Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase

Bioorganic & Medicinal Chemistry Letters
James E TarverKenneth G Carson

Abstract

A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.

References

Mar 12, 2010·Journal of Medicinal Chemistry·John G AllenPhilip Babij
Feb 8, 2013·Nature Medicine·Roland Baron, Michaela Kneissel
Jul 2, 2014·Nature Reviews. Drug Discovery·Michael Kahn
Jan 13, 2015·Journal of Endocrinological Investigation·E CairoliI Chiodini
Mar 4, 2015·Nature·Satoshi KakugawaJean-Paul Vincent
Apr 3, 2015·Journal of Cellular Biochemistry·Robert Brommage
Aug 19, 2015·Metabolism: Clinical and Experimental·Polyzois MakrasAthanasios D Anastasilakis
Jan 30, 2016·Bioorganic & Medicinal Chemistry Letters·Qiang HanKenneth G Carson

❮ Previous
Next ❯

Citations

Jul 17, 2019·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Sofia Movérare-SkrticClaes Ohlsson
Dec 27, 2019·Journal of Pineal Research·Yuguang ZhaoEdith Yvonne Jones
Jan 10, 2019·Bone Research·Robert BrommageQingyun Liu
Oct 10, 2020·Communications Biology·Yuguang ZhaoEdith Yvonne Jones
Mar 2, 2021·Molecular Metabolism·Yuguang ZhaoE Yvonne Jones
Mar 31, 2021·Journal of Medicinal Chemistry·Elliott D BaylePaul V Fish
Apr 23, 2021·Future Medicinal Chemistry·Yuguang ZhaoPaul V Fish
Jun 4, 2021·Nature·Dustin J FlanaganOwen J Sansom
Jul 6, 2021·Journal of Bone and Mineral Research : the Official Journal of the American Society for Bone and Mineral Research·Roy B ChoiAlexander G Robling
Jun 26, 2018·ACS Medicinal Chemistry Letters·Radu M SuciuBenjamin F Cravatt

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Bioorganic & Medicinal Chemistry Letters
Qiang HanKenneth G Carson
Bioorganic & Medicinal Chemistry Letters
Steven W KortumRuth E TenBrink
Bioorganic & Medicinal Chemistry Letters
William J McClellanMichael R Michaelides
© 2022 Meta ULC. All rights reserved