Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. - Wikidata - awgldk - TriplyDB

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

http://www.wikidata.org/entity/Q36586506

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Open access chemical probes for epigenetic targets The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network.Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains Exploiting Epigenetic Alterations in Prostate Cancer.Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery Developing Spindlin1 small-molecule inhibitors by using protein microarrays.T-cell-intrinsic Tif1α/Trim24 regulates IL-1R expression on TH2 cells and TH2 cell-mediated airway allergy.TRIM24 Is an Oncogenic Transcriptional Activator in Prostate Cancer.Discovery of a PCAF Bromodomain Chemical Probe.Selective targeting of Bromodomains of the Bromodomain-PHD Fingers family impairs osteoclast differentiation.Progress in the Development of non-BET Bromodomain Chemical Probes.Targeting epigenetic regulators for cancer therapy: modulation of bromodomain proteins, methyltransferases, demethylases, and microRNAs.Selective targeting of epigenetic reader domains.Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development.Biological function and histone recognition of family IV bromodomain-containing proteins.Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology.Structural features and inhibitors of bromodomains.Histone H3 lysine 23 acetylation is associated with oncogene TRIM24 expression and a poor prognosis in breast cancer.Targeting transcriptional co-activators in advanced prostate cancer.GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain Chemical probes and inhibitors of bromodomains outside the BET family.Chemical Space Expansion of Bromodomain Ligands Guided by in Silico Virtual Couplings (AutoCouple).Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesion.Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands.Discovery of a PCAF Bromodomain Chemical Probe

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Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

http://www.wikidata.org/entity/Q36586506

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2015 nî lūn-bûn

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Structure-Guided Design of IAC ...... 4-BRPF1 Bromodomain Inhibitor.

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Structure-Guided Design of IAC ...... 4-BRPF1 Bromodomain Inhibitor.

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Structure-Guided Design of IAC ...... 4-BRPF1 Bromodomain Inhibitor.

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Structure-Guided Design of IAC ...... 4-BRPF1 Bromodomain Inhibitor.

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ACS.JMEDCHEM.5B00405

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Journal of Medicinal Chemistry

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Structure-Guided Design of IAC ...... 4-BRPF1 Bromodomain Inhibitor.

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Alessia Petrocchi

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Anne Yau

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Elisabetta Leo

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Gang Liu

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Giulio Draetta

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Govindan Subramanian

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Guillaume Poncet-Montange

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Hannah E Shepard

http://www.w3.org/2001/XMLSchema#string

Jay Theroff

http://www.w3.org/2001/XMLSchema#string

Jennifer P Bardenhagen

http://www.w3.org/2001/XMLSchema#string

P2860

RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

Selective inhibition of BET bromodomains

Structural insights into recognition of acetylated histone ligands by the BRPF1 bromodomain

Histone recognition and large-scale structural analysis of the human bromodomain family

TRIM24 links a non-canonical histone signature to breast cancer

Trim24 targets endogenous p53 for degradation

ZINC--a free database of commercially available compounds for virtual screening

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

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1440-1454

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10.1021/ACS.JMEDCHEM.5B00405

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4

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59

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Michelle Craig Barton

Jannik N Andersen

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2015-06-10T00:00:00Z

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278043989

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26061247

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4755933

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