Gergely Gyimesi
YOU?
Author Swipe
View article: Polypharmacology translates between species and phylogenetic distance: A functional, bioinformatic, and structural study on organic anion transporting polypeptides
Polypharmacology translates between species and phylogenetic distance: A functional, bioinformatic, and structural study on organic anion transporting polypeptides Open
Recently, we postulated the existence of 'multitarget binding sites', reoccurring structural motifs that interconnect otherwise structurally, functionally, and/or phylogenetically distant proteins. In this study, we functionally assessed a…
View article: The Concise Guide to PHARMACOLOGY 2023/24: Transporters
The Concise Guide to PHARMACOLOGY 2023/24: Transporters Open
The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and over 6000…
View article: Genetic studies of paired metabolomes reveal enzymatic and transport processes at the interface of plasma and urine
Genetic studies of paired metabolomes reveal enzymatic and transport processes at the interface of plasma and urine Open
View article: SLC66 Lysosomal amino acid transporters in GtoPdb v.2023.1
SLC66 Lysosomal amino acid transporters in GtoPdb v.2023.1 Open
This is a family of 5 evolutionarily related proteins. Their structural similarities suggest that they are transporters. Biochemical evidence supports transporter activity for SLC66A1 (LAAT1) and SLC66A4 (CTNS; Cystinosin), primarily expor…
View article: Transporter-Mediated Drug Delivery
Transporter-Mediated Drug Delivery Open
Transmembrane transport of small organic and inorganic molecules is one of the cornerstones of cellular metabolism. Among transmembrane transporters, solute carrier (SLC) proteins form the largest, albeit very diverse, superfamily with ove…
View article: Transporter-Mediated Drug Delivery
Transporter-Mediated Drug Delivery Open
Transmembrane transport of small organic and inorganic molecules is one of the cornerstones of cellular metabolism. Among transmembrane transporters, solute carrier (SLC) proteins form the largest, albeit very diverse, superfamily with ove…
View article: Systematic in silico discovery of novel solute carrier-like proteins from proteomes
Systematic in silico discovery of novel solute carrier-like proteins from proteomes Open
Solute carrier (SLC) proteins represent the largest superfamily of transmembrane transporters. While many of them play key biological roles, their systematic analysis has been hampered by their functional and structural heterogeneity. Base…
View article: Discovery of novel gating checkpoints in the Orai1 calcium channel by systematic analysis of constitutively active mutants of its paralogs and orthologs
Discovery of novel gating checkpoints in the Orai1 calcium channel by systematic analysis of constitutively active mutants of its paralogs and orthologs Open
In humans, there are three paralogs of the Orai Ca2+ channel that form the core of the store-operated calcium entry (SOCE) machinery. While the STIM-mediated gating mechanism of Orai channels is still under active investigation,…
View article: The Less Well-Known Little Brothers: The SLC9B/NHA Sodium Proton Exchanger Subfamily—Structure, Function, Regulation and Potential Drug-Target Approaches
The Less Well-Known Little Brothers: The SLC9B/NHA Sodium Proton Exchanger Subfamily—Structure, Function, Regulation and Potential Drug-Target Approaches Open
The SLC9 gene family encodes Na + /H + exchangers (NHEs), a group of membrane transport proteins critically involved in the regulation of cytoplasmic and organellar pH, cell volume, as well as systemic acid-base and volume homeostasis. NHE…
View article: Systematic <i>in silico</i> discovery of novel solute carrier-like proteins from proteomes
Systematic <i>in silico</i> discovery of novel solute carrier-like proteins from proteomes Open
Solute carrier (SLC) proteins represent the largest superfamily of transmembrane transporters. While many of them play key biological roles, their systematic analysis has been hampered by their functional and structural heterogeneity. Base…
View article: Dissecting gating mechanisms of Orai calcium channel paralogs using constitutively active Orai mutants that mimic STIM1-gated state
Dissecting gating mechanisms of Orai calcium channel paralogs using constitutively active Orai mutants that mimic STIM1-gated state Open
In humans, there are three paralogs of the Orai Ca 2+ channel, which lie at the heart of the store-operated calcium entry (SOCE) machinery. While the STIM-mediated gating mechanism of Orai channels is still being actively investigated, sev…
View article: SLC66 Lysosomal amino acid transporters in GtoPdb v.2021.2
SLC66 Lysosomal amino acid transporters in GtoPdb v.2021.2 Open
This is a family of 5 evolutionarily related proteins. Their structural similarities suggest that they are transporters. Biochemical evidence supports transporter activity for SLC66A1 (LAAT1) and SLC66A4 (CTNS; Cystinosin). The functions o…
View article: Sequence Features of Mitochondrial Transporter Protein Families
Sequence Features of Mitochondrial Transporter Protein Families Open
Mitochondrial carriers facilitate the transfer of small molecules across the inner mitochondrial membrane (IMM) to support mitochondrial function and core cellular processes. In addition to the classical SLC25 (solute carrier family 25) mi…
View article: Inactivation-mimicking block of the epithelial calcium channel TRPV6
Inactivation-mimicking block of the epithelial calcium channel TRPV6 Open
Small-molecule piperazine derivatives mimic inactivation by calmodulin to selectively and potently block TRPV6 channels.
View article: SLC66 Lysosomal amino acid transporters (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database
SLC66 Lysosomal amino acid transporters (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database Open
This is a family of 5 evolutionarily related proteins. Their structural similarities suggest that they are transporters. Biochemical evidence supports transporter activity for SLC66A1 (LAAT1) and SLC66A4 (CTNS; Cystinosin). The functions o…
View article: Sequence Features of Mitochondrial Transporter Protein Families
Sequence Features of Mitochondrial Transporter Protein Families Open
Mitochondrial carriers facilitate the transfer of small molecules across the inner mitochondrial membrane (IMM) to support mitochondrial function and core cellular processes. In addition to the classical mitochondrial carrier family SLC25,…
View article: Sodium-coupled glucose transport, the SLC5 family, and therapeutically relevant inhibitors: from molecular discovery to clinical application
Sodium-coupled glucose transport, the SLC5 family, and therapeutically relevant inhibitors: from molecular discovery to clinical application Open
Sodium glucose transporters (SGLTs) belong to the mammalian solute carrier family SLC5. This family includes 12 different members in human that mediate the transport of sugars, vitamins, amino acids, or smaller organic ions such as choline…
View article: Correction: Unraveling the structural elements of pH sensitivity and substrate binding in the human zinc transporter SLC39A2 (ZIP2).
Correction: Unraveling the structural elements of pH sensitivity and substrate binding in the human zinc transporter SLC39A2 (ZIP2). Open
VOLUME 294 (2019) PAGES 8046–8063 Due to publisher error, Figs. 4 and 5 were duplicated. This error has been corrected online. Unraveling the structural elements of pH sensitivity and substrate binding in the human zinc transporter SLC39A2…
View article: Vitamin C Alimentation via SLC Solute Carriers
Vitamin C Alimentation via SLC Solute Carriers Open
In humans, ascorbic acid is an essential vitamin, antioxidant, and cofactor of a variety of metal ion–dependent enzymatic reactions. In this review, the transport of L-ascorbic acid is described from food to target cells. Transport of asco…
View article: Chapter 3 Vitamin C Alimentation via SLC Solute Carriers
Chapter 3 Vitamin C Alimentation via SLC Solute Carriers Open
Although mortality rates from pneumonia and sepsis are decreasing in many parts of the world, the incidence of these conditions continues to rise, likely due to an increasingly ageing population. Case reports and observational studies indi…
View article: Unraveling the structural elements of pH sensitivity and substrate binding in the human zinc transporter SLC39A2 (ZIP2)
Unraveling the structural elements of pH sensitivity and substrate binding in the human zinc transporter SLC39A2 (ZIP2) Open
The transport and ion-coupling mechanisms of ZIP transporters remain largely uncharacterized. Previous work in our laboratory has revealed that the solute carrier family 39 member A2 (SLC39A2/ZIP2) increases its substrate transport rate in…
View article: ORAI1 channel gating and selectivity is differentially altered by natural mutations in the first or third transmembrane domain
ORAI1 channel gating and selectivity is differentially altered by natural mutations in the first or third transmembrane domain Open
Key points Gain‐of‐function mutations in the highly selective Ca 2+ channel ORAI1 cause tubular aggregate myopathy (TAM) characterized by muscular pain, weakness and cramping. TAM‐associated mutations in ORAI1 first and third transmembrane…
View article: A novel proton transfer mechanism in the SLC11 family of divalent metal ion transporters
A novel proton transfer mechanism in the SLC11 family of divalent metal ion transporters Open
View article: ABCMdb reloaded: updates on mutations in ATP binding cassette proteins
ABCMdb reloaded: updates on mutations in ATP binding cassette proteins Open
http://abcm2.hegelab.org.
View article: Access Path to the Ligand Binding Pocket May Play a Role in Xenobiotics Selection by AhR
Access Path to the Ligand Binding Pocket May Play a Role in Xenobiotics Selection by AhR Open
Understanding of multidrug binding at the atomic level would facilitate drug design and strategies to modulate drug metabolism, including drug transport, oxidation, and conjugation. Therefore we explored the mechanism of promiscuous bindin…
View article: The Hydroxyl Side Chain of a Highly Conserved Serine Residue Is Required for Cation Selectivity and Substrate Transport in the Glial Glutamate Transporter GLT-1/SLC1A2
The Hydroxyl Side Chain of a Highly Conserved Serine Residue Is Required for Cation Selectivity and Substrate Transport in the Glial Glutamate Transporter GLT-1/SLC1A2 Open
Glutamate transporters maintain synaptic concentration of the excitatory neurotransmitter below neurotoxic levels. Their transport cycle consists of cotransport of glutamate with three sodium ions and one proton, followed by countertranspo…
View article: A Call for Systematic Research on Solute Carriers
A Call for Systematic Research on Solute Carriers Open