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73 results about "Degron" patented technology
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A degron is a portion of a protein that is important in regulation of protein degradation rates. Known degrons include short amino acid sequences, structural motifs and exposed amino acids (often Lysine or Arginine) located anywhere in the protein. In fact, some proteins can even contain multiple degrons. Degrons are present in a variety of organisms, from the N-degrons (see N-end Rule) first characterized in yeast to the PEST sequence of mouse ornithine decarboxylase. Degrons have been identified in prokaryotes as well as eukaryotes. While there are many types of different degrons, and a high degree of variability even within these groups, degrons are all similar for their involvement in regulating the rate of a protein’s degradation. Much like protein degradation (see proteolysis) mechanisms are categorized by their dependence or lack thereof on Ubiquitin, a small protein involved in proteasomal protein degradation, Degrons may also be referred to as “Ubiquitin-dependent" or “Ubiquitin-independent".
Covalent cereblon ligands
PCT designated stage expiredWO2025096856A1Organic active ingredientsOrganic chemistryCereblonProtein target
This invention provides Degrons and Degraders that covalently bind to cereblon which is a component of the E3 ubiquitin ligase. The Degrons provided herein can be used to modulate the activity of cereblon either alone or as covalently linked to a Tail. In addition, the Degron can be linked to a Targeting Ligand which binds to a Target Protein to provide a Degrader.
Owner:C4 THERAPEUTICS INC
Directed degron molecules and applications thereof
PendingUS20250066325A1Organic active ingredientsOrganic chemistryProtein targetPharmaceutical Substances
This invention is related to molecules and methods of use of said molecules or compounds comprising said molecules. A molecule may be a pomalidomide or a thalidomide analogue. A method of inducing degradation of a target protein comprising one or more zinc finger polypeptides in a cell may comprise exposing a cell transfected with the target protein with a molecule as described herein, a pharmaceutically acceptable salt thereof, or any combination thereof. A method of inducing degradation of a target protein comprising one or more FK506 binding protein (FKBP) domains or degradation of a target amine in a cell may comprise exposing a cell transfected with the target protein or comprising the target amine with a composition comprising a molecule as described herein, a pharmaceutically acceptable salt thereof, or any combination of compositions comprising molecules as described herein and pharmaceutically acceptable salts thereof. A method may improve on-target effects and reduce off-target effects.
Owner:THE BRIGHAM & WOMEN S HOSPITAL INC +1
A method for identifying modified amino acid degrons (MAADs)
PendingJP2025539386AMicrobiological testing/measurementMicroorganism librariesOrganic chemistryAmino acid
The present invention relates to modified amino acid degrons (MAADs) and methods for identifying factors that mediate the selective degradation of MAAD-tagged proteins.
Owner:エーテーハーチューリッヒ
Precision lifespan control of intracellularly delivered therapeutic proteins
PCT designated stageWO2026055466A1BacteriaFusion with degradation motifTherapeutic proteinEndonuclease
An isolated peptide for regulating intracellular protein degradation that includes a linker sequence fused to a C-end degron peptide and, optionally, a caging molecule bonded to the carboxyl group of a C -terminal alanine residue. Also disclosed is a method for temporal control of protein degradation that relies on fusing a protein of interest at its C- terminus to the degron peptide having a caging molecule, and a method for high-fidelity gene editing that utilizes an RNA-dependent endonuclease modified at the C -terminus with the caged isolated peptide. A fusion protein for high-fidelity gene editing is further provided.
Owner:BOSTON COLLEGE
Synthesis and in vitro characterization of proteolysis targeting chimeras (protacs) for degradation of DNA methyltransferase 1 (DNMT1)
PCT designated stage expiredWO2025006902A3Organic chemistryPharmaceutical non-active ingredientsDiseaseCell Proliferation Process
Disclosed are bifunctional compounds (degraders) comprising a [Targeting ligand]-[Linker]-[Degron] adduct, the targeting ligand comprising a substituted pyridine compound, the bifunctional compounds targeting the epigenetic writer protein deoxyribonucleic acid methyltransferase 1, which is responsible for the maintenance of DNA methylation during cell proliferation, for degradation. Also disclosed are pharmaceutical compositions containing the compounds and methods of using the compounds to treat diseases and disorders characterized or mediated by aberrant DNMT1 activity.
