Membrane transporters in drug development and as determinants of precision medicine

A Galetin, KLR Brouwer, D Tweedie… - Nature Reviews Drug …, 2024 - nature.com
The effect of membrane transporters on drug disposition, efficacy and safety is now well
recognized. Since the initial publication from the International Transporter Consortium …

Targeting SLC transporters: small molecules as modulators and therapeutic opportunities

A Schlessinger, N Zatorski, K Hutchinson… - Trends in biochemical …, 2023 - cell.com
Solute carrier (SLCs) transporters mediate the transport of a broad range of solutes across
biological membranes. Dysregulation of SLCs has been associated with various …

Cryo-EM structures of human organic anion transporting polypeptide OATP1B1

Z Shan, X Yang, H Liu, Y Yuan, Y **ao, J Nan… - Cell Research, 2023 - nature.com
Members of the solute carrier organic anion transporting polypeptide (OATPs) family
function as transporters for a large variety of amphipathic organic anions including …

Molecular basis of polyspecific drug and xenobiotic recognition by OCT1 and OCT2

Y Suo, NJ Wright, H Guterres, JG Fedor… - Nature structural & …, 2023 - nature.com
A wide range of endogenous and xenobiotic organic ions require facilitated transport
systems to cross the plasma membrane for their disposition. In mammals, organic cation …

Structural basis of promiscuous substrate transport by Organic Cation Transporter 1

YC Zeng, M Sobti, A Quinn, NJ Smith… - Nature …, 2023 - nature.com
Abstract Organic Cation Transporter 1 (OCT1) plays a crucial role in hepatic metabolism by
mediating the uptake of a range of metabolites and drugs. Genetic variations can alter the …

Molecular basis for selective uptake and elimination of organic anions in the kidney by OAT1

JL Parker, T Kato, G Kuteyi, O Sitsel… - Nature Structural & …, 2023 - nature.com
In mammals, the kidney plays an essential role in maintaining blood homeostasis through
the selective uptake, retention or elimination of toxins, drugs and metabolites. Organic anion …

Structural insights into human organic cation transporter 1 transport and inhibition

S Zhang, A Zhu, F Kong, J Chen, B Lan, G He, K Gao… - Cell discovery, 2024 - nature.com
The human organic cation transporter 1 (hOCT1), also known as SLC22A1, is integral to
hepatic uptake of structurally diversified endogenous and exogenous organic cations …

The substrate and inhibitor binding mechanism of polyspecific transporter OAT1 revealed by high-resolution cryo-EM

T Dou, T Lian, S Shu, Y He, J Jiang - Nature structural & molecular …, 2023 - nature.com
Organic anion transporters (OATs) of the SLC22 family have crucial roles in the transport of
organic anions, including metabolites and therapeutic drugs, and in transporter-mediated …

Structural and functional annotation of solute carrier transporters: implication for drug discovery

V Dvorak, G Superti-Furga - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
ABSTRACT Introduction Solute carriers (SLCs) represent the largest group of membrane
transporters in the human genome. They play a central role in controlling the …

Permeability of metformin across an in vitro blood–brain barrier model during normoxia and oxygen-glucose deprivation conditions: role of organic cation transporters …

S Sharma, Y Zhang, KA Akter, S Nozohouri, SR Archie… - Pharmaceutics, 2023 - mdpi.com
Our lab previously established that metformin, a first-line type two diabetes treatment,
activates the Nrf2 pathway and improves post-stroke recovery. Metformin's brain …