Results 51 to 60 of about 152,508 (309)

A New Recruitable E3 Ligase UHRF1 Supporting Targeted Protein Degradation: A Minimal Azide as a Recruitment Ligand. [PDF]

Adv Sci (Weinh)
Targeted protein degradation is often limited by the scarcity of usable E3 ligases. Herein, we report the first small‐molecule GPX4 degraders that incorporate either electrophilic warheads or a minimal azide group as an E3 recruitment ligand. The azide‐based degrader DK‐5070 effectively drives potent GPX4 degradation; mechanistic studies reveal that ...
Lin Z, Duan K, Wan R, Jiang T, Wei J, Sun M, Skryl'nikova MA, Gureev MA, Zhang ZM, Zhang Z, Ding K, Ma N, Liu T, Tan Y, Li Z.   +14 more
europepmc   +2 more sources

Chemoselectivity of Tertiary Azides in Strain‐Promoted Alkyne‐Azide Cycloadditions [PDF]

Chemistry – A European Journal, 2018
AbstractThe strain‐promoted alkyne‐azide cycloaddition (SPAAC) is the most commonly employed bioorthogonal reaction with applications in a broad range of fields. Over the years, several different cyclooctyne derivatives have been developed and investigated in regard to their reactivity in SPAAC reactions with azides.
Dennis Svatunek, Nicole Houszka, Trevor A. Hamlin, F. Matthias Bickelhaupt, Hannes Mikula   +4 more
openaire   +5 more sources

Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation

FEBS Letters, EarlyView.
Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang, Ruslana Romaniuk, Hristo L. Svilenov   +2 more
wiley   +1 more source

Synthesis and structure of catena-poly[[[bis(pyridin-2-yl)amine]cadmium(II)]-di-μ2-azido]

Acta Crystallographica Section E: Crystallographic Communications
In the title compound, [Cd(N3)2(C10H9N3)]n, the cadmium(II) ion displays a distorted CdN6 octahedral geometry arising from one bidentate ligand and four azide ions and forms zigzag polymeric [100] chains via the bridging azide ions, both of which show μ1,
Zouaoui Setifi, Fatima Setifi, Joel T. Mague, Mohammed Hadi Al-Douh   +3 more
doaj   +1 more source

Weak M(II)-Azide-4,4‘-Bipy Ferromagnets Based on Unusual Diamondoid (M = Mn) and 2D Arrays (M = Co, Ni)

, 2016
Four compounds of general formula [M(4,4‘bipy)(N3)2]n (M = Mn (1), Zn (2), Co (3), Ni (4)) have been synthesized and magnetostructurally characterized by means of X-ray diffraction analysis, IR and ESR spectroscopies, and measurements of the magnetic ...
Susana Martín (2962941), Luis Lezama (1318113), M. Isabel Arriortua (2252194), Roberto Cortés (2962950), Zurine E. Serna (2962944), Teófilo Rojo (2522158), J. Luis Pizarro (2962947), J. Ignacio Ruiz de Larramendi (2962953), M. Gotzone Barandika (2252191)   +8 more
core   +1 more source

Emerging experimental and computational methods for studying redox‐regulated structural transitions

FEBS Letters, EarlyView.
Redox reactions can reshape proteins and alter how they behave in cells, with important consequences for health and disease. This review explores emerging experimental and computational approaches for discovering these redox‐sensitive protein switches, revealing their structural effects, and predicting their behavior, opening new opportunities to ...
Tasneem Rass, Dana Reichmann, Gábor Erdős   +2 more
wiley   +1 more source

Well-Defined Diimine Copper(I) Complexes as Catalysts in Click Azide-Alkyne Cycloaddition Reactions

Molecules, 2013
A series of 1,4-disubstituted 1,2,3-triazoles have been prepared in high yields while respecting the stringent Click criteria. In these reactions, highly stable pre-formed complexes bearing diimine ligands were used.
Silvia Díez-González, Jordi Markalain Barta   +1 more
doaj   +1 more source

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

Molecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla, Christopher Dirks, Caroline Eiden, Sonja K. Fesenmayer, Femke M. Hormann, Yolande Klootsema, Ingrid Lilienthal, Si Min Zhang, Nikolas Herold, Sean G. Rudd   +9 more
wiley   +1 more source

Synthesis of 1,4-Disubstituted Mono and Bis-triazolocarbo-acyclonucleoside Analogues of 9-(4-Hydroxybutyl)guanine by Cu(I)-Catalyzed Click Azide-Alkyne Cycloaddition [PDF]

, 2011
A series of novel mono-1,2,3-triazole and bis-1,2,3-triazole acyclonucleoside analogues of 9-(4-hydroxybutyl)guanine was prepared via copper(I)-catalyzed 1,3-dipolar cycloaddition of N-9 propargylpurine, N-1-propargylpyrimidines/as-triazine with the ...
Krim, Jamal, Taourirte, Mohamed, Engels, Joachim W., Moha Taourirte, Jamal Krim, Joachim W. Engels   +5 more
core   +1 more source

USP29‐regulated noncanonical stabilization of the hypoxia‐inducible factor‐α in aggressive prostate cancer

Molecular Oncology, EarlyView.
We identify USP29 as the only DUB mirroring CA9 expression, a marker of hypoxia and HIF pathway activation associated with PCA aggressiveness. USP29 stabilizes HIF‐1α and HIF‐2α via a noncanonical mechanism that is independent of PHD/pVHL activity yet relies on proteasomal regulation, establishing USP29 as a previously unrecognized regulator of hypoxic
Amelie S Schober, Leire Moreno‐Cugnon, Laura Martínez‐Pérez, Amaia Ercilla, Amaia Zabala‐Letona, Adrián Vicente‐Barrueco, Maider Fagoaga‐Eugui, Saioa Garcia‐Longarte, Blanca Calle‐Ciborro, Encarnación Pérez‐Andrés, Onintza Carlevaris, Sara Pozo, Isabel Mendizabal, Ugo Mayor, Arkaitz Carracedo, Violaine Sée, Edurne Berra   +16 more
wiley   +1 more source