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Ligands
Ligands
Origin of place United Kingdom
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Supplier Biosynth Carbosynth
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Updated 3/2/2022
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Ligands

The ligands product category collects compounds which interact with proteins or nucleic acids at a molecular level. Targets of these ligands include enzymes, ion channels, nuclear receptors, GPCRs, transporters, ligands targeting protein-protein interactions, DNA cross-linkers, and other targets.

 

DNA Cross Linkers
These compounds cause DNA interstrand crosslinks that include natural alkylating agents such as mitomycin C or synthetic agents, such as platinum compounds. These DNA lesions, if left unrepaired, lead to disruption of DNA replication and transcription and therefore have genotoxic and cytotoxic consequences. DNA cross linkers thus have therapeutic applications in treating solid tumors, as well as autoimmune diseases and dermatological conditions. The DNA cross linkers available from Biosynth Carbosynth are listed below.

Enzyme Modulators
Enzyme modulators product range includes enzyme inhibitors and activators of various enzyme classes such as oxidoreductases, transferases, hydrolases, lyases, isomerases and ligases. We offer a rich collection of kinase inhibitors and other enzymes involved in cell signalling, which are key tools for cancer research, cell biology, physiology and others. The latest additions to our enzyme modulators product range include specific inhibitors of enzymes involved in DNA repair, transcriptional regulation, DNA remodelling, epigenetics, kinase cascades, effector proteins and more.

GPCRs
The compounds listed below interact with G-protein coupled receptors (GPCRs), also known as 7 transmembrane (7-TM) receptors. GPCRs are activated by specific ligands, which cause a conformational change in the receptor and activation of the coupled G-protein at the intracellular site of the membrane, which in turn triggers a cascade of downstream reactions. The ligands listed here are targeting multiple subfamilies of GCPRs such as acetylcholine receptors, adenosine receptors, adrenergic receptors, cannabinoid and opioid receptors, chemokine receptors, dopamine receptors, serotonin receptors, histamine receptors, metabotropic glutamate receptors, peptide receptors, prostanoid receptors, purinergic receptors, smoothened receptors, and other GCPRs.

Ion Channels

Ion channels are transmembrane proteins with the ability to control ion currents across cell membrane. They are essential for maintaining resting membrane potential as well as for generation of action potentials in neurons, muscle and endocrine cells. Our collection of ion channel modulators include blockers of ligand-gated and voltage-gated channels, as well as mechanosensitive, cyclic nucleotide-gated channels and more.

Ion channel modulators therefore modulate or disrupt potassium, sodium and calcium currents as well as chloride and proton gradients across biological membranes. Ion channel modulators are widely used in cardiovascular and neuroscience research.


Nuclear Receptors
The list of compounds below either mimic or block the activity of endogenous ligands of nuclear receptors.  Broadly, nuclear receptors can be grouped into steroid and non-steroid hormone receptors that are regulated by endogenous agonists. Thirdly, nuclear receptors with unknown ligand and mode of action are known as orphan receptors. Ligand-bound nuclear receptors undergo conformational changes and act as transcription factors. These bind to DNA response elements in promoters of target genes to regulate transcription. These compounds have therapeutic potential in reproductive, metabolic and proliferative diseases.

Protein Interactions
Compounds in this list act by modulating the interactions among proteins such as chaperone proteins, heat shock proteins, microtubules, transcription factors, immune checkpoint proteins and cytokines. For example, disruption of structural protein interactions such as microtubules have therapeutic applications in cancer treatment. Furthermore, modulating the interaction of bromodomain-containing proteins has implications on chromatin remodelling and epigenetic regulation. Products in this range include small molecule compounds and antibodies.

Transporters
The products in the transporter category are inhibitors of membrane transport proteins that are moving ions, small molecules and proteins across biological membranes. Transporters are grouped into three classes of ATP-driven transporters: P-type, F-type or V-type ATPases and ATP-binding cassette transporters. The fourth class of transporters are the SLC superfamily of solute carriers that mediate the transport of a variety of solutes, such as inorganic ions, amino acids, sugars and complex organic molecules. 

Other Targets
These compounds act on targets other than 7-TM receptors, nuclear receptors, enzymes, ion channels, protein interactions, transporters and do not have DNA crosslinking activity. Other targets include imidazoline receptors and sigma receptors. This list of compounds also includes products with known applications, but with unknown or non-specific mode of action.
 
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