Owner:DANA FARBER CANCER INSTITUTE INC
Maltose dependent degrons, maltose-responsive promoters, stabilization constructs, and their use in production of non-catabolic compounds
The present disclosure relates to the use of a maltose dependent degron to control stability of a protein of interest fused thereto at the post-translational level. The present disclosure also relates to the use of a maltose dependent degron in combination with a maltose-responsive promoter to control gene expression at the transcriptional level and to control protein stability at the post-translational level. The present disclosure also relates to the use of a stabilization construct that couples expression of a cell-growth-affecting protein with the production of non-catabolic compounds. The present disclosure further relates to the use of a synthetic maltose-responsive promoter. The present disclosure further provides compositions and methods for using a maltose dependent degron, a maltose-responsive promoter, and a stabilization construct, either alone or in various combinations, for the production of non-catabolic compounds in genetically modified host cells.
Owner:AMYRIS INC +1
VHH anti-PROTAC antibodies and complexes
PendingCN121240880AAntibody ingredientsImmunoglobulins against cell receptors/antigens/surface-determinantsAntiendomysial antibodiesProtein target
The present invention relates to a monospecific or bispecific antibody, or an antibody fragment or fusion protein thereof, capable of binding to the VHL ligand VH032 (or derivative thereof) degrading moiety (degradation determinant) of a proteolytic targeting chimera (PROTAC), and optionally to a target protein. The invention also relates to complexes (PAX) of such antibodies, or antibody fragments or fusion proteins thereof, with PROTACS, as well as methods for their production, and their respective medical and non-medical uses.
Owner:MERCK PATENT GMBH
Engineered CAS9 endonucleases with enhanced editing efficiency
Mutant Cas9 proteins are described that have one or more mutations in a Keap1 degron sequence of the Cas9 protein. The one or more mutations can increase the half-life of the mutant proteins. Nucleic acid sequences and constructs comprising a sequence that encode a mutant Cas9 protein, as well as methods of enhancing CRISPR efficiency by administering one or more guide RNAs (gRNAs) to a cell comprising the mutant Cas9 proteins are also disclosed herein.
Owner:THE UNIV OF NORTH CAROLINA AT CHAPEL HILL
KRAS proteolysis targeting chimeras
Provided herein are KRAS proteolytic targeting chimeras (PROTACs), compositions comprising the KRAS PROTACs, and methods of making and using the KRAS PROTACs, for example, to promote degradation of KRAS and / or to treat KRAS-related cancers. In embodiments, KRAS PROTAC has the structural formula: or a pharmaceutically acceptable salt thereof, where the values of the variables (e.g., ring A, X4, Y, R2, R3, R4, L ', Detron) are as described herein.
Owner:PAQ THERAPEUTICS INC
Chemical targeting SWI / SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 4 (smarca4) and use in diffuse intrinsic pontine glioma (DIPG)
The present disclosure relates to bifunctional compounds comprising targeting moiety that binds SWI / SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 4 (SMARCA4) or SMARCA2 and SMARCA4, and a degron that binds an E3 ubiquitin ligase. The disclosure further provides compositions and methods for treating diseases or conditions mediated by aberrant activity of SMARCA4 or SMARCA2 and SMARCA4, including diffuse midline glioma harboring a H3K27M mutation.
Owner:DANA FARBER CANCER INSTITUTE INC
Selective histone deacetylase 8 (HDAC8) degraders and methods of use thereof
The present disclosure relates to compounds, compositions, and methods for treating diseases or conditions mediated by aberrant histone deacetylase 8 (HDAC8) activity. The compounds disclosed comprise HDAC8 Targeting Ligand TL moiety covalently linked to a Dergon moiety recruiting E3 ubiquitin ligase to HDAC8. In some embodiments, the degron may bind the E3 ligase which is von Rippel-Lindau (VHL) tumor suppressor.
Owner:DANA FARBER CANCER INSTITUTE INC
Sustained transgene expression of IMID-responsive peptide-suicide protein fusion polypeptides and uses thereof
PCT designated stageWO2026030634A2Fusion with DNA-binding domainAntibody mimetics/scaffoldsCereblonPharmaceutical drug
Provided herein are targeting constructs for sustained transgene expression of inducible cell death systems that include degron mutants and cereblon mutants. Also provided are pharmaceutical compositions comprising the targeting constructs, and methods for use of the same. The methods of use include methods of inducing cell death in a cell, and methods of treating patients in need thereof.
