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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Применить Всего найдено 13. Отображено 9.
07-01-2021 дата публикации

In vivo engineered cereblon protein

Номер: US20210002337A1
Автор: Benjamin F. Cravatt, Benjamin HORNING, Brian Nordin, David Weinstein, Dean Stamos, Ekaterina Vinogradova, Gabe SIMON, Kristen BALTGALVIS, Matthew Patricelli, Todd Kinsella
Принадлежит: Scripps Research Institute, Vividion Therapeutics Inc

Disclosed herein are in vivo engineered cereblon protein and methods of making the same. The in vivo engineered cereblon protein can include a site-specific non-naturally occurring modification at cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3, the modification comprising a moiety resulting from an in vivo Michael addition reaction between an exogenous Michael acceptor and the cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3.

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Номер записи: 1
03-03-2022 дата публикации

Cereblon modulators and uses thereof

Номер: US20220062248A1
Автор: Benjamin F. Cravatt, Benjamin HORNING, David Weinstein, Dean Stamos, Ekaterina Vinogradova, Gabe SIMON, Matthew Patricelli
Принадлежит: Scripps Research Institute, Vividion Therapeutics Inc

Disclosed herein are compositions and methods for modulating cereblon neosubstrates. A small molecule modulator of Formula (I*), or a pharmaceutically acceptable salt or solvate thereof can be used to modulate cereblon neosubstrates.

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Номер записи: 2
22-09-2022 дата публикации

In vivo engineered cereblon protein

Номер: US20220298213A1
Автор: Benjamin F. Cravatt, Benjamin HORNING, Brian Nordin, David Weinstein, Dean Stamos, Ekaterina Vinogradova, Gabe SIMON, Kristen BALTGALVIS, Matthew Patricelli, Todd Kinsella
Принадлежит: Scripps Research Institute, Vividion Therapeutics Inc

Disclosed herein are in vivo engineered cereblon protein and methods of making the same. The in vivo engineered cereblon protein can include a site-specific non-naturally occurring modification at cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3, the modification comprising a moiety resulting from an in vivo Michael addition reaction between an exogenous Michael acceptor and the cysteine 287 as set forth in SEQ ID NO: 1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3.

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Номер записи: 3
02-07-2020 дата публикации

Cereblon modulators and uses thereof

Номер: US20200206201A1
Автор: Benjamin F. Cravatt, Benjamin HORNING, David Weinstein, Dean Stamos, Gabe SIMON, Matthew Patricelli
Принадлежит: Scripps Research Institute, Vividion Therapeutics Inc

Disclosed herein are compositions and methods for modulating cereblon neosubstrates. A small molecule modulator of Formula (I*), or a pharmaceutically acceptable salt or solvate thereof can be used to modulate cereblon neosubstrates.

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Номер записи: 4
09-07-2020 дата публикации

IN VIVO ENGINEERED CEREBLON PROTEIN

Номер: US20200216507A1
Автор: CRAVATT Benjamin F., HORNING Benjamin, PATRICELLI Matthew, SIMON Gabe, Stamos Dean, Weinstein David
Принадлежит:

Disclosed herein are in vivo engineered cereblon protein and methods of making the same. The in vivo engineered cereblon protein can include a site-specific non-naturally occurring modification at cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3, the modification comprising a moiety resulting from an in vivo Michael addition reaction between an exogenous Michael acceptor and the cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3. 1. An in vivo engineered cereblon protein consisting of a non-naturally occurring covalent modification at cysteine 287 as set forth in SEQ ID NO:1 , or cysteine 286 as set forth in SEQ ID NO: 2 or 3 , the modification resulting from an in vivo Michael addition reaction between an exogenous Michael acceptor and the cysteine 287 as set forth in SEQ ID NO:1 , or cysteine 286 as set forth in SEQ ID NO: 2 or 3 , wherein a sulfur atom at the cysteine residue undergoes the Michael reaction with a double bond of the exogenous Michael acceptor , and wherein the engineered cereblon has reduced engagement potency at cysteine 318 as set forth in SEQ ID NO:1 or at cysteine 317 as set forth in SEQ ID NO: 2 or 3.2. The in vivo engineered cereblon of claim 1 , wherein the IMiD pocket-dependent binding on the engineered cereblon protein is prevented by the modification.3. The in vivo engineered cereblon of claim 1 , wherein the engineered cereblon protein has an inhibited or reduced binding for immunomodulatory drugs as compared to unmodified cereblon.4. (canceled)5. The in vivo engineered cereblon of claim 1 , wherein the amino acid residue at cysteine 318 as set forth in SEQ ID NO:1 or cysteine 317 as set forth in SEQ ID NO: 2 or 3 is not modified.6. The in vivo engineered cereblon of claim 1 , wherein the amino acid residues at cysteine 234 claim 1 , cysteine 205 claim 1 , cysteine 219 claim 1 , cysteine 366 claim 1 , cysteine 188 claim 1 , and cysteine 343 as set forth ...

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Номер записи: 5
30-07-2020 дата публикации

COMPOUNDS AND METHODS OF MODULATING PROTEIN DEGRADATION

Номер: US20200239530A1
Автор: HORNING Benjamin, PATRICELLI Matthew, SIMON Gabe, Stamos Dean
Принадлежит:

Disclosed herein are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the protein is part of the E3 ligase complex and the protein is modified to alter the substrate recognition of the E3 ligase complex. In some instances, also provided herein are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the protein is modified or tagged for degradation. In some instances, additionally provided herein are cysteine-containing protein binding domains that interact with a probe and/or a ligand described herein. 2. The protein-probe adduct of claim 1 , wherein the protein is selected from Ankyrin repeat and BTB/POZ domain-containing protein 1 claim 1 , Ankyrin repeat and BTB/POZ domain-containing protein 2 claim 1 , Activating molecule in BECN1-regulated autophagy protein 1 claim 1 , Anaphase-promoting complex subunit 11 claim 1 , Anaphase-promoting complex subunit 15 claim 1 , Anaphase-promoting complex subunit 16 claim 1 , Anaphase-promoting complex subunit 2 claim 1 , Anaphase-promoting complex subunit 7 claim 1 , Rabankyrin-5 claim 1 , Ankyrin repeat and IBR domain-containing protein 1 claim 1 , Amyloid protein-binding protein 2 claim 1 , Apoptosis-resistant E3 ubiquitin protein ligase 1 claim 1 , E3 ubiquitin-protein ligase ARIH1 claim 1 , E3 ubiquitin-protein ligase ARIH2 claim 1 , Armadillo repeat-containing protein 5 claim 1 , Ankyrin repeat and SOCS box protein 2 claim 1 , Ankyrin repeat and SOCS box protein 6 claim 1 , Transcriptional regulator ATRX claim 1 , Transcription regulator protein BACH1 claim 1 , Transcription regulator protein BACH2 claim 1 , Baculoviral IAP repeat-containing protein 2 claim 1 , Baculoviral IAP repeat-containing protein 3 claim 1 , Baculoviral IAP repeat-containing protein 6 claim 1 , Breast cancer type 1 susceptibility protein claim 1 , F-box/WD repeat-containing protein 1A claim 1 , Cullin-associated NEDD8-dissociated protein 1 claim 1 , ...

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Номер записи: 6
03-10-2023 дата публикации

Cereblon modulators and uses thereof

Номер: US11771689B2
Автор: Benjamin F. Cravatt, Benjamin HORNING, David Weinstein, Dean Stamos, Ekaterina Vinogradova, Gabe SIMON, Matthew Patricelli
Принадлежит: Scripps Research Institute, Vividion Therapeutics Inc

Disclosed herein are compositions and methods for modulating cereblon neosubstrates. A small molecule modulator of Formula (I*), or a pharmaceutically acceptable salt or solvate thereof can be used to modulate cereblon neosubstrates.

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Номер записи: 7
05-08-2020 дата публикации

Compounds and methods of modulating protein degradation

Номер: EP3688012A1
Автор: Benjamin HORNING, Dean Stamos, Gabe SIMON, Matthew Patricelli
Принадлежит: Vividion Therapeutics Inc

Disclosed herein are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the protein is part of the E3 ligase complex and the protein is modified to alter the substrate recognition of the E3 ligase complex. In some instances, also provided herein are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the protein is modified or tagged for degradation. In some instances, additionally provided herein are cysteine-containing protein binding domains that interact with a probe and/or a ligand described herein.

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Номер записи: 8
03-11-2021 дата публикации

In vivo engineered cereblon protein

Номер: EP3902556A1
Автор: Benjamin F. Cravatt, Benjamin HORNING, David Weinstein, Dean Stamos, Gabe SIMON, Matthew Patricelli
Принадлежит: Scripps Research Institute, Vividion Therapeutics Inc

Disclosed herein are in vivo engineered cereblon protein and methods of making the same. The in vivo engineered cereblon protein can include a site-specific non-naturally occurring modification at cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3, the modification comprising a moiety resulting from an in vivo Michael addition reaction between an exogenous Michael acceptor and the cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO: 2 or 3.

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Номер записи: 9