8GZC
Crystal structure of EP300 HAT domain in complex with compound 10
Summary for 8GZC
Entry DOI | 10.2210/pdb8gzc/pdb |
Descriptor | Histone acetyltransferase p300, ZINC ION, (2~{R},4~{R})-4-fluoranyl-1-[1-(4-methoxyphenyl)cyclohexyl]carbonyl-~{N}-(1~{H}-pyrazolo[4,3-b]pyridin-5-yl)pyrrolidine-2-carboxamide, ... (4 entities in total) |
Functional Keywords | epigenetics, sbdd, histone acetyltransferase, transferase |
Biological source | Homo sapiens (human) More |
Total number of polymer chains | 2 |
Total formula weight | 106134.95 |
Authors | Takahashi, M.,Hanzawa, H. (deposition date: 2022-09-26, release date: 2023-01-11, Last modification date: 2023-11-29) |
Primary citation | Kanada, R.,Kagoshima, Y.,Suzuki, T.,Nakamura, A.,Funami, H.,Watanabe, J.,Asano, M.,Takahashi, M.,Ubukata, O.,Suzuki, K.,Aikawa, T.,Sato, K.,Goto, M.,Setsu, G.,Ito, K.,Kihara, K.,Kuroha, M.,Kohno, T.,Ogiwara, H.,Isoyama, T.,Tominaga, Y.,Higuchi, S.,Naito, H. Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor. J.Med.Chem., 66:695-715, 2023 Cited by PubMed: 36572866DOI: 10.1021/acs.jmedchem.2c01641 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2 Å) |
Structure validation
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