CAS: 174132-31-1; (S)-2-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-3-(4-((Tert-Butoxycarbonyl)Amino)Phenyl)Propanoic Acid

相似化合物

214750-77-3 102281-45-8 943-80-6

上下游产品

Fmoc-4-氨基-L-苯丙氨酸 4-Amino-N-[(9H-Fluoren-9-Ylmethoxy)Carbonyl]-L-Phenylalanine 95753-56-3
Fmoc-对硝基-L-苯丙氨酸 N-α-Fmoc-4-Nitro-L-Phenylalanine 95753-55-2

📜Fmoc-对硝基-L-苯丙氨酸置于palladium 10% On Activated Carbon,甲酸铵,碳酸氢钠体系中,用 1,4-二氧六环,甲醇,水 用作溶剂,化学反应 28.0H,反应生成Fmoc-4-氨基苯丙氨酸
参考文献:Incorporation Of Non-Natural Amino Acids Improves Cell Permeability And Potency Of Specific Inhibitors Of Proteasome Trypsin-Like Sites
标题:Incorporation Of Non-Natural Amino Acids Improves Cell Permeability And Potency Of Specific Inhibitors Of Proteasome Trypsin-Like Sites
摘要:Proteasomes Degrade The Majority Of Proteins In Mammalian Cells By A Concerted Action Of Three Distinct Pairs Of Active Sites. The Chymotrypsin-Like Sites Are Targets Of Antimyeloma Agents Bortezomib And Carfilzomib. Inhibitors Of The Trypsin-Like Site Sensitize Multiple Myeloma Cells To These Agents. Here We Describe Systematic Effort To Develop Inhibitors With Improved Potency And Cell Permeability,Yielding Azido-Phe-Leu-Leu-4-Aminomethyl-Phe-Methyl Vinyl Sulfone (4A,Lu-102),And A Fluorescent Activity-Based Probe For This Site. X-Ray Structures Of 4A And Related Inhibitors Complexed With Yeast Proteasomes Revealed The Structural Basis For Specificity. Nontoxic To Myeloma Cells When Used As A Single Agent,4A Sensitized Them To Bortezomib And Carfilzomib. This Sensitizing Effect Was Much Stronger Than The Synergistic Effects Of Histone Acetylase Inhibitors Or Additive Effects Of Doxorubicin And Dexamethasone,Raising The Possibility That Cornbinations Of Inhibitors Of The Trypsin-Like Site With Bortezomib Or Carfilzomib Would Have Stronger Antincoplastic Activity Than Combinations Currently Used Clinically.
Doi:10.1021/jm3016987

专利信息

专利号:US-11279734-B2
优先权日:2017-12-01
标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries
发明人：PENTELUTE BRADLEY L; TOUTI FAYCAL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.

专利号:US-8338565-B2
优先权日:2008-08-20
标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
发明人：LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.