Database of articles cited by EMDB/PDB/SASBDB data

Keywords
Structure methods	All X-ray diffraction NMR electron microscopy small angle scattering neutron diffraction fiber diffraction powder diffraction infrared spectroscopy EPR fluorescence transfer theoretical model Hybrid
Author
Journal
IF	>30 >20 >10 >5 all

Title	Solid-phase synthesis and biological evaluation of des-hydroxy pseudouridimycin analogs.
Journal, issue, pages	ACS Med Chem Lett, Year 2026
Publish date	Mar 11, 2026
Authors	Avraz F Anwar / Linlin You / David Degen / Katie J Burns / Michael J Garza / Richard H Ebright / Juan R Del Valle /
PubMed Abstract	Pseudouridimycin (PUM) is a C-nucleoside/peptide antibiotic that selectively inhibits bacterial RNA polymerase (RNAP) and exhibits potent activity against drug-resistant pathogens. However, PUM ...Pseudouridimycin (PUM) is a C-nucleoside/peptide antibiotic that selectively inhibits bacterial RNA polymerase (RNAP) and exhibits potent activity against drug-resistant pathogens. However, PUM suffers from chemical instability due to self-immolative cleavage of its central hydroxamate bond. Here, we employed cryo-electron microscopy to determine structures of PUM () and a chemically stabilized des-hydroxy analog of PUM () bound to an RNAP transcription complex. Guided by the observed bound conformation, we developed an efficient solid-phase synthesis of 50 des-hydroxy PUM analogs modified at the Gln residue and Gdn-Gly tail. Several analogs retained low-micromolar RNAP-inhibitory activity, with a -substituted phenyl amidine analog () emerging as the most potent inhibitor (IC = 0.95 μM). These results establish a versatile synthetic platform and structural framework for optimizing stabilized PUM derivatives and provide a foundation for the development of RNAP-targeted therapeutics against resistant bacterial pathogens.
External links	ACS Med Chem Lett / PubMed:41890570 / PubMed Central
Methods	EM (single particle)
Resolution	3.06 - 3.32 Å
Structure data	73220 9ynp EMDB-73220, PDB-9ynp: Cryo-EM structure of Escherichia coli transcription initiation complex with GpA and pseudouridimycin (PUM) Method: EM (single particle) / Resolution: 3.06 Å 73221 9ynq EMDB-73221, PDB-9ynq: Cryo-EM structure of Escherichia coli transcription initiation complex with GpA and des-hydroxy pseudouridimycin (des-hydroxy PUM) Method: EM (single particle) / Resolution: 3.32 Å
Chemicals	ChemComp-ZN: Unknown entry ChemComp-MG: Unknown entry ChemComp-PUM: (1S)-1,4-anhydro-5-[(N-carbamimidoylglycyl-N~2~-hydroxy-L-glutaminyl)amino]-5-deoxy-1-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-D-ribitol / antibioticYM PDB Unreleased entry PDB-1cyh*: Unknown entry
Source	escherichia coli str. k-12 substr. mg1655 (bacteria)
Keywords	TRANSCRIPTION / TRANSFERASE/DNA/RNA/INHIBITOR / Transcription initiation complex / Pseudouridimycin (PUM) / Inhibitor / Antibacterial agent / TRANSFERASE-DNA-RNA-INHIBITOR complex / Des-hydroxy pseudouridimycin (des-hydroxy PUM)