FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3048321732> ?p ?o ?g. }

• W3048321732 endingPage "5233" @default.
• W3048321732 startingPage "5225" @default.
• W3048321732 abstract "Histone methylation reader proteins (HMRPs) regulate gene transcription by recognizing, at their “aromatic cage” domains, various Lys/Arg methylation states on histone tails. Because epigenetic dysregulation underlies a wide range of diseases, HMRPs have become attractive drug targets. However, structure-based efforts in targeting them are still in their infancy. Structural information from functionally unrelated aromatic-cage-containing proteins (ACCPs) and their cocrystallized ligands could be a good starting point. In this light, we mined the Protein Data Bank to retrieve the structures of ACCPs in complex with cationic peptidic/small-molecule ligands. Our analysis revealed that the vast majority of retrieved ACCPs belong to three classes: transcription regulators (chiefly HMRPs), signaling proteins, and hydrolases. Although acyclic (and monocyclic) amines and quats are the typical cation-binding functional groups found in HMRP small-molecule inhibitors, numerous atypical cationic groups were identified in non-HMRP inhibitors, which could serve as potential bioisosteres to methylated Lys/Arg on histone tails. Also, as HMRPs are involved in protein–protein interactions, they possess large binding sites, and thus, their selective inhibition might only be achieved by large and more flexible (beyond rule of five) ligands. Hence, the ligands of the collected dataset represent suitable versatile templates for further elaboration into potent and selective HMRP inhibitors." @default.
• W3048321732 created "2020-08-13" @default.
• W3048321732 creator A5010380284 @default.
• W3048321732 creator A5016519042 @default.
• W3048321732 creator A5049231945 @default.
• W3048321732 date "2020-08-07" @default.
• W3048321732 modified "2023-09-25" @default.
• W3048321732 title "Exploring Cocrystallized Aromatic Cage Binders to Target Histone Methylation Reader Proteins" @default.
• W3048321732 cites W105839754 @default.
• W3048321732 cites W1939922453 @default.
• W3048321732 cites W1966882047 @default.
• W3048321732 cites W1979827504 @default.
• W3048321732 cites W1991072488 @default.
• W3048321732 cites W1998137132 @default.
• W3048321732 cites W1999478182 @default.
• W3048321732 cites W2004976660 @default.
• W3048321732 cites W2009593219 @default.
• W3048321732 cites W2012745625 @default.
• W3048321732 cites W2013059500 @default.
• W3048321732 cites W2015041117 @default.
• W3048321732 cites W2032729355 @default.
• W3048321732 cites W2036158314 @default.
• W3048321732 cites W2037428681 @default.
• W3048321732 cites W2059971190 @default.
• W3048321732 cites W2060237924 @default.
• W3048321732 cites W2067831535 @default.
• W3048321732 cites W2069506489 @default.
• W3048321732 cites W2071180837 @default.
• W3048321732 cites W2074679890 @default.
• W3048321732 cites W2076333986 @default.
• W3048321732 cites W2081996507 @default.
• W3048321732 cites W2106482095 @default.
• W3048321732 cites W2114326383 @default.
• W3048321732 cites W2130479394 @default.
• W3048321732 cites W2135575165 @default.
• W3048321732 cites W2140902413 @default.
• W3048321732 cites W2144275955 @default.
• W3048321732 cites W2155754186 @default.
• W3048321732 cites W2158331775 @default.
• W3048321732 cites W2167202592 @default.
• W3048321732 cites W2169678694 @default.
• W3048321732 cites W2179066627 @default.
• W3048321732 cites W2238621957 @default.
• W3048321732 cites W2315423922 @default.
• W3048321732 cites W2542506932 @default.
• W3048321732 cites W2724716579 @default.
• W3048321732 cites W2768016189 @default.
• W3048321732 cites W2797262353 @default.
• W3048321732 cites W3020215747 @default.
• W3048321732 doi "https://doi.org/10.1021/acs.jcim.0c00765" @default.
• W3048321732 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32786701" @default.
• W3048321732 hasPublicationYear "2020" @default.
• W3048321732 type Work @default.
• W3048321732 sameAs 3048321732 @default.
• W3048321732 citedByCount "5" @default.
• W3048321732 countsByYear W30483217322021 @default.
• W3048321732 countsByYear W30483217322022 @default.
• W3048321732 crossrefType "journal-article" @default.
• W3048321732 hasAuthorship W3048321732A5010380284 @default.
• W3048321732 hasAuthorship W3048321732A5016519042 @default.
• W3048321732 hasAuthorship W3048321732A5049231945 @default.
• W3048321732 hasConcept C104317684 @default.
• W3048321732 hasConcept C119157956 @default.
• W3048321732 hasConcept C150194340 @default.
• W3048321732 hasConcept C161624437 @default.
• W3048321732 hasConcept C185592680 @default.
• W3048321732 hasConcept C190727270 @default.
• W3048321732 hasConcept C22709980 @default.
• W3048321732 hasConcept C33288867 @default.
• W3048321732 hasConcept C41091548 @default.
• W3048321732 hasConcept C55493867 @default.
• W3048321732 hasConcept C64927066 @default.
• W3048321732 hasConcept C70721500 @default.
• W3048321732 hasConcept C86339819 @default.
• W3048321732 hasConcept C86803240 @default.
• W3048321732 hasConceptScore W3048321732C104317684 @default.
• W3048321732 hasConceptScore W3048321732C119157956 @default.
• W3048321732 hasConceptScore W3048321732C150194340 @default.
• W3048321732 hasConceptScore W3048321732C161624437 @default.
• W3048321732 hasConceptScore W3048321732C185592680 @default.
• W3048321732 hasConceptScore W3048321732C190727270 @default.
• W3048321732 hasConceptScore W3048321732C22709980 @default.
• W3048321732 hasConceptScore W3048321732C33288867 @default.
• W3048321732 hasConceptScore W3048321732C41091548 @default.
• W3048321732 hasConceptScore W3048321732C55493867 @default.
• W3048321732 hasConceptScore W3048321732C64927066 @default.
• W3048321732 hasConceptScore W3048321732C70721500 @default.
• W3048321732 hasConceptScore W3048321732C86339819 @default.
• W3048321732 hasConceptScore W3048321732C86803240 @default.
• W3048321732 hasFunder F4320310414 @default.
• W3048321732 hasFunder F4320320875 @default.
• W3048321732 hasFunder F4320320879 @default.
• W3048321732 hasIssue "10" @default.
• W3048321732 hasLocation W30483217321 @default.
• W3048321732 hasOpenAccess W3048321732 @default.
• W3048321732 hasPrimaryLocation W30483217321 @default.
• W3048321732 hasRelatedWork W1983315005 @default.
• W3048321732 hasRelatedWork W2007548422 @default.

• next