LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 2 of total 2

Search options

  1. Article ; Online: Site-Selective Modification of Secondary Amine Moieties on Native Peptides, Proteins, and Natural Products with Ynones.

    Gao, Feng / Chang, Mengyang / Meng, Xiang / Xu, Hang / Gnawali, Giri / Dong, Yue / Lopez, Byrdie / Wang, Wei

    Bioconjugate chemistry

    2023  Volume 34, Issue 9, Page(s) 1553–1562

    Abstract: Site-selective modification of biologically relevant secondary amines in peptides, proteins, and natural products has been challenging due to the similar reactivity between primary and secondary amines. Even for the secondary amines, their reactivities ... ...

    Abstract Site-selective modification of biologically relevant secondary amines in peptides, proteins, and natural products has been challenging due to the similar reactivity between primary and secondary amines. Even for the secondary amines, their reactivities are significantly influenced by their structures and environment. Herein, we report a ynone Michael bioconjugation method for selective modification of secondary amines in unprotected peptides and proteins and complex natural products. We show that fine tuning the electronic effect of the ynones enables controlling the Michael acceptor reactivity for the selective reaction with the structurally different secondary amines in densely functionalized complex structures and complicated biological environment.
    MeSH term(s) Peptides ; Amines ; Biological Products
    Chemical Substances Peptides ; Amines ; Biological Products
    Language English
    Publishing date 2023-08-30
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 1024041-x
    ISSN 1520-4812 ; 1043-1802
    ISSN (online) 1520-4812
    ISSN 1043-1802
    DOI 10.1021/acs.bioconjchem.3c00246
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 3400: 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.

  2. Article ; Online: Selective Elimination of Senescent Cancer Cells by Galacto-Modified PROTACs.

    Chang, Mengyang / Gao, Feng / Gnawali, Giri / Xu, Hang / Dong, Yue / Meng, Xiang / Li, Wenpan / Wang, Zhiren / Lopez, Byrdie / Carew, Jennifer S / Nawrocki, Steffan T / Lu, Jianqin / Zhang, Qing-Yu / Wang, Wei

    Journal of medicinal chemistry

    2024  Volume 67, Issue 9, Page(s) 7301–7311

    Abstract: Although the selective and effective clearance of senescent cancer cells can improve cancer treatment, their development is confronted by many challenges. As part of efforts designed to overcome these problems, prodrugs, whose design is based on ... ...

    Abstract Although the selective and effective clearance of senescent cancer cells can improve cancer treatment, their development is confronted by many challenges. As part of efforts designed to overcome these problems, prodrugs, whose design is based on senescence-associated β-galactosidase (SA-β-gal), have been developed to selectively eliminate senescent cells. However, chemotherapies relying on targeted molecular inhibitors as senolytic drugs can induce drug resistance. In the current investigation, we devised a new strategy for selective degradation of target proteins in senescent cancer cells that utilizes a prodrug composed of the SA-β-gal substrate galactose (galacto) and the proteolysis-targeting chimeras (PROTACs) as senolytic agents. Prodrugs Gal-ARV-771 and Gal-MS99 were found to display senolytic indexes higher than those of ARV-771 and MS99. Significantly, results of
    MeSH term(s) Humans ; Animals ; Cellular Senescence/drug effects ; Galactose/chemistry ; Galactose/pharmacology ; Prodrugs/pharmacology ; Prodrugs/chemistry ; Prodrugs/therapeutic use ; Mice ; Proteolysis/drug effects ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/therapeutic use ; Xenograft Model Antitumor Assays ; beta-Galactosidase/metabolism ; Mice, Nude ; Cell Line, Tumor ; Cell Proliferation/drug effects ; A549 Cells ; Etoposide/pharmacology ; Senotherapeutics/pharmacology ; Senotherapeutics/chemistry ; Proteolysis Targeting Chimera
    Chemical Substances Galactose (X2RN3Q8DNE) ; Prodrugs ; Antineoplastic Agents ; beta-Galactosidase (EC 3.2.1.23) ; Etoposide (6PLQ3CP4P3) ; Senotherapeutics ; Proteolysis Targeting Chimera
    Language English
    Publishing date 2024-04-18
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.4c00152
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

    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.

To top