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  1. Article ; Online: Cyclobutanone Inhibitors of Diaminopimelate Desuccinylase (DapE) as Potential New Antibiotics.

    Habeeb Mohammad, Thahani S / Kelley, Emma H / Reidl, Cory T / Konczak, Katherine / Beulke, Megan / Javier, Janielle / Olsen, Kenneth W / Becker, Daniel P

    International journal of molecular sciences

    2024  Volume 25, Issue 2

    Abstract: Based on our previous success in using cyclobutanone derivatives as enzyme inhibitors, we have designed and prepared a 37-member library of α-aminocyclobutanone amides and sulfonamides, screened for inhibition of the bacterial enzyme diaminopimelate ... ...

    Abstract Based on our previous success in using cyclobutanone derivatives as enzyme inhibitors, we have designed and prepared a 37-member library of α-aminocyclobutanone amides and sulfonamides, screened for inhibition of the bacterial enzyme diaminopimelate desuccinylase (DapE), which is a promising antibiotic target, and identified several inhibitors with micromolar inhibitory potency. Molecular docking suggests binding of the deprotonated hydrate of the strained cyclobutanone, and thermal shift analysis with the most potent inhibitor (
    MeSH term(s) Molecular Docking Simulation ; Anti-Bacterial Agents/pharmacology ; Enzyme Inhibitors/pharmacology
    Chemical Substances Anti-Bacterial Agents ; Enzyme Inhibitors
    Language English
    Publishing date 2024-01-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2019364-6
    ISSN 1422-0067 ; 1422-0067 ; 1661-6596
    ISSN (online) 1422-0067
    ISSN 1422-0067 ; 1661-6596
    DOI 10.3390/ijms25021339
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Synthesis and characterization of the N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE) alternate substrate analog N,N-dimethyl-l,l-SDAP.

    Liveris, Zachary J / Kelley, Emma H / Simmons, Emma / Konczak, Katherine / Lutz, Marlon R / Ballicora, Miguel / Olsen, Kenneth W / Becker, Daniel P

    Bioorganic & medicinal chemistry

    2023  Volume 91, Page(s) 117415

    Abstract: Growing antibiotic resistance by pathogenic bacteria has led to a global crisis. The bacterial enzyme N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE) provides a very attractive target for the discovery of a new class of antibiotics, as it resides ...

    Abstract Growing antibiotic resistance by pathogenic bacteria has led to a global crisis. The bacterial enzyme N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE) provides a very attractive target for the discovery of a new class of antibiotics, as it resides exclusively in many pathogenic bacterial strains and is a key enzyme in the lysine biosynthetic pathway. This pathway is responsible for the production of lysine as well as meso-diaminopimelate (m-DAP), both of which are required for peptidoglycan cell-wall synthesis, and lysine for peptide synthesis. The enzyme DapE catalyzes the hydrolysis of N-succinyl-l,l-diaminopimelic acid (l,l-SDAP) to succinate and l,l-diaminopimelic acid (l,l-DAP), and due to its absence in humans, inhibition of DapE avoids mechanism-based side effects. We have executed the asymmetric synthesis of N,N-dimethyl-SDAP, an l,l-SDAP substrate analog and an analog of the synthetic substrate of our previously described DapE assay. Previous modeling studies advocated that N,N-dimethyl-SDAP might function as an inhibitor, however the compound behaves as a substrate, and we have demonstrated the use of N,N-dimethyl-SDAP as the substrate in a modified ninhydrin-based DapE assay. Thermal shift experiments of DapE in the presence of N,N-dimethyl-SDAP are consistent with a melt temperature (T
    MeSH term(s) Humans ; Diaminopimelic Acid/chemistry ; Diaminopimelic Acid/metabolism ; Lysine ; Succinates ; Drug Resistance, Bacterial
    Chemical Substances Diaminopimelic Acid (583-93-7) ; Lysine (K3Z4F929H6) ; Succinates ; succinyldiaminopimelate desuccinylase (EC 3.5.1.18)
    Language English
    Publishing date 2023-07-12
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2023.117415
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3815: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: Biochemical and Structural Analysis of the Bacterial Enzyme Succinyl-Diaminopimelate Desuccinylase (DapE) from

    Kelley, Emma H / Minasov, George / Konczak, Katherine / Shuvalova, Ludmilla / Brunzelle, Joseph S / Shukla, Shantanu / Beulke, Megan / Thabthimthong, Teerana / Olsen, Kenneth W / Inniss, Nicole L / Satchell, Karla J F / Becker, Daniel P

    ACS omega

    2024  Volume 9, Issue 3, Page(s) 3905–3915

    Abstract: There is an urgent need for new antibiotics given the rise of antibiotic resistance, and succinyl-diaminopimelate desuccinylase (DapE, E.C. 3.5.1.18) has emerged as a promising bacterial enzyme target. DapE ... ...

    Abstract There is an urgent need for new antibiotics given the rise of antibiotic resistance, and succinyl-diaminopimelate desuccinylase (DapE, E.C. 3.5.1.18) has emerged as a promising bacterial enzyme target. DapE from
    Language English
    Publishing date 2024-01-08
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.3c08231
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Tetrazole-based inhibitors of the bacterial enzyme N-succinyl-l,l-2,6-diaminopimelic acid desuccinylase as potential antibiotics.

    DiPuma, Thomas / Thabthimthong, Teerana / Kelley, Emma H / Konczak, Katherine / Beulke, Megan / Herbert, Claire / S Habeeb Mohammad, Thahani / Starus, Anna / Nocek, Boguslaw / Olsen, Kenneth W / Holz, Richard C / Becker, Daniel P

    Bioorganic & medicinal chemistry letters

    2023  Volume 83, Page(s) 129177

    Abstract: Based on a hit from a high-throughput screen, a series of phenyltetrazole amides was synthesized and assayed for inhibitory potency against DapE from Haemophilus influenzae (HiDapE). The inhibitory potency was modest but confirmed, with the most potent ... ...

    Abstract Based on a hit from a high-throughput screen, a series of phenyltetrazole amides was synthesized and assayed for inhibitory potency against DapE from Haemophilus influenzae (HiDapE). The inhibitory potency was modest but confirmed, with the most potent analog containing an aminothiazole moiety displaying an IC
    MeSH term(s) Anti-Bacterial Agents/pharmacology ; Catalytic Domain ; Diaminopimelic Acid/chemistry ; Diaminopimelic Acid/metabolism ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/metabolism ; Zinc/chemistry ; Tetrazoles/chemistry
    Chemical Substances Anti-Bacterial Agents ; Diaminopimelic Acid (583-93-7) ; Enzyme Inhibitors ; Zinc (J41CSQ7QDS) ; Tetrazoles
    Language English
    Publishing date 2023-02-09
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2023.129177
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3203: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

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