SLC transporters: structure, function, and drug discovery

C Colas, PMU Ung, A Schlessinger - Medchemcomm, 2016 - pubs.rsc.org
The human solute carrier (SLC) transporters are important targets for drug development.
Structure-based drug discovery for SLC transporters requires the description of their …

Structures of the TMC-1 complex illuminate mechanosensory transduction

H Jeong, S Clark, A Goehring… - Nature, 2022 - nature.com
The initial step in the sensory transduction pathway underpinning hearing and balance in
mammals involves the conversion of force into the gating of a mechanosensory transduction …

Intestinal serotonin and fluoxetine exposure modulate bacterial colonization in the gut

TC Fung, HE Vuong, CDG Luna, GN Pronovost… - Nature …, 2019 - nature.com
The gut microbiota regulates levels of serotonin (5-hydroxytryptamine (5-HT)) in the
intestinal epithelium and lumen,,,–. However, whether 5-HT plays a functional role in …

Molecular modeling of drug–transporter interactions—an international transporter consortium perspective

A Schlessinger, MA Welch… - Clinical …, 2018 - Wiley Online Library
Membrane transporters play diverse roles in the pharmacokinetics and pharmacodynamics
of small‐molecule drugs. Understanding the mechanisms of drug‐transporter interactions at …

Curvature induction and membrane remodeling by FAM134B reticulon homology domain assist selective ER-phagy

RM Bhaskara, P Grumati, J Garcia-Pardo… - Nature …, 2019 - nature.com
Abstract FAM134B/RETREG1 is a selective ER-phagy receptor that regulates the size and
shape of the endoplasmic reticulum. The structure of its reticulon-homology domain (RHD) …

Role of FAM134 paralogues in endoplasmic reticulum remodeling, ER‐phagy, and Collagen quality control

A Reggio, V Buonomo, R Berkane, RM Bhaskara… - EMBO …, 2021 - embopress.org
Degradation of the endoplasmic reticulum (ER) via selective autophagy (ER‐phagy) is vital
for cellular homeostasis. We identify FAM134A/RETREG2 and FAM134C/RETREG3 as ER …

Multiplexed measurement of variant abundance and activity reveals VKOR topology, active site and human variant impact

MA Chiasson, NJ Rollins, JJ Stephany, KA Sitko… - elife, 2020 - elifesciences.org
Vitamin K epoxide reductase (VKOR) drives the vitamin K cycle, activating vitamin K-
dependent blood clotting factors. VKOR is also the target of the widely used anticoagulant …

Structural relationship between the putative hair cell mechanotransduction channel TMC1 and TMEM16 proteins

A Ballesteros, C Fenollar-Ferrer, KJ Swartz - Elife, 2018 - elifesciences.org
The hair cell mechanotransduction (MET) channel complex is essential for hearing, yet it's
molecular identity and structure remain elusive. The transmembrane channel–like 1 (TMC1) …

A direct interaction of cholesterol with the dopamine transporter prevents its out-to-inward transition

T Zeppelin, LK Ladefoged, S Sinning… - PLoS computational …, 2018 - journals.plos.org
Monoamine transporters (MATs) carry out neurotransmitter reuptake from the synaptic cleft,
a key step in neurotransmission, which is targeted in the treatment of neurological disorders …

Structural basis of nucleotide sugar transport across the Golgi membrane

JL Parker, S Newstead - Nature, 2017 - nature.com
Glycosylation is a fundamental cellular process that, in eukaryotes, occurs in the lumen of
both the Golgi apparatus and the endoplasmic reticulum. Nucleotide sugar transporters …