Results 11 to 20 of about 4,236,805 (394)

Current ADC Linker Chemistry [PDF]

open access: yesPharmaceutical Research, 2015
The list of ADCs in the clinic continues to grow, bolstered by the success of first two marketed ADCs: ADCETRIS® and Kadcyla®. Currently, there are 40 ADCs in various phases of clinical development. However, only 34 of these have published their structures.
Jain, Nareshkumar   +3 more
openaire   +3 more sources

Equivariant 3D-conditional diffusion model for molecular linker design [PDF]

open access: yesNature Machine Intelligence, 2022
Fragment-based drug discovery has been an effective paradigm in early-stage drug development. An open challenge in this area is designing linkers between disconnected molecular fragments of interest to obtain chemically relevant candidate drug molecules.
Ilia Igashov   +8 more
semanticscholar   +1 more source

Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation

open access: yesACS Medicinal Chemistry Letters, 2022
A platform to accelerate optimization of proteolysis targeting chimeras (PROTACs) has been developed using a direct-to-biology (D2B) approach with a focus on linker effects.
Charles E. Hendrick   +8 more
semanticscholar   +1 more source

E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points

open access: yesFrontiers in Chemistry, 2021
Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new and exciting class of therapeutic agents that promise to significantly impact drug discovery.
Aleša Bricelj   +4 more
semanticscholar   +1 more source

Architecture of the linker-scaffold in the nuclear pore

open access: yesScience, 2022
Description INTRODUCTION In eukaryotic cells, the selective bidirectional transport of macromolecules between the nucleus and cytoplasm occurs through the nuclear pore complex (NPC).
S. Petrovic   +12 more
semanticscholar   +1 more source

Linker Design Impacts Antibody-Drug Conjugate Pharmacokinetics and Efficacy via Modulating the Stability and Payload Release Efficiency

open access: yesFrontiers in Pharmacology, 2021
The development of antibody-drug conjugates (ADCs) has significantly been advanced in the past decade given the improvement of payloads, linkers and conjugation methods.
Dian Su, Donglu Zhang
semanticscholar   +1 more source

A Kinetic Model for the Enzymatic Action of Cellulase [PDF]

open access: yes, 2009
We develop a mechanochemical model for the dynamics of cellulase, a two-domain enzyme connected by a peptide linker, as it extracts and hydrolyzes a cellulose polymer from a crystalline substrate.
Makarov, Dmitrii E.   +2 more
core   +2 more sources

Engineering a Highly Defective Stable UiO-66 with Tunable Lewis- Brønsted Acidity: The Role of the Hemilabile Linker

open access: yesJournal of the American Chemical Society, 2020
The stability of metal–organic frameworks (MOFs) typically decreases with an increasing number of defects, limiting the number of defects that can be created and limiting catalytic and other applications. Herein, we use a hemilabile (Hl) linker to create
Xiao Feng   +14 more
semanticscholar   +1 more source

Modulating Linker Composition of Haptens Resulted in Improved Immunoassay for Histamine. [PDF]

open access: yes, 2019
Histamine (HA) is an important food contaminant generated during food fermentation or spoilage. However, an immunoassay for direct (derivatization free) determination of HA has rarely been reported due to its small size to induce the desired antibodies ...
Dong, Jie-Xian   +9 more
core   +1 more source

Development of applicable thiol-linked antibody–drug conjugates with improved stability and therapeutic index

open access: yesDrug Delivery, 2022
Maleimides are typically applicable for coupling with reactive thiol moieties of antibodies in antibody–drug conjugates (ADCs) via the thiol-Michael click chemistry.
Yanming Wang   +6 more
doaj   +1 more source

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