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Merck

Targeted Protein Degradation by Small Molecules.

Annual review of pharmacology and toxicology (2016-10-13)
Daniel P Bondeson, Craig M Crews
초록

Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of disease-relevant proteins. Here, we review recent advances in the use of small molecules to degrade proteins in a selective manner. First, we highlight all-small-molecule techniques with direct clinical application. Second, we describe techniques that may find broader acceptance in the biomedical research community that require little or no synthetic chemistry. In addition to serving as innovative research tools, these new approaches to control intracellular protein levels offer the potential to develop novel therapeutics targeting proteins that are not currently pharmaceutically vulnerable.

MATERIALS
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Sigma-Aldrich
C5 Lenalidomide-C6-PEG1-C3-PEG1-Butyl NH2 hydrochloride, ≥95%
Sigma-Aldrich
VH 032 amide-alkyl C3-acid, ≥95%
Sigma-Aldrich
(S,R,S)-AHPC-CO-PEG4-C2-amine HCl, ≥95%
Sigma-Aldrich
4-Aminomethyl-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione hydrochloride, ≥95%
Sigma-Aldrich
Thalidomide-NH-PEG2-COOH, ≥95%
Sigma-Aldrich
VH 032 amide-PEG3-acid, ≥95.0%
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Opto-pomalidomide, ≥95%
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Pomalidomide-benzyl-piperazine hydrochloride
Sigma-Aldrich
3-((4-(Piperidin-4-yl)phenyl)amino)piperidine-2,6-dione hydrochloride, ≥95%
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1H-Isoindole-1,3(2H)-dione, 4-[(4-aminobutyl)amino]-2-(2,6-dioxo-3-piperidinyl)-, hydrochloride, ≥95%
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Pentanoic acid, 5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-, ≥95%
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FBnG-C3-PEG3-C3-NH2 hydrochloride, ≥95%
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Pomalidomide-PEG1-C2-amine HCl, ≥95.0%
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Opto-pomalidomide-C2-NH2 hydrochloride, ≥95%
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(S,R,S)-AHPC-pyridine-PEG1-piperazine hydrochloride
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CCW16-C4-BocNH, 95%
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2-(2,6-dioxopiperidin-3-yl)-5-(piperidin-4-yl)isoindole-1,3-dione hydrochloride, ≥95%
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(S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH2 hydrochloride
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3-(3-Fluoro-4-piperidin-4-ylphenylamino)piperidine-2,6-dione hydrochloride, ≥95%
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Pomalidomide-PEG1-C2-azide, ≥95.0%
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C5 Lenalidomide-pyrimidine-piperazine-PEG1-NH2 hydrochloride, ≥95%
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C5 Lenalidomide-pyridine-PEG1-piperazine hydrochloride, ≥95%
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L-Prolinamide, N-[2-[2-(carboxymethoxy)ethoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-, ≥95%
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(S,R,S)-AHPC-di-trimethylamide-dioxodisulfide-carbonate ester
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C5 Lenalidomide-PEG6-Butyl NH2 hydrochloride, ≥95%
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CCW16-PEG3-BocNH, ≥95%
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(S,R,S)-VL285 Phenol-C2-NH2 hydrochloride
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(S,R,S)-VL285 Phenol-PEG1-piperazine hydrochloride
Sigma-Aldrich
(S,R,S)-AHPC-methylamino-PEG1-NH2 hydrochloride
Sigma-Aldrich
C5 Lenalidomide-difluoroPEG1-C4-piperazine Hydrochloride, ≥95%