166410-28-2

Upstream product

• 57260-73-8 N-BOC-1,2-diaminoethane 
• 28920-43-6 (fluorenylmethoxy)carbonyl chloride 
• 82911-69-1 N-(9H-fluoren-2-ylmethoxycarbonyloxy)succinimide 
• 213322-15-7 N-(9H-fluorenylmethoxycarbonyloxy)succinimide 
• 109273-24-7 2,3-diaminopropionic acid t-butyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 112670-29-8 N-(tert-butyloxycarbonyl)-1,2-diaminoethane toluensulfonic acid salt 

Downstream Products

• 207129-12-2 N-Boc-N'-Fmoc-imidazolidine-2-carboxylic acid 
• 166410-32-8 N-Fmoc-ethylenediamine 
• 225797-46-6 {2-[5-(2-oxo-hexahydro-thieno[3,4-d]imidazol-6-yl)-pentanoylamino]-ethyl}-carbamic acid tert-butyl ester 
• 391624-47-8 [2-(9H-fluoren-9-ylmethoxycarbonylamino)-ethyl]-carbamic acid 4-nitro-phenyl ester 
• 391624-46-7 9-fluorenylmethyl N-(2-aminoethyl)carbamate hydrochloride 

Relevant academic research and scientific papers

LIGAND LINKER SUBSTRATE

Ligand functionalized substrate including a solid substrate, which has been modified to provide grafted catching ligand groups covalently bound via a linker, methods of preparing said ligand functionalized substrate and the use thereof, such as to increase binding rate and the dynamic binding capacity (DBC).

PEPTIDE NUCLEIC ACID (PNA) MONOMERS WITH AN ORTHOGONALLY PROTECTED ESTER MOIETY

This application pertains to orthogonally protected esters of peptide nucleic acid (PNA) monomers, which ester groups can be removed under conditions that permit typical backbone and side chain acid- and base-labile protecting groups to remain substantially intact thereby permitting the high yield of PNA monomer carboxylic acids that are suitable for use in PNA oligomer synthesis. Exemplary ester groups include, but are not limited to, 2,2,2-trichloroethyl (TCE), 2,2,2-tribromoethyl (TBE), 2-bromoethyl (2-BE) and 2-iodoethyl groups (2-IE). This invention also pertains to novel methods for the synthesis of Backbone Ester compounds and related Backbone Ester Acid Salts.

Tri-Orthogonal Scaffolds for the Solid-Phase Synthesis of Peptides

Multi-orthogonal scaffolds can be useful for the attachment of several different compounds to the same central skeleton. Such compounds can find applications in the development of protein mimics because of their potential to mimic several distant epitopes

SILVESTROL ANTIBODY-DRUG CONJUGATES AND METHODS OF USE

The invention relates generally to a silvestrol molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody conjugated by a linker to one or more silvestrol drug moieties and methods of treatment.

Molecular recognition of surface-immobilized carbohydrates by a synthetic lectin

The molecular recognition of carbohydrates and proteins mediates a wide range of physiological processes and the development of synthetic carbohydrate receptors ("synthetic lectins") constitutes a key advance in biomedical technology. In this article we report a synthetic lectin that selectively binds to carbohydrates immobilized in a molecular monolayer. Inspired by our previous work, we prepared a fluorescently labeled synthetic lectin consisting of a cyclic dimer of the tripeptide Cys-His-Cys, which forms spontaneously by air oxidation of the monomer. Amine-tethered derivatives of N-acetylneuraminic acid (NANA), β-D-galactose, β-Dglucose and α-D-mannose were microcontact printed on epoxide-terminated self-assembled monolayers. Successive prints resulted in simple microarrays of two carbohydrates. The selectivity of the synthetic lectin was investigated by incubation on the immobilized carbohydrates. Selective binding of the synthetic lectin to immobilized NANA and β-D-galactose was observed by fluorescence microscopy. The selectivity and affinity of the synthetic lectin was screened in competition experiments. In addition, the carbohydrate binding of the synthetic lectin was compared with the carbohydrate binding of the lectins concanavalin A and peanut agglutinin. It was found that the printed carbohydrates retain their characteristic selectivity towards the synthetic and natural lectins and that the recognition of synthetic and natural lectins is strictly orthogonal.

A ratiometric fluorescent nanoprobe for H2O2 sensing and in vivo detection of drug-induced oxidative damage to the digestive system

Hydrogen peroxide is a biologically important reactive oxygen species (ROS) and plays crucial roles in living organisms. Herein, a FRET-based ratiometric fluorescent probe has been developed for detecting H2O2in vitro and in vivo. In this nanoprobe, carbon dots serve as the energy donor and carrier for the H2O2 recognition element. This nanoprobe exhibits fast-response, low toxicity, high sensitivity (with a detection limit of 0.5 μM) and selectivity towards H2O2 over other reactive oxygen or nitrogen species. The nanoprobe has been successfully applied in the detection of H2O2 in live cells and in zebrafish larvae. By incubating the nanoprobe with zebrafishes, the nanoprobe can be absorbed by the fishes within 1 h and accumulates mainly in the abdominal region. Due to its small size (～4 nm), the nanoprobe is gradually excreted by zebrafishes without long-term accumulation. Moreover, as the first ratiometric chemoprobe that can detect H2O2in vivo, the nanoprobe has been found capable of detecting and locating endogenous H2O2 in zebrafishes as a result of drug-induced oxidative damage. The successful detection of H2O2 by the nanoprobe in vivo may support its eventual use in clinical applications.

Structure-affinity relationships of glutamine mimics incorporated into phosphopeptides targeted to the SH2 domain of signal transducer and activator of transcription 3

In cancer cells, signal transducer and activator of transcription 3 (Stat3) participates in aberrant growth, survival, angiogenesis, and invasion signals and is a validated target for anticancer drug design. We are targeting its SH2 domain to prevent docking to cytokine and growth factor receptors and subsequent signaling. One of the important elements of the recognition sequence, pTyr-Xxx-Xxx-Gln, is glutamine. We incorporated novel Gln mimics into a lead peptide, pCinn-Leu-Pro-Gln-NHBn, and found that a linear, unconstrained side chain and carboxamide are necessary for high affinity, and the benzamide can be eliminated. Replacement of Gln-NHBn with (R)-4-aminopentanamide or 2-aminoethylurea produced inhibitors with equal or greater potency than that of the lead, as judged by fluorescence polarization (IC50 values were 110 and 130 nM, respectively). When Pro was replaced with cis-3,4- methanoproline, the glutamine mimic, (4R,5S)-4-amino-5-benzyloxyhexanamide resulted in an IC50 of 69 nM, the highest affinity Stat3 inhibitor reported to date. 2009 American Chemical Society.

A generic building block for C- and N-terminal protein-labeling and protein-immobilization

Expressed protein ligation (EPL) and bioconjugation based on the maleimide group (MIC-conjugation) provide powerful tools for protein modification. In the light of the importance of site-selectively modified proteins for the study of protein function, a f

Solid-phase synthesis of oligourea peptidomimetics employing the Fmoc protection strategy

A solid-phase-Fmoc-based-synthesis strategy is described for oligourea peptidomimetics as well as a convenient general synthesis approach for the preparation of the required building blocks 5a-j and 5k. These are suitable for use in peptide or robot synthesizers, which is illustrated by the synthesis of oligourea peptidomimetics of part of Leu-enkephalin (10) and a neurotensin derivative (17).

Topologically segregated, encoded solid phase libraries

The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.