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Broad Applications of PROTACS for Targeted Protein Degradation Employing a Molecular Glue-Linker-Warhead Approach
This technology is a high-affinity E3-ligase binder, which has been optimized toward the specific proteolysis targeting chimera (PROTAC) mediated degradation of particular proteins. A PROTAC is a heterobifunctional molecule composed of two active domains and a linker, capable of removing specific unwanted proteins. This technology opens the door for...
Published: 2/6/2024
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Inventor(s): Christopher Hulme, Kevin Schofield
Keywords(s):
Category(s): Technology Classifications > Life Sciences > Small Molecules, Technology Classifications > Life Sciences > Therapeutics
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Discovery of Novel DYRK1A Inhibitors
DYRK1A has been implicated in multiple disease states, including Alzheimer's Disease and Down Syndrome. Researchers have discovered a new chemotype that has been exemplified with significant DYRK1A activity and have developed brain-penetrant small molecule DYRK1A inhibitors toward Alzheimer's and the cognitive deficits of Down Syndrome. Future...
Published: 1/10/2024
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Inventor(s): Christopher Hulme, Timothy Chavez, Nathan Bedard
Keywords(s):
Category(s): Technology Classifications > Healthcare Portfolios > Neurology, Technology Classifications > Life Sciences > Therapeutics, Technology Classifications > Life Sciences > Small Molecules
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DYRK/CLK PROTACS
This invention describes a set of novel molecules that target and degrade DYRK/CLK for several potential therapeutic purposes.
Background:
Proteolysis-targeting chimeric molecules (PROTACs) are small molecules used to decrease a gene’s protein expression by targeting the protein for ubiquitination and degradation after it is created. This mechanism...
Published: 11/16/2023
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Inventor(s): Christopher Hulme, Kevin Schofield, Walter Becker, Garrit Wilms
Keywords(s):
Category(s): Technology Classifications > Life Sciences > Small Molecules, Technology Classifications > Life Sciences > Therapeutics
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Small Molecule DYRK/CLK Inhibitors and Uses Thereof
This invention is a new composition of matter spanning a 6,6-fused chemotype. The 6,6-analogs display strong inhibitory activity across protein kinases such as the DYRK family, including DYRK1A, DYRK2, and DYRK3, along with inhibiting CLK. The dual DYRK/CLK inhibitors have displayed activity in 3-D organoid models of glioblastoma. It is subsequently...
Published: 11/16/2023
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Inventor(s): Christopher Hulme, Alessandra Fistrovich, Yeng Jeng Shaw, Sourav Banerjee, Curtis Thorne, Nathan Bedard, Carly Cabel
Keywords(s):
Category(s): Technology Classifications, Technology Classifications > Healthcare Portfolios
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Tunable Fluorescent Indolizine Tetracycles
This technology is tunable fluorescent probes that are able to span the colors of the rainbow. The main benefit of this technology is that it can be prepared in only one or two steps; as opposed to the five to seven steps it would normally take. Not only is this technology quicker, but the cost of goods is also more reasonable and compares very favorably...
Published: 11/16/2023
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Inventor(s): Christopher Hulme, Nathan Bedard, Andrew Sennett
Keywords(s):
Category(s): Technology Classifications, Technology Classifications > Life Sciences, Technology Classifications > Research Tools, Technology Classifications > Research Tools > Reagents
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Novel Inhibitors of the Androgen Receptor for the Treatment of Castration Resistant Prostate Cancer (CRPC)
This invention is a new class of heterocyclic small-molecules designed to antagonize the androgen receptor. These molecules have promising biological activity in a prostate specific cell line.
Background:
The primary method for treating early stage prostate cancer is via androgen deprivation therapy because prostate cancer needs androgen in order...
Published: 11/16/2023
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Inventor(s): Christopher Hulme, Yeng Jeng Shaw, Vijay Gokhale
Keywords(s):
Category(s): Technology Classifications > Life Sciences > Therapeutics
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