49573-30-0Relevant articles and documents
Syntheses of aromatic aldehydes by laccase of pleurotus ostreatus MTCC-1801
Chaurasia, Pankaj Kumar,Yadava, Sudha,Bharati, Shashi Lata,Singh, Sunil Kumar
, p. 2535 - 2544 (2014)
GRAPHICAL ABSTRACT Selective bioconversion of the aromatic methyl group to its aldehyde group is one of the best applications of the laccases. In the present communication, crude laccase, obtained from the liquid culture medium of the fungal strain Pleurotus ostreatus MTCC-1801, has been used for the selective bioconversion of toluene, 3-nitrotoluene, 4-nitrotoluene, 2-fluorotoluene, 4-fluorotoluene, 2-chlorotoluene, 3-chlorotoluene, 4-chlorotoluene, and 3,4-dimethoxytoluene to benzaldehyde, 3-nitrobenzaldehyde, 4-nitrobenzaldehyde, 2-fluorobenzaldehyde, 4-fluorobenzaldehyde, 2-chlorobenzaldehyde, 3-chlorobenzaldehyde, 4-chlorobenzaldehyde, and 3,4-dimethoxybenzaldehyde, respectively, in the presence of 2,2′-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt (ABTS) as a mediator molecule. Time taken by these conversions was 1-2 h, and average yield of products was more than 93%.
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP)
Romero, F. Anthony,Murray, Jeremy,Lai, Kwong Wah,Tsui, Vickie,Albrecht, Brian K.,An, Le,Beresini, Maureen H.,De Leon Boenig, Gladys,Bronner, Sarah M.,Chan, Emily W.,Chen, Kevin X.,Chen, Zhongguo,Choo, Edna F.,Clagg, Kyle,Clark, Kevin,Crawford, Terry D.,Cyr, Patrick,De Almeida Nagata, Denise,Gascoigne, Karen E.,Grogan, Jane L.,Hatzivassiliou, Georgia,Huang, Wei,Hunsaker, Thomas L.,Kaufman, Susan,Koenig, Stefan G.,Li, Ruina,Li, Yingjie,Liang, Xiaorong,Liao, Jiangpeng,Liu, Wenfeng,Ly, Justin,Maher, Jonathan,Masui, Colin,Merchant, Mark,Ran, Yingqing,Taylor, Alexander M.,Wai, John,Wang, Fei,Wei, Xiaocang,Yu, Dong,Zhu, Bing-Yan,Zhu, Xiaoyu,Magnuson, Steven
, p. 9162 - 9183 (2017)
Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical tool 1 (GNE-272) for the bromodomain of CBP that was moderately potent and selective over BRD4(1). In pursuit of a more potent and selective CBP inhibitor, we used structure-based design. Constraining the aniline of 1 into a tetrahydroquinoline motif maintained potency and increased selectivity 2-fold. Structure-activity relationship studies coupled with further structure-based design targeting the LPF shelf, BC loop, and KAc regions allowed us to significantly increase potency and selectivity, resulting in the identification of non-CNS penetrant 19 (GNE-781, TR-FRET IC50 = 0.94 nM, BRET IC50 = 6.2 nM; BRD4(1) IC50 = 5100 nM) that maintained good in vivo PK properties in multiple species. Compound 19 displays antitumor activity in an AML tumor model and was also shown to decrease Foxp3 transcript levels in a dose dependent manner.
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)
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.
TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER
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, (2021/01/29)
A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.
MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Paragraph 001195-001197, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
CYCLIC-AMP RESPONSE ELEMENT BINDING PROTEIN (CBP) AND/OR ADENOVIRAL E1A BINDING PROTEIN OF 300 KDA (P300) DEGRADATION COMPOUNDS AND METHODS OF USE
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Page/Page column 109-110, (2020/09/12)
Bivalent compounds composition comprises one or more of the bivalent compounds. The bivalent compound comprises a cyclic-AMP response element binding protein (CBP) and/or adenoviral E1A binding protein of 300kDa (P300) ligand (CBP/P300 ligand) conjugated
IMIDAZOPIPERAZINONE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
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Paragraph 0536-0538, (2019/10/20)
The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
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Paragraph 0493-0494, (2019/10/17)
The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
cGAS ANTAGONIST COMPOUNDS
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Paragraph 0224, (2017/11/06)
Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
THERAPEUTIC COMPOUNDS AND USES THEREOF
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Page/Page column 68; 69, (2017/12/29)
The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R5-R6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
