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CREBBP focused library

CREBBP focused libraryCREB binding protein (CREBBP) is a coactivator of transcription factor CREB that activates genes in cAMP transcriptional pathway. The coactivator binds to transcription factor activation domains positions histone acetyltransferases near specific nucleosomes in target gene promoter regions, recognizing the acetylated lysine residue.

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Halogen-Enriched Fragments

Halogen-Enriched Fragment LibraryOur Halogen-Enriched Fragment Library comprises 430 brominated fragments that can explore binding sites for favorable halogen bond interactions to identify unique binding modes that are complementary to those obtained from classical fragment-based screening.
 

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Chelator Fragment Library

Chelator Fragments LibraryFragment-based lead design (FBLD) could be used to identify new metal-binding groups for metalloenzyme inhibitors. Several small-molecule chelators have been shown to effectively inhibit metalloproteins, therefore the design,

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DNMT1 and DNMT3b Libraries

DNMT focused librariesEnzymes involved in the epigenetic regulation of the genome represent promising starting points for therapeutic intervention by small molecules, and DNA methyltransferases (DNMT) are emerging targets for the development of a new class of cancer therapeutics.

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BRD4 Focused Library

Bromodomain-containing Protein 4 (BRD4)Epigenetic regulators are new popular targets for cancer treatment. One of the promising epigenetic drug targets is Bromodomain-containing Protein 4 (BRD4) that binds to acetylated histone lysine residues and stimulates transcriptional elongation leading to expression of growth-promoting genes. 

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General fragments library

Supplier stockUPDATED! The library has been updated by 384 fragments!
The central purpose of this specially designed Fragment Library is to provide

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Catalogs & Booklets
This section contains information on current Otava's products and services (downloadable files in PDF format).




 
Glycomimetics Focused Library

Glycomimetics Focused LibrarySeveral glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept has inspired the development of important classes of therapeutics, such as anti-influenza, anti-inflammatory, Gaucher’s disease, hepatitis and cancer drugs.

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HATs Focused Library

Histone Acetyltransferase target-focused libraryPost-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyltransferases (HATs) catalyze the acetylation of histones on specific lysine residues. 

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Liver X Receptor Beta Library

Liver X receptor β (LXR Beta) modulatorsLiver X receptors (LXRs) are nuclear receptors that regulate the metabolism of cholesterol and bile acids. LXRs function as nuclear cholesterol sensors that are activated in response to elevated intracellular cholesterol levels in multiple cell types.

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HDAC Focused Libraries

GPCR focused librariesClassical histone deacetylases (HDACs classes I, II, and IV) are a promising novel class of epigenetic anti-cancer drug targets. Inhibition of histone deacetylases results in hyperacetylation of histones and modulates gene expression by creating an open chromatin state that leads to expression of previously silenced genes.

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DOT1L Focused Library

GPCR focused librariesHistone methyltransferases are promising epigenetic drug targets. Several drugs that inhibit histone methyltransferases have been developed for anticancer therapy. DOT1L histone H3 methyltransferase methylates lysine 79 on histone H3 (H3K79), within the globular histone domain upon which DNA is wrapped.

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Inhibitors
inhib.jpgOTAVA offers a number of INHIBITORS and other biologically active compounds modulating activity of distinct macromolecular targets