835616-61-0Relevant articles and documents
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND METHODS OF USE THEREOF
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Page/Page column 166-167, (2021/06/26)
Provided herein are compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer 5 or a metabolic disease.
Targeted degradation of the enhancer lysine acetyltransferases CBP and p300
Vannam, Raghu,Sayilgan, Jan,Ojeda, Samuel,Karakyriakou, Barbara,Hu, Eileen,Kreuzer, Johannes,Morris, Robert,Herrera Lopez, Xcanda Ixchel,Rai, Sumit,Haas, Wilhelm,Lawrence, Michael,Ott, Christopher J.
, p. 503 - 12,514 (2021/01/26)
The enhancer factors CREB-binding protein (CBP) and p300 (also known as KAT3A and KAT3B) maintain gene expression programs through lysine acetylation of chromatin and transcriptional regulators and by scaffolding functions mediated by several protein-protein interaction domains. Small molecule inhibitors that target some of these domains have been developed; however, they cannot completely ablate p300/CBP function in cells. Here we describe a chemical degrader of p300/CBP, dCBP-1. Leveraging structures of ligand-bound p300/CBP domains, we use in silico modeling of ternary complex formation with the E3 ubiquitin ligase cereblon to enable degrader design. dCBP-1 is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression. As an efficient degrader of this unique class of acetyltransferases, dCBP-1 is a useful tool alongside domain inhibitors for dissecting the mechanism by which these factors coordinate enhancer activity in normal and diseased cells.
Sulfur-containing compound based on glutaryl imide skeleton and application of compound
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Paragraph 0347-0349, (2020/09/12)
The present disclosure relates to compound shown in a formula (I) or salts, solvates, isotope-enriched analogs, tautomers, polymorphs, stereoisomers, or mixtures of stereoisomers of the compound, andthe application thereof in the treatment of tumours. The present disclosure also provides tumor treatment application of the compound showed in a formula (I') or pharmaceutically acceptable salts, solvates, isotope-enriched analogs, tautomers, polymorphic substances, stereoisomers, or mixtures of stereoisomers of the compound.