ライフサイエンスコーパス: PROTAC

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1 PROTAC technology employs small molecules that recruit t

2 PROTACs conjugate a target warhead to an E3 ubiquitin li

3 igase should be varied to rapidly generate a PROTAC with the desired degradation profile.

4 the first time, we report the formation of a PROTAC by Cu(I)-catalyzed cycloaddition of a thalidomide

5 opment, we discovered that the capacity of a PROTAC to induce degradation involves more than just tar

6 substrates using bivalent compounds known as PROTACs (for 'proteolysis-targeting chimeras').

7 In HeLa cells, our SirReal-based PROTAC induced isotype-selective Sirt2 degradation that

8 Thus, our SirReal-based PROTAC is the first example of a probe that is able to c

9 egradation of the target protein promoted by PROTACs.

10 elopment of a proteolysis targeting chimera (PROTAC) based on the combination of the unique features

11 ased upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation.

12 Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging alternative the

13 ader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved e

14 Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 l

15 Proteolysis targeting chimeras (PROTACs) are bispecific molecules containing a target pr

16 bifunctional proteolysis targeting chimeras (PROTACs) containing a VHL ligand can hijack the E3 ligas

17 lecule-based proteolysis-targeting chimeras (PROTACs) have demonstrated that this technology can effe

18 he design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for induc

19 The generation of effective PROTACs depends on the nature of the protein/ligase liga

20 the compounds; thus, as a starting point for PROTAC development, both the target ligand and the recru

21 ways and new VHL ligands for next-generation PROTACs.

22 We describe Homo-PROTACs as an approach to dimerize an E3 ligase to trigg

23 We provide proof-of-concept of Homo-PROTACs using diverse molecules composed of two instance

24 bility of PROTACs to form the ternary ligase-PROTAC-target protein complex and a MSD assay to measure

25 Moreover, PROTAC-mediated protein degradation offers a general str

26 synthesis, and evaluation of a new class of PROTAC BET degraders.

27 The synthesis of PROTAC compounds that mediate the degradation of c-ABL a

28 y assay was used to determine the ability of PROTACs to form the ternary ligase-PROTAC-target protein

29 ick chemistry" approach for the synthesis of PROTACs.

30 or does not necessarily generate more potent PROTACs and underscores the key roles played by the conj

31 ing an ubiquitin ligase to a target protein, PROTACs promote ubiquitination and proteasomal degradati

32 Triazolodiazepine PROTACs exhibited positive cooperativities of ternary co

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