{N}-[3-[(3-pentoxyphenyl)amino]phenyl]propanamide | Authors: | Guichou, J.F, Gelin, M, Allemand, F. | Deposit date: | 2023-07-17 | Release date: | 2023-12-13 | Last modified: | 2024-01-03 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Development of HC-258, a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. Acs Med.Chem.Lett., 14, 2023
|
|
6S66
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6s66 by Molmil](/molmil-images/mine/6s66) | Crystal structure of hTEAD2 in complex with a trisubstituted pyrazole inhibitor | Descriptor: | 1-(2-azanylethyl)-3-(3,4-dichlorophenyl)-~{N}-(phenylmethyl)pyrazole-4-carboxamide, MYRISTIC ACID, Transcriptional enhancer factor TEF-4 | Authors: | Sturbaut, M, Allemand, F, Guichou, J.F. | Deposit date: | 2019-07-02 | Release date: | 2020-07-22 | Last modified: | 2022-02-02 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Discovery of a cryptic site at the interface 2 of TEAD - Towards a new family of YAP/TAZ-TEAD inhibitors. Eur.J.Med.Chem., 226, 2021
|
|
8PON
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8pon by Molmil](/molmil-images/mine/8pon) | TEAD2 in complex with an inhibitor | Descriptor: | 4-fluoranyl-2-[(3-phenylmethoxyphenyl)amino]benzoic acid, MYRISTIC ACID, Transcriptional enhancer factor TEF-4 | Authors: | Guichou, J.F. | Deposit date: | 2023-07-05 | Release date: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings. Bioorg.Med.Chem.Lett., 95, 2023
|
|
6S64
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6s64 by Molmil](/molmil-images/mine/6s64) | Crystal structure of hTEAD2 in complex with a trisubstituted pyrazole inhibitor | Descriptor: | 3-[3-(3,4-dichlorophenyl)-4-[(phenylmethyl)carbamoyl]pyrazol-1-yl]propanoic acid, MYRISTIC ACID, PALMITIC ACID, ... | Authors: | Sturbaut, M, Allemand, F, Guichou, J.F. | Deposit date: | 2019-07-02 | Release date: | 2020-07-22 | Last modified: | 2022-02-02 | Method: | X-RAY DIFFRACTION (2.22 Å) | Cite: | Discovery of a cryptic site at the interface 2 of TEAD - Towards a new family of YAP/TAZ-TEAD inhibitors. Eur.J.Med.Chem., 226, 2021
|
|
8E1O
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8e1o by Molmil](/molmil-images/mine/8e1o) | Crystal structure of hTEAD2 bound to a methoxypyridine lipid pocket binder | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 5-methoxy-N-({3-[2-(methylamino)-2-oxoethyl]phenyl}methyl)-4-{(E)-2-[trans-4-(trifluoromethyl)cyclohexyl]ethenyl}pyridine-2-carboxamide, Transcriptional enhancer factor TEF-4 | Authors: | Noland, C.L, Dey, A, Zbieg, J, Crawford, J. | Deposit date: | 2022-08-10 | Release date: | 2023-08-16 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.25 Å) | Cite: | Targeting the Hippo pathway in cancers via ubiquitination dependent TEAD degradation Biorxiv, 2024
|
|
5DQ8
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5dq8 by Molmil](/molmil-images/mine/5dq8) | |
6CDY
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6cdy by Molmil](/molmil-images/mine/6cdy) | Crystal structure of TEAD complexed with its inhibitor | Descriptor: | 2-[(4H-1,2,4-triazol-3-yl)sulfanyl]-N-{4-[(3s,5s,7s)-tricyclo[3.3.1.1~3,7~]decan-1-yl]phenyl}acetamide, Transcriptional enhancer factor TEF-4 | Authors: | LIU, S, HAN, X, LUO, X. | Deposit date: | 2018-02-09 | Release date: | 2020-07-01 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.32 Å) | Cite: | Lats1/2 Sustain Intestinal Stem Cells and Wnt Activation through TEAD-Dependent and Independent Transcription. Cell Stem Cell, 26, 2020
|
|