Owner:SENTI BIOSCI INC +1
Nonhuman animal and use for same
A genetically modified non-human animal in which an auxin-inducible degron system controls degradation of a target protein in a living body includes: a chromosome containing a first nucleic acid that encodes a mutant TIR1 family protein having a mutation at an auxin-binding site and having affinity to an auxin analog.
Owner:INTER UNIV RES INST RES ORG OF INFORMATION & SYST +1
Heterocyclic degronimers for target protein degradation
This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.
Owner:C4 THERAPEUTICS INC
Heterocyclic degradation determinants for target protein degradation
The present invention provides heterocyclic compounds ("degradation determinants") that bind to E3 ubiquitin ligase (typically by cerebron) that can be used as-is or linked to targeting ligands against selected target proteins for therapeutic purposes, methods of use and compositions thereof, and methods of their preparation.
Owner:C4 THERAPEUTICS INC
Degraders and degrons for targeted protein degradation
Owner:C4 THERAPEUTICS INC
Auxin-inducible degron system kit and use thereof
An auxin-inducible degron system kit that controls degradation of a target protein in a non-plant-derived eukaryotic cell, the kit containing a first nucleic acid that encodes a mutant TIR1 family protein having a mutation at an auxin-binding site, an auxin analog that has an affinity to the mutant TIR1 family protein and a second nucleic acid that encodes a degradation tag containing at least a part of an Aux / IAA family protein and having an affinity to a complex of the mutant TIR1 family protein and the auxin analog.
Owner:INTER UNIV RES INST RES ORG OF INFORMATION & SYST +1
Novel drug-induced degradation label
PendingCN120265754AOrganic active ingredientsFusion with DNA-binding domainPharmacy medicinePharmaceutical drug
The present invention provides novel drug-inducible degradation tags (degradation determinants), as well as fusion proteins, cells and pharmaceutical compositions comprising the drug-inducible degradation tags. Nucleic acid sequences and vectors encoding the new degradation determinants are also provided. Also provided herein are methods of using the novel degradation determinants, fusion proteins, cells, pharmaceutical compositions, nucleic acid sequences, and vectors.
Owner:THE INST OF CANCER RES ROYAL CANCER HOSPITAL +2
Degron fusion constructs
Provided herein are degrons, compositions, and chimeric molecules comprising the degrons, and methods of using the degrons and chimeric molecules.
Owner:VECTORY THERAPEUTICS BV
Method for robust control of gene expression
Disclosed herein include methods, compositions, and kits suitable for robust and tunable control of payload gene expression. Some embodiments provide rationally designed circuits, including miRNA-level and / or protein-level incoherent feed-forward loop circuits, that maintain the expression of a payload at an efficacious level. The circuit can comprise a promoter operably linked to a polynucleotide encoding a fusion protein comprising a payload protein, a protease, and one or more self-cleaving peptide sequences. The payload protein can comprise a degron and a cut site the protease is capable of cutting to expose the degron. The circuit can comprise a promoter operably linked to a polynucleotide comprising a payload gene, a silencer effector cassette, and one or more silencer effector binding sequences.
Owner:CALIFORNIA INST OF TECH
KRAS G12D proteolysis targeting chimeras
Provided herein are KRAS G12D proteolysis targeting chimeras (PROTACs), compositions comprising the KRAS G12D PROTACs, and methods of making and using the KRAS G12D PROTACs, e.g., to promote degradation of KRAS G12D and / or treat KRAS G12D-associated cancers. In an embodiment, the KRAS G12D PROTAC has the following structural formula:[KRAS G12Di]-L′-[Degron],or a pharmaceutically acceptable salt thereof, wherein values for the variables (e.g., KRAS G12Di, L′, Degron) are as described herein.
Owner:PAQ THERAPEUTICS INC
N / O-linked degrons and degronimers for protein degradation
This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.
Owner:C4 THERAPEUTICS INC
C 3 - carbon-linked glutarimide degradation determinants
The present invention provides degron bodies with carbon-linked E3 ubiquitin ligase targeting moieties (degrons) that can be linked to targeting ligands for proteins selected for degradation in vivo, methods and compositions for their use, and methods for their preparation.
Owner:C4 THERAPEUTICS INC
Maltose dependent degrons, maltose-responsive promoters, stabilization constructs, and their use in production of non-catabolic compounds
The present disclosure relates to the use of a maltose dependent degron to control stability of a protein of interest fused thereto at the post-translational level. The present disclosure also relates to the use of a maltose dependent degron in combination with a maltose-responsive promoter to control gene expression at the transcriptional level and to control protein stability at the post-translational level. The present disclosure also relates to the use of a stabilization construct that couples expression of a cell-growth-affecting protein with the production of non-catabolic compounds. The present disclosure further relates to the use of a synthetic maltose-responsive promoter. The present disclosure further provides compositions and methods for using a maltose dependent degron, a maltose-responsive promoter, and a stabilization construct, either alone or in various combinations, for the production of non-catabolic compounds in genetically modified host cells.
Owner:AMYRIS INC +1
Bicyclic-substituted glutarimide cereblon binders
This invention provides Degron compounds which bind to cereblon which is a component of the E3 ubiquitin ligase. The Degrons provided herein can be used to modulate the activity of cereblon either alone or as covalently linked to a Tail. Alternatively, the Degron can be linked to a Targeting Ligand which binds to a Target Protein for protein degradation.
Owner:C4 THERAPEUTICS INC
Bicyclic-substituted glutarimide cereblon binders
This invention provides Degron compounds which bind to cereblon which is a component of the E3 ubiquitin ligase. The Degrons provided herein can be used to modulate the activity of cereblon either alone or as covalently linked to a Tail. Alternatively, the Degron can be linked to a Targeting Ligand which binds to a Target Protein for protein degradation.
Owner:C4 THERAPEUTICS INC
Drug-regulatable, inducible cytokine expression
Disclosed are nucleic acids comprising a nucleotide sequence encoding a polypeptide comprising a cytokine, or a functional portion of the cytokine; a transmembrane-intracellular amino acid sequence or a transmembrane amino acid sequence; and an immunomodulatory imide drug (IMiD)-degradable degron, wherein the nucleotide sequence encoding the polypeptide comprises a promoter operatively associated with the nucleotide sequence encoding polypeptide. Also disclosed are related recombinant expression vectors, viral particles, host cells, populations of cells, pharmaceutical compositions, methods of treating or preventing cancer, and methods of enhancing the immune response to a cancer.
Owner:THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
Modified degradation determinant polypeptides and uses thereof
PendingCN121443627AFusion with degradation motifPeptide/protein ingredientsImmunomodulationsPharmaceutical drug
Provided herein are modified degradation determinants having increased sensitivity to one or more immunomodulatory drugs (IMiDs). Also provided herein are modified selebrons having an increased sensitivity to one or more IMiDs. Also provided herein are modified degradation determinants that exhibit reduced degradation upon binding to one or more IMiDs. Also provided are induced degradable proteins, induced cell death systems, and activation conditionally controlling polypeptides employing the modified degradation determinants, the modified seleburon, and methods and / or uses thereof.
Owner:SENTI BIOSCI INC
Reporters constructs, systems and assays
PCT designated stageWO2025248260A1Antibody mimetics/scaffoldsMicrobiological testing/measurementAssayRecognition sequence
The present invention provides an isolated nucleic acid encoding a reporter fusion protein comprising a selection marker, a protease recognition sequence and a degron.
Owner:UCL BUSINESS LTD
Stabilized peptide-mediated targeted protein degradation
The invention relates to stable peptide-mediated targeted protein degradation. Specifically, the invention relates to a chimera, and more specifically relates to a nailing peptide degradation determinant chimera. The present invention relates to a protein fusion protein that acts as a protein degradation inducing moiety by binding a nailing peptide that binds to a disease-related protein to a small molecule degradation determinant (e.g., a cereblone-or VHL-binding small molecule as a degradation determinant) or a polypeptide sequence degradation determinant (e.g., a Cop1-binding Trib peptide as a degradation determinant); or by binding a stapling peptide degradation determinant to a peptide (e.g., a stapling peptide) or a small molecule bound to a disease-associated protein to act as a protein degradation inducing moiety. The present application also relates to methods of targeted degradation of endogenous proteins by using a stapling peptide degradation determinant chimera that can be used to treat proliferative diseases or other conditions, where elimination of a disease-causing or disease-associated protein may have a therapeutic benefit. The invention also provides a method for preparing the compounds and intermediates thereof.
Owner:DANA FARBER CANCER INSTITUTE INC