- PDB-5nne: Crystal Structure of the first bromodomain of human BRD4 in compl... -
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基本情報
登録情報
データベース: PDB / ID: 5nne
タイトル
Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated TOP2A peptide (K1201ac/K1204ac)
要素
Bromodomain-containing protein 4
GKA(ALY)GK(ALY)TQMY
キーワード
TRANSCRIPTION / Bromodomain / complex
機能・相同性
機能・相同性情報
apoptotic chromosome condensation / positive regulation of single stranded viral RNA replication via double stranded DNA intermediate / sister chromatid segregation / resolution of meiotic recombination intermediates / female meiotic nuclear division / DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complex / embryonic cleavage / DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activity / Transcription of E2F targets under negative control by DREAM complex / DNA binding, bending ...apoptotic chromosome condensation / positive regulation of single stranded viral RNA replication via double stranded DNA intermediate / sister chromatid segregation / resolution of meiotic recombination intermediates / female meiotic nuclear division / DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complex / embryonic cleavage / DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activity / Transcription of E2F targets under negative control by DREAM complex / DNA binding, bending / DNA topoisomerase (ATP-hydrolysing) / RNA polymerase II C-terminal domain binding / DNA topological change / P-TEFb complex binding / negative regulation of DNA damage checkpoint / SUMOylation of DNA replication proteins / chromosome, centromeric region / host-mediated suppression of viral transcription / ATP-dependent activity, acting on DNA / positive regulation of T-helper 17 cell lineage commitment / hematopoietic progenitor cell differentiation / condensed chromosome / positive regulation of G2/M transition of mitotic cell cycle / RNA polymerase II CTD heptapeptide repeat kinase activity / : / protein kinase C binding / male germ cell nucleus / histone reader activity / condensed nuclear chromosome / ubiquitin binding / chromosome segregation / transcription coregulator activity / positive regulation of transcription elongation by RNA polymerase II / regulation of circadian rhythm / p53 binding / rhythmic process / chromosome / chromatin organization / regulation of inflammatory response / histone binding / Potential therapeutics for SARS / transcription coactivator activity / positive regulation of canonical NF-kappaB signal transduction / transcription cis-regulatory region binding / positive regulation of apoptotic process / chromatin remodeling / protein heterodimerization activity / ribonucleoprotein complex / protein serine/threonine kinase activity / DNA damage response / chromatin binding / regulation of transcription by RNA polymerase II / chromatin / positive regulation of DNA-templated transcription / nucleolus / enzyme binding / magnesium ion binding / protein homodimerization activity / positive regulation of transcription by RNA polymerase II / protein-containing complex / DNA binding / RNA binding / nucleoplasm / ATP binding / nucleus / cytoplasm 類似検索 - 分子機能
DTHCT / DTHCT (NUC029) region / DNA topoisomerase 2, TOPRIM domain / C-terminal associated domain of TOPRIM / C-terminal associated domain of TOPRIM / DNA topoisomerase II, eukaryotic-type / : / Topoisomerase (Topo) IIA-type catalytic domain profile. / DNA topoisomerase, type IIA, alpha-helical domain superfamily / DNA topoisomerase, type IIA, domain A ...DTHCT / DTHCT (NUC029) region / DNA topoisomerase 2, TOPRIM domain / C-terminal associated domain of TOPRIM / C-terminal associated domain of TOPRIM / DNA topoisomerase II, eukaryotic-type / : / Topoisomerase (Topo) IIA-type catalytic domain profile. / DNA topoisomerase, type IIA, alpha-helical domain superfamily / DNA topoisomerase, type IIA, domain A / DNA topoisomerase, type IIA, domain A, alpha-beta / DNA gyrase/topoisomerase IV, subunit A / DNA Topoisomerase IV / DNA topoisomerase, type IIA, subunit B, domain 2 / DNA gyrase B / DNA topoisomerase, type IIA / DNA topoisomerase, type IIA, conserved site / DNA topoisomerase II signature. / TopoisomeraseII / DNA topoisomerase, type IIA, subunit B, C-terminal / Toprim domain / DNA topoisomerase, type IIA-like domain superfamily / Toprim domain profile. / TOPRIM domain / Bromodomain protein 4, C-terminal / C-terminal domain of bromodomain protein 4 / Brdt, bromodomain, repeat I / Brdt, bromodomain, repeat II / NET domain superfamily / NET domain profile. / : / NET domain / Bromodomain extra-terminal - transcription regulation / Histidine kinase-, DNA gyrase B-, and HSP90-like ATPase / Bromodomain-like / Histone Acetyltransferase; Chain A / Histidine kinase/HSP90-like ATPase superfamily / Bromodomain, conserved site / Bromodomain signature. / Bromodomain / bromo domain / Bromodomain (BrD) profile. / Bromodomain / Bromodomain-like superfamily / Ribosomal protein S5 domain 2-type fold, subgroup / Ribosomal protein S5 domain 2-type fold / Up-down Bundle / Mainly Alpha 類似検索 - ドメイン・相同性
Bromodomain-containing protein 4 / DNA topoisomerase 2-alpha 類似検索 - 構成要素
ジャーナル: Mol Cell / 年: 2019 タイトル: Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains. 著者: Jean-Philippe Lambert / Sarah Picaud / Takao Fujisawa / Huayun Hou / Pavel Savitsky / Liis Uusküla-Reimand / Gagan D Gupta / Hala Abdouni / Zhen-Yuan Lin / Monika Tucholska / James D R ...著者: Jean-Philippe Lambert / Sarah Picaud / Takao Fujisawa / Huayun Hou / Pavel Savitsky / Liis Uusküla-Reimand / Gagan D Gupta / Hala Abdouni / Zhen-Yuan Lin / Monika Tucholska / James D R Knight / Beatriz Gonzalez-Badillo / Nicole St-Denis / Joseph A Newman / Manuel Stucki / Laurence Pelletier / Nuno Bandeira / Michael D Wilson / Panagis Filippakopoulos / Anne-Claude Gingras / 要旨: Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the interactomes of BRD2, ...Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the interactomes of BRD2, BRD3, BRD4, and BRDT following treatment with the pan-BET BRD inhibitor JQ1, revealing broad rewiring of the interaction landscape, with three distinct classes of behavior for the 603 unique interactors identified. A group of proteins associate in a JQ1-sensitive manner with BET BRDs through canonical and new binding modes, while two classes of extra-terminal (ET)-domain binding motifs mediate acetylation-independent interactions. Last, we identify an unexpected increase in several interactions following JQ1 treatment that define negative functions for BRD3 in the regulation of rRNA synthesis and potentially RNAPII-dependent gene expression that result in decreased cell proliferation. Together, our data highlight the contributions of BET protein modules to their interactomes allowing for a better understanding of pharmacological rewiring in response to JQ1.
解像度: 1.15→29.1 Å / Cor.coef. Fo:Fc: 0.975 / Cor.coef. Fo:Fc free: 0.97 / SU B: 0.893 / SU ML: 0.019 / 交差検証法: THROUGHOUT / ESU R: 0.032 / ESU R Free: 0.033 / 詳細: HYDROGENS HAVE BEEN ADDED IN THE RIDING POSITIONS