| WO 2021/053555 |
glue degraders and methods
of use thereof |
Novartis
AG |
glue degrader
compounds
binding to and altering the specificity of a cereblon (CRBN) complex
to induce ubiquitination and degradation of a protein; binders to
the tris-tryptophan pocket of cereblon E3 ligase; 18 compounds synthesized
and tested |
| WO 2021/249517 |
a molecular glue regulating
CDK12–DDB1 interaction to trigger cyclin K degradation |
National Institute of Biological
Sciences, Beijing |
molecular glues for triggering
polyubiquitination and degradation of CCNK (cyclin K); creating a
modified CDK12 protein binding DDB1 of the DDB1–CUL4–RBX1
complex; 31 compounds synthesized and tested |
| WO 2020/006264 |
ligands to cereblon
(CRBN) |
Dana-Farber
Cancer Institute |
compounds
with immunomodulatory
activity, methods of making them, and pharmaceutical compositions;
61 compounds synthesized and tested; ∼70 potential targeted
proteins listed |
| WO 2008/115516 |
4′-O-substituted
isoindoline derivatives and compositions comprising and methods of
using the same |
Celgene
Corp. |
74 4′-O-substituted
isoindoline derivative compounds synthesized and tested; pharmaceutical
compositions of these compounds disclosed |
| WO 2021/126805 |
modulation of protein
degradation |
Orionis
Biosciences |
agent
in treating a disease
by recruitment and/or ubiquitination and/or degradation of proteins
such as argininosuccinate synthetase |
| WO 2021/178920 |
compounds for targeted degradation
of BRD9 |
C4 Therapeutics |
BRD9 protein degradation
compounds provided for treatment of disorders mediated by BRD9, including
abnormal cellular proliferation |
| WO 2021/127080 |
detection of novel degradation-related
interactions |
Orionis
Biosciences |
method
for detecting and
identifying protein–protein or protein–small molecule
interactions using a MAPPITT assay with CRBN, IKZF1, DDB1, PROTAC,
FKBP1A, and VHL |
| WO 2014/094138 |
screening methods to identify
inhibitors of E2 enzymes by stabilization of noncovalent ubiquitin–E2
complexes for use in cancer therapy and other disorders |
University of Montreal |
stabilization of the interaction
of noncovalent donor ubiquitin with E2 enzymes, including CDC34–ubiquitin
interaction, and therapeutic methods for inhibiting enzymes involved
in the cell ubiquitin–proteasome system (UPS) |
| WO 2015/200795, WO 2017/117118 |
compositions and methods
for inducing conformational changes in cereblon other E3 ubiquitin
ligases |
Celgene Corp. |
screening methods, computational
methods, and biomarkers based on the elucidation of the interaction
among cereblon, its substrates, and certain compounds or agents, including
small molecules, peptides, and proteins |
| WO 2020/079103 |
method for identifying
a
chemical compound or agent inducing ubiquitination of a protein of
interest |
CEMM Research
Center for
Molecular Medicine |
method for identifying compounds
or agents that can induce ubiquitination of a protein of interest,
for treating cancer or other diseases |
