Albert Einstein College of Medicine

Industrial Research Limited

Victoria Link Limited

Other

The Johns Hopkins University

Alber Einslein College of Medicine

Callaghan Innovation Research Limited

Albert Einstein College of Medecine of Yeshiva University

Vern L Schramm

Peter Charles Tyler

Richard Hubert Furneaux

Gary Brian Evans

Keith Clinch

Shivali Ashwin Gulab

Anthony A Sauve

Anthony Sauvé

Jef D Boeke

Ivana Celic

Steven D Schwartz

Benjamin B Braunheim

Alistair Ian Longshaw

Peter Michael Kelly

Olga Vladimirovna Zubkova

Jennifer Mary Mason

Dirk Henning Lenz

Anthony David Woolhouse

Quan Du

Richard Fröhlich

Chandan Guha

Setu Roday

Kami Kim

Ben William Greatrex

Douglas Ronald Crump

Benjamin Horenstein

Antti Marko Haapalainen

Richard Frohlich

Shivall Ashwah Ashwin Gulab

Zhen Wang

Shanzhi Wang

Farah Lamiable-Oulaidi

Karl Jürgen Shaffer

Ashna Ashneen Khan

Richard Hurbert Furneaux

Richard Froehlich

Simon Peter Harold Mee

Provided herein are inhibitors of DNA methyltransferase 1 (an enzyme responsible for the maintenance of DNA CpG methylation marks in human cells) and their use for inhibiting DNA methyltransferase 1. The invention relates to compounds, pharmaceutical compositions, and methods for inhibiting DNA methyltransferase 1. The inhibitors are compounds of the general formula: 

Inhibitors of DNMT1 as anticancer therapeutic agents

Methods of treating infections due to(), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering to the subject an inhibitor ofMTAN (5'-methylthioadenosine nucleosidase) having the structure of formula (I) 

Treatment of helicobacter pylori infections

Methods and systems for obtaining inhibitors of human DNA methyltransferase 1 (DNMT1) are disclosed where the methods involve designing compounds that resemble the DNMT1 transition state.

DNA methyltransferase 1 transition state structure and uses thereof

Methods of treating infections due to(), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering inhibitors ofMTAN (5'-methylthioadenosine nucleosidase) to the subject.

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Methods of treating infections due to(), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering inhibitors ofMTAN (5'-methylthioadenosine nucleosidase) to the subject, where the inhibitors have the structure 

Treatment of H. pylori infections using MTAN inhibitors

The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (1) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5&#x2032;-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.

3-hydroxypyrrolidine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase

Methods and devices are disclosed for treating or preventing infections in a subject due tousing coformycin analogs and inhibitors of5'-methylthioadenosine deaminase (MTADA).

The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5&#x2032;-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.

The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5'-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.

Methods, assays and compounds for treating bacterial infections by inhibiting methylthioinosine phosphorylase

The invention relates to the treatment of cancer using an inhibitor of 5'-methylthioadenosine phosphorylase (MTAP). The invention particularly relates to the treatment of prostate cancer and head and neck cancer.

Methods of treating cancer using inhibitors of 5'-methylthioadenosine phosphorylase

Inhibitors of saporin-L1 are disclosed, as are related compositions and uses thereof, in particular in cancer therapy that employs saporin-L1-linked immunotoxins.

Saporin-L1 inhibitors and uses thereof

The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.

Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases

Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.

SIR2 regulation

Provided are methods of designing a putative inhibitor of a 5'-methylthioadenosine/S-adenosylhomocysteine nucleosidase. The methods comprise designing a chemically stable compound that resembles the charge and geometry of the 5&#x2032;-methylthioadenosine/S-adenosylhomocysteine nucleosidase transition state. Also provided are methods of inhibiting 5&#x2032;-methylthioadenosine/S-adenosylhomocysteine nucleosidases using the inhibitors found by the above methods.

Transition state structure of 5'-methylthioadenosine/s-adenosylhomocysteine nucleosidases

This application provides fluorescent probes, substrates, kits and methods for detecting the presence or absence of an enzyme, such as ricin, that catalyzes the release of adenine from a GAGA RNA tetraloop.

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New Rochelle, NY, United States of America

Vern L Schramm