Multivalent inhibitors for carbohydrate‐processing enzymes: beyond the “lock‐and‐key” concept

SG Gouin - Chemistry–A European Journal, 2014 - Wiley Online Library
During the last decades, tremendous chemical efforts have been dedicated to design
monovalent inhibitors of carbohydrate‐processing enzymes, with comparatively few rewards …

The C‐terminal domains of the NMDA receptor: How intrinsically disordered tails affect signalling, plasticity and disease

XL Warnet, H Bakke Krog… - European Journal of …, 2021 - Wiley Online Library
NMDA receptors are part of the ionotropic glutamate receptor family, and are crucial for
neurotransmission and memory. At the cellular level, the effects of activating these receptors …

Avidity-based bright and photostable light-up aptamers for single-molecule mRNA imaging

B Bühler, J Schokolowski, A Benderoth… - Nature Chemical …, 2023 - nature.com
Fluorescent light-up aptamers (FLAPs) have emerged as valuable tools to visualize RNAs,
but are mostly limited by their poor brightness, low photostability, and high fluorescence …

Effective concentrations enforced by intrinsically disordered linkers are governed by polymer physics

CS Sørensen, M Kjaergaard - Proceedings of the National …, 2019 - National Acad Sciences
Many multidomain proteins contain disordered linkers that regulate interdomain contacts,
and thus the effective concentrations that govern intramolecular reactions. Effective …

Deconstructing behavioral neuropharmacology with cellular specificity

BC Shields, E Kahuno, C Kim, PF Apostolides, J Brown… - Science, 2017 - science.org
INTRODUCTION Animal behavior is mediated by molecular, cellular, and circuit
components of the brain. However, because many proteins are broadly expressed, it has …

Synthesis, spectroscopic characterizations, carbonic anhydrase II inhibitory activity, anticancer activity and docking studies of new Schiff bases of sulfa drugs

S Alyar, ÜÖ Özmen, Ş Adem, H Alyar, E Bilen… - Journal of Molecular …, 2021 - Elsevier
Herein we present the synthesis, and biological evaluation of new Schiff bases incorporating
(2‑hydroxy-5-methylbenzaldehyde sulfisoxazole (S2M-S1) and 2‑hydroxy-5 …

Intrinsically disordered linkers control tethered kinases via effective concentration

M Dyla, M Kjaergaard - Proceedings of the National …, 2020 - National Acad Sciences
Kinase specificity is crucial to the fidelity of signaling pathways, yet many pathways use the
same kinases to achieve widely different effects. Specificity arises in part from the enzymatic …

Designing nanomolar antagonists of DC-SIGN-mediated HIV infection: ligand presentation using molecular rods

S Ordanini, N Varga, V Porkolab, M Thépaut… - Chemical …, 2015 - pubs.rsc.org
DC-SIGN antagonists were designed combining one selective monovalent glycomimetic
ligand with trivalent dendrons separated by a rigid core of controlled length. The design …

Structural basis for kinesin-1: cargo recognition

S Pernigo, A Lamprecht, RA Steiner, MP Dodding - Science, 2013 - science.org
Kinesin-mediated cargo transport is required for many cellular functions and plays a key role
in pathological processes. Structural information on how kinesins recognize their cargoes is …

Emerging trends in enzyme inhibition by multivalent nanoconstructs

N Kanfar, E Bartolami, R Zelli, A Marra… - Organic & …, 2015 - pubs.rsc.org
Multivalent nanoconstructs, extensively used for enhancing the recognition of biomolecular
targets, have been recently exploited for enzyme inhibition showing interesting properties …