FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3193265536> ?p ?o ?g. }

• W3193265536 endingPage "3089" @default.
• W3193265536 startingPage "3082" @default.
• W3193265536 abstract "Tuberculosis is a global health problem caused by infection with the Mycobacterium tuberculosis (Mtb) bacteria. Although antibiotic treatment has dramatically reduced the impact of tuberculosis on the population, the existence and spreading of drug resistant strains urgently demands the development of new drugs that target Mtb in a different manner than currently used antibiotics. The prokaryotic ubiquitin-like protein (Pup) proteasome system is an attractive target for new drug development as it is unique to Mtb and related bacterial genera. Using a Pup-based fluorogenic substrate, we screened for inhibitors of Dop, the Mtb depupylating protease, and identified I-OMe-Tyrphostin AG538 (1) and Tyrphostin AG538 (2). The hits were validated and determined to be fast-reversible, non-ATP competitive inhibitors. We synthesized >25 analogs of 1 and 2 and show that several of the synthesized compounds also inhibit the depupylation actions of Dop on native substrate, FabD-Pup. Importantly, the pupylation activity of PafA, the sole Pup ligase in Mtb, was also inhibited by some of these compounds." @default.
• W3193265536 created "2021-08-16" @default.
• W3193265536 creator A5018977985 @default.
• W3193265536 creator A5024676614 @default.
• W3193265536 creator A5025516602 @default.
• W3193265536 creator A5030020521 @default.
• W3193265536 creator A5050982618 @default.
• W3193265536 creator A5051860831 @default.
• W3193265536 creator A5075639306 @default.
• W3193265536 creator A5080047287 @default.
• W3193265536 creator A5088622927 @default.
• W3193265536 date "2021-09-12" @default.
• W3193265536 modified "2023-10-16" @default.
• W3193265536 title "Development of Tyrphostin Analogues to Study Inhibition of the <i>Mycobacterium tuberculosis</i> Pup Proteasome System**" @default.
• W3193265536 cites W1526377515 @default.
• W3193265536 cites W1563650227 @default.
• W3193265536 cites W1604716826 @default.
• W3193265536 cites W1969090679 @default.
• W3193265536 cites W1974129529 @default.
• W3193265536 cites W1975173458 @default.
• W3193265536 cites W1989125447 @default.
• W3193265536 cites W2003362406 @default.
• W3193265536 cites W2005756027 @default.
• W3193265536 cites W2008653827 @default.
• W3193265536 cites W2021702829 @default.
• W3193265536 cites W2029935944 @default.
• W3193265536 cites W2041286214 @default.
• W3193265536 cites W2043509228 @default.
• W3193265536 cites W2044163830 @default.
• W3193265536 cites W2044949396 @default.
• W3193265536 cites W2058666659 @default.
• W3193265536 cites W2065542724 @default.
• W3193265536 cites W2066476512 @default.
• W3193265536 cites W2081368671 @default.
• W3193265536 cites W2081444617 @default.
• W3193265536 cites W2081929782 @default.
• W3193265536 cites W2082501870 @default.
• W3193265536 cites W2118057304 @default.
• W3193265536 cites W2127936263 @default.
• W3193265536 cites W2134189462 @default.
• W3193265536 cites W2138338587 @default.
• W3193265536 cites W2147917253 @default.
• W3193265536 cites W2155986708 @default.
• W3193265536 cites W2159586303 @default.
• W3193265536 cites W2160927584 @default.
• W3193265536 cites W2171814990 @default.
• W3193265536 cites W2402360108 @default.
• W3193265536 cites W2463036497 @default.
• W3193265536 cites W2581720655 @default.
• W3193265536 cites W2589417595 @default.
• W3193265536 cites W2607968173 @default.
• W3193265536 cites W2611401896 @default.
• W3193265536 cites W2611777757 @default.
• W3193265536 cites W2794094959 @default.
• W3193265536 cites W2795324006 @default.
• W3193265536 cites W2806538628 @default.
• W3193265536 cites W4210757594 @default.
• W3193265536 cites W4235301825 @default.
• W3193265536 cites W4246274378 @default.
• W3193265536 doi "https://doi.org/10.1002/cbic.202100333" @default.
• W3193265536 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8596589" @default.
• W3193265536 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34387015" @default.
• W3193265536 hasPublicationYear "2021" @default.
• W3193265536 type Work @default.
• W3193265536 sameAs 3193265536 @default.
• W3193265536 citedByCount "3" @default.
• W3193265536 countsByYear W31932655362022 @default.
• W3193265536 crossrefType "journal-article" @default.
• W3193265536 hasAuthorship W3193265536A5018977985 @default.
• W3193265536 hasAuthorship W3193265536A5024676614 @default.
• W3193265536 hasAuthorship W3193265536A5025516602 @default.
• W3193265536 hasAuthorship W3193265536A5030020521 @default.
• W3193265536 hasAuthorship W3193265536A5050982618 @default.
• W3193265536 hasAuthorship W3193265536A5051860831 @default.
• W3193265536 hasAuthorship W3193265536A5075639306 @default.
• W3193265536 hasAuthorship W3193265536A5080047287 @default.
• W3193265536 hasAuthorship W3193265536A5088622927 @default.
• W3193265536 hasBestOaLocation W31932655361 @default.
• W3193265536 hasConcept C142724271 @default.
• W3193265536 hasConcept C175114707 @default.
• W3193265536 hasConcept C181199279 @default.
• W3193265536 hasConcept C185592680 @default.
• W3193265536 hasConcept C27740335 @default.
• W3193265536 hasConcept C2776714187 @default.
• W3193265536 hasConcept C2777975735 @default.
• W3193265536 hasConcept C2780035454 @default.
• W3193265536 hasConcept C2780374374 @default.
• W3193265536 hasConcept C2781069245 @default.
• W3193265536 hasConcept C2908647359 @default.
• W3193265536 hasConcept C501593827 @default.
• W3193265536 hasConcept C523546767 @default.
• W3193265536 hasConcept C54355233 @default.
• W3193265536 hasConcept C55493867 @default.
• W3193265536 hasConcept C64903051 @default.
• W3193265536 hasConcept C71924100 @default.
• W3193265536 hasConcept C86803240 @default.
• W3193265536 hasConcept C89423630 @default.
• W3193265536 hasConcept C98274493 @default.

• next