Ocular Diseases small molecules library

Description

ChemDiv’s library of small molecule agents targeting pathways involved in eye disease development contains 13,000 compounds.

Our comprehensive small molecule library specifically targets a range of ocular diseases, offering a diverse selection of compounds designed for the therapeutic intervention of a range of eye diseases.

Diabetic Macular Edema (DME):

DME arises as a complication of diabetic retinopathy, the most prevalent diabetic eye disease, and a leading cause of irreversible blindness. Vascular adhesion protein-1 (VAP-1), a homodimeric sialylated glycoprotein, is implicated in DME development. Inhibiting the human VAP-1 enzyme is considered a promising approach for the treatment of DME.

Cataract:

Cataract is a progressive eye condition characterized by the lens becoming opaque, leading to reduced transparency, and potentially affecting one or both eyes. Several discovery programs worldwide have been focusing on investigating the protective role of Aldose Reductase inhibitors in preventing cataract formation in diabetic patients.

Glaucoma:

Glaucoma is characterized by irreversible neurodegeneration, involving retinal nerve fiber layer thinning, optic nerve head cupping, and retinal ganglion cell (RGC) death. Ocular hypertension, or elevated intraocular pressure (IOP), is a major risk factor for most types of glaucoma. Established treatment methods include IOP reduction through topical drugs, laser therapy, and surgical intervention. Key protein targets and pathways include Carbonic Anhydrase (CA) inhibition, which decrease aqueous humor (AH) production, and Rho-associated protein kinase (ROCK) II inhibition, which enhances conventional AH outflow pathways, increases retinal blood flow, and provides neuronal protection against stress.

Age-Related Macular Degeneration (AMD):

AMD occurs due to abnormalities in the retinal pigment epithelium, leading to damage in the macula [1,2]. AD is a multifactorial disorder without a predominant etiological factor and a leading cause of central vision loss in patients aged 65 or older [3,4].

Our small molecule library is a meticulously curated collection of 13,000 compounds, specifically designed for targeted drug discovery in ocular diseases. It encompasses a diverse array of small molecule compounds, focusing on seven distinct targets related to four major ocular conditions. The library's composition reflects the latest advancements in ocular therapeutics, incorporating emerging targets such as retinol-binding protein 4 (RBP4), which plays a crucial role in the transport of vitamin A to the retina, factor D, a key enzyme in the alternative complement pathway implicated in ocular inflammation, and the Vascular Endothelial Growth Factor (VEGF) pathway, known for its significance in neovascular diseases. The design of this screening library is guided by cutting-edge research in ophthalmology, ensuring that the included compounds are not only diverse but also relevant to current and emerging needs in the treatment of ocular diseases. This library stands as a valuable resource for researchers and pharmaceutical companies aiming to develop novel treatments for complex eye conditions, offering a broad spectrum of chemical entities to explore and potentially revolutionize therapeutics against eye diseases.

Publications

1.        Haddad S, Chen CA, Santangelo SL, Seddon JM. The genetics of age-related macular degeneration: a review of progress to date. Surv Ophthalmol. 2006 Jul-Aug;51(4):316-63. doi: 10.1016/j.survophthal.2006.05.001. PMID: 16818082.

2.        Cheng KJ, Hsieh CM, Nepali K, Liou JP. Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye. J Med Chem. 2020 Oct 8;63(19):10533-10593. doi: 10.1021/acs.jmedchem.9b01033. Epub 2020 Jun 2. PMID: 32482069.

3.        Chou R, Dana T, Bougatsos C, Grusing S, Blazina I. Screening for Impaired Visual Acuity in Older Adults: Updated Evidence Report and Systematic Review for the US Preventive Services Task Force. JAMA. 2016 Mar 1;315(9):915-33. doi: 10.1001/jama.2016.0783. PMID: 26934261.

Rastoin O, Pagès G, Dufies M. Experimental Models in Neovascular Age Related Macular Degeneration. Int J Mol Sci. 2020 Jun 29;21(13):4627. doi: 10.3390/ijms21134627. PMID: 32610682; PMCID: PMC7370120