- COMPOUNDS COMPRISING CLEAVABLE LINKER AND USES THEREOF
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Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.
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Page/Page column 173
(2019/01/21)
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- Tyrosine-derived stimuli responsive, fluorescent amino acids
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A series of fluorescent unnatural amino acids (UAAs) bearing stilbene and meta-phenylenevinylene (m-PPV) backbone have been synthesized and their optical properties were studied. These novel UAAs were derived from protected diiodo-l-tyrosine using palladi
- Cheruku, Pradeep,Huang, Jen-Huang,Yen, Hung-Ju,Iyer, Rashi S.,Rector, Kirk D.,Martinez, Jennifer S.,Wang, Hsing-Lin
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p. 1150 - 1158
(2015/03/04)
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- The synthesis of 13C9-15N-labeled 3,5-diiodothyronine and thyroxine
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Thyroid hormones undergo extensive metabolism to regulate hormone activity. A labeled thyroid hormone would be useful to track hormone metabolism through various pathways. While radiolabeled thyroid hormones have been synthesized and used for in vivo studies, a stable isotope labeled form of thyroid hormone is required for studying thyroid hormone metabolism by LC-MS/MS, an analytical technique that has certain advantages without the complications of radioactivity. Here we report the synthesis of 13C9- 15N-T2 and 13C9-15N- T4, two labeled thyroid hormone derivatives suitable for in vivo LC-MS/MS studies. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications to view the free supplemental file.
- Hackenmueller, Sarah A.,Scanlan, Thomas S.
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p. 1439 - 1446
(2013/05/22)
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- SUBSTITUTED 4-PHENOXYPHENOL ANALOGS AS MODULATORS OF PROLIFERATING CELL NUCLEAR ANTIGEN ACTIVITY
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In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds,which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention
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Paragraph 00586
(2013/03/26)
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- Tyrosine-based poly(m-phenyleneethynylene-p-phenyleneethynylene)s. Helix folding and responsiveness to a base
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The Sonogashira-Hagihara polymerization of 3',5'-diiodo-N-α-tert-butoxycarbonyl-l-tyrosine methyl ester (1) and 3',5'-diiodo-N-α-tert-butoxycarbonyl-O-methyl-l-tyrosine methyl ester (2) with para-diethynylbenzene (3) was carried out to obtain optically active poly(m-phenyleneethynylene-p-phenyleneethynylene)s [poly(1) and poly(2)] with Mn's ranging from 9900 to 15,000 in 80-87% yields. Poly(1) exhibited intense CD signals in DMSO and THF, but did not in CH2Cl2, indicating that it took a predominantly one-handed helical conformation in the former two solvents. On the other hand, there was no evidence for poly(2) to take a helical structure in these solvents. Poly(1) turned the CD sign at 390 nm from plus to minus in DMSO/H2O = 9/1 (v/v) by the addition of NaOH. Alkaline hydrolysis of ester moieties of poly(1) and poly(2) gave the corresponding polymers having carboxy groups [poly(1a) and poly(2a)]. Poly(1a) and poly(2a) increased the CD intensity by the addition of NaOH.
- Liu, Ruiyuan,Sogawa, Hiromitsu,Shiotsuki, Masashi,Masuda, Toshio,Sanda, Fumio
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p. 2255 - 2263
(2011/10/05)
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- A convenient catalyst for aqueous and protein Suzuki-Miyaura cross-coupling
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(Figure Presented) A phosphine-free palladium catalyst for aqueous Suzuki-Miyaura cross-coupling is presented. The catalyst is active enough to mediate hindered, ortho-substituted biaryl couplings but mild enough for use on peptides and proteins. The Suzuki-Miyaura couplings on protein substrates are the first to proceed in useful conversions. Notably, hydrophobic aryl and vinyl groups can be transferred to the protein surface without the aid of organic solvent since the aryl- and vinylboronic acids used in the coupling are water-soluble as borate salts. The convenience and activity of this catalyst prompts use in both general synthesis and bioconjugation.
- Chalker, Justin M.,Wood, Charlotte S. C.,Davis, Benjamin G.
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supporting information; experimental part
p. 16346 - 16347
(2010/01/29)
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- Characterization of thyroid hormone receptor α (TRα)-specific analogs with varying inner- and outer-ring substituents
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Analogs of the TRα-specific thyromimetic CO23 were synthesized and analyzed in vitro using competitive binding and transactivation assays. Like CO23, all analogs bind to both thyroid hormone receptor subtypes with about the same affinity; however, modification of CO23 by derivatization of the 3′ position of the outer-ring or replacement of the inner-ring iodides with bromides attenuates binding. Despite lacking a preference in binding to TRα, all analogs display TRα-specificity in transactivation assays using U2OS and HeLa cells. At best, several agonists exhibit an approximately 6-12-fold preference in transactivation when tested with TRα in HeLa cells. One analog, CO24, showed in vivo TRα-specific action in a tadpole metamorphosis assay.
- Ocasio, Cory A.,Scanlan, Thomas S.
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p. 762 - 770
(2008/09/17)
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- Synthesis and sar of dhodotyrosine-derived glycine-site N-methyl-D-aspartate receptor ligands
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A series of analogues of the novel diiodotyrosine derived NMDA glycine-site ligand (R)-4 was prepared in which the aryl substitution, chain length and amino acid groups were varied. