Last update 01 Nov 2024

SLC16A4 x MCT1

Last update 01 Nov 2024

Basic Info

Related Targets

SLC16A4MCT1

Drugs associated with SLC16A4 x MCT1

NGY-091

Target

MCT1 x SLC16A4

Mechanism

MCT1 inhibitors [+1]

Active Org.

Nirogy Therapeutics, Inc.

Originator Org.

Nirogy Therapeutics, Inc.

Active Indication

Neoplasms

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with SLC16A4 x MCT1

100 Translational Medicine associated with SLC16A4 x MCT1

0 Patents (Medical) associated with SLC16A4 x MCT1

Literatures (Medical) associated with SLC16A4 x MCT1

01 Nov 2023·Journal of Dairy Science

Benefits of barley straw as a forage for dairy calves before and after weaning

Article

Author: Antúnez-Tort, G ; Cajarville, C ; Fàbregas, F ; Terré, M ; Ahangarani, M A ; Vidal, M ; Bach, A

The aim of this study was to assess the potential consequences on calf intake, performance, behavior, ruminal microbiome, and ruminal epithelium development of combining the inclusion of chopped barley straw and alfalfa hay during the pre- and postweaning periods keeping concentrate to forage ratio constant among dietary treatments. Forty-five Holstein calves (44 ± 5.7 kg of body weight [BW] and 3 ± 1.5 d of age) individually penned were blocked by BW and randomly assigned to a common pellet concentrate fed ad libitum along with one of following forage feeding strategies: barley straw before and after weaning (S-S), barley straw before and alfalfa hay after weaning (S-A), or alfalfa hay before and after weaning (A-A). All calves received the same milk replacer regimen. Forage was supplied in a separated bucket at the rate of 7.5% (preweaning) and 15% (postweaning) of total solid feed intake of the previous day. Feed intake and BW were recorded daily and weekly, respectively. Rumen samples were obtained via a stomach tube at 53, 66, and 87 d and were composite in 3 samples of 5 animals each for subsequent rumen microbiome analysis. A rumen epithelium sample was taken by endoscopy at 90 d to assess gene expression of OCLN, CLDN4, SLC9A1, SLC9A3, SLC16A1, SLC16A4, IL6, and TGFB1. Data were analyzed with a mixed-effects model accounting for the fixed effects of block, forage, week of study, and their interaction, and calf as a random effect. The type of forage fed did not affect concentrate feed, forage, or total DM intake before weaning. However, S-A and A-A calves consumed less concentrate feed and S-A calves grew at a lower rate after weaning than S-S calves. Expression of the gene coding for SLC16A1 in the rumen epithelium was greatest in S-S among treatments. Rumen microbiome did not differ among treatments, while the relative abundance of Acidaminococcus and Selenomas genera increased, while Alloprevotella, Bifidobaterium, Olsenella, and Succiclasticum genera decreased with age. In conclusion, feeding barley straw before and after weaning was more effective than feeding alfalfa hay in promoting concentrate feed intake after weaning and fostering an increase in the expression of SLC16A1 in the rumen epithelium.

12 Jan 2023·Journal of Medicinal ChemistryQ1 · MEDICINE

Indole Derivatives as New Structural Class of Potent and Antiproliferative Inhibitors of Monocarboxylate Transporter 1 (MCT1; SLC16A1)

Q1 · MEDICINE

Article

Author: Pahnke, Jens ; Juvale, Kapil ; Puri, Sachin ; Stefan, Katja ; Khan, Sharuk L. ; Stefan, Sven Marcel

The solute carrier (SLC) monocarboxylate transporter 1 (MCT1; SLC16A1) represents a promising target for the treatment of cancer; however, the MCT1 modulator landscape is underexplored with only roughly 100 reported compounds. To expand the knowledge about MCT1 modulation, we synthesized a library of 16 indole-based molecules and subjected these to a comprehensive biological assessment platform. All compounds showed functional inhibitory activities against MCT1 at low nanomolar concentrations and great antiproliferative activities against the MCT1-expressing cancer cell lines A-549 and MCF-7, while the compounds were selective over MCT4 (SLC16A4). Lead compound 24 demonstrated a greater potency than the reference compound, and molecular docking revealed strong binding affinities to MCT1. Compound 24 led to cancer cell cycle arrest as well as apoptosis, and it showed to sensitize these cancer cells toward an antineoplastic agent. Strikingly, compound 24 had also significant inhibitory power against the multidrug transporter ABCB1 and showed to reverse ABCB1-mediated multidrug resistance (MDR).

01 Feb 2019·Pflügers Archiv - European Journal of PhysiologyQ4 · MEDICINE

Involvement of butyrate in electrogenic K+ secretion in rat rectal colon

Q4 · MEDICINE

Article

Author: Hayashi, Mikio ; Matsuda, Hiroko ; Inagaki, Akihiro ; Andharia, Naaz

Short-chain fatty acids (SCFAs), such as acetate, propionate, and butyrate, are synthesized from dietary carbohydrates by colonic bacterial fermentation. These SCFAs supply energy, suppress cancer, and affect ion transport. However, their roles in ion transport and regulation in the intracellular environment remain unknown. In order to elucidate the roles of SCFAs, we measured short-circuit currents (I_SC) and performed RT-PCR and immunohistochemical analyses of ion transporters in rat rectal colon. The application of 30 mM butyrate shifted I_SC in a negative direction, but did not attenuate the activity of epithelial Na⁺ channels (ENaC). The application of bumetanide, a Na⁺-K⁺-2Cl^- cotransporter inhibitor, to the basolateral side reduced the negative I_SC shift induced by butyrate. The application of XE991, a KCNQ-type K⁺ channel inhibitor, to the apical side decreased the I_SC shift induced by butyrate in a dose-dependent manner. The I_SC shift was independent of HCO₃^- and insensitive to ibuprofen, an SMCT1 inhibitor. The mucosa from rat rectal colon expressed mRNAs of H⁺-coupled monocarboxylate transporters (MCT1, MCT4, and MCT5, also referred to as SLC16A1, SLC16A3, and SLC16A4, respectively). RT-PCR and immunofluorescence analyses demonstrated that KCNQ2 and KCNQ4 localized to the apical membrane of surface cells in rat rectal colon. These results indicate that butyrate, which may be transported by H⁺-coupled monocarboxylate transporters, activates K⁺ secretion through KCNQ-type K⁺ channels on the apical membrane in rat rectal colon. KCNQ-type K⁺ channels may play a role in intestinal secretion and defense mechanisms in the gastrointestinal tract.

Analysis

Perform a panoramic analysis of this field.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis