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Structure of the human multidrug transporter ABCG2

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ABCG2 is an ATP-binding cassette transporter that exports a wide range of xenobiotic compounds and has been recognized as a contributing factor for multidrug resistance in cancer cells. Substrate and inhibitor interactions with ABCG2 have been extensively ...

ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD2023

Cysteine-Cysteine Cross-Conjugation of both Peptides and Proteins with a Bifunctional Hypervalent Iodine-Electrophilic Reagent

Jérôme Waser, Stefano Nicolai, Abhaya Kumar Mishra

Peptide and protein bioconjugation sees ever-growing applications in the pharmaceutical sector. Novel strategies and reagents that can address the chemo- and regioselectivity issues inherent to these biomolecules, while delivering stable and functionalizab ...

Weinheim2023

Clathrin-associated AP-1 control stermination of STING signalling

Andrea Ablasser, Jonathan Jean-Pierre Ricci, Chong Liu, Pengbiao Xu, Ying Liu, Sophie Marie Elisabeth Rivara

Stimulator of interferon genes (STING) functions downstream of cyclic GMP-AMP synthase in DNA sensing or as a direct receptor for bacterial cyclic dinucleotides and small molecules to activate immunity during infection, cancer and immunotherapy(1-10). Prec ...

NATURE PORTFOLIO2022

Efficient immune responses require Ca2+ fluxes across ORAI1 channels during engagement of T cell receptors (TCR) at the immune synapse (IS) between T cells and antigen presenting cells. Here, we show that ZDHHC20-mediated S-acylation of the ORAI1 channel a ...

eLIFE SCIENCES PUBL LTD2021

High specificity accompanied with the ability to recruit immune cells has made recombinant therapeutic antibodies an integral part of drug development. Here we present a generic approach to generate two novel IgG-derived antibody formats that are based on ...

Informa UK Limited2019

Memristive Biosensors based on Full-size Antibodies and Antibody Fragments

Giovanni De Micheli, Sandro Carrara, Ioulia Tzouvadaki, Sébastien Naus

For the first time memristive biosensors developed by the incorporation of scAbs (single-chain antibody fragments) enabling label-free detection of free Prostate Specific Antigen (fPSA) for early-stage detection of prostate cancer (PC) are reported. In add ...

2019

Structural basis of small-molecule inhibition of human multidrug transporter ABCG2

Henning Paul-Julius Stahlberg, Melanie Zechner

ABCG2 is an ATP-binding cassette (ABC) transporter that protects tissues against xenobiotics, affects the pharmacokinetics of drugs and contributes to multidrug resistance. Although many inhibitors and modulators of ABCG2 have been developed, understanding ...

Springer Nature2018

Structure of a zosuquidar and UIC2-bound human-mouse chimeric ABCB1

Henning Paul-Julius Stahlberg

The multidrug transporter ABCB1 (P-glycoprotein) is an ATP-binding cassette transporter that has a key role in protecting tissues from toxic insult and contributes to multidrug extrusion from cancer cells. Here, we report the near-atomic resolution cryo-EM ...

Proceedings of the National Academy of Sciences2018

Cryo-EM structures of a human ABCG2 mutant trapped in ATP-bound and substrate-bound states

Henning Paul-Julius Stahlberg

ABCG2 is a transporter protein of the ATP-binding-cassette (ABC) family that is expressed in the plasma membrane in cells of various tissues and tissue barriers, including the blood-brain, blood-testis and maternal-fetal barriers(1-4). Powered by ATP, it t ...

Springer Nature America, Inc2018

Introducing tolerance to foreign and partly foreign proteins by erythrocyte binding and artificial glycosylations

Kym Lorenz Brünggel

Over the last few years, protein drugs have steadily gained importance in the clinic. Compared to small molecule drugs, protein drugs are taken up by antigen presenting cells, which degrade the proteins into peptides that are then presented on major histoc ...

EPFL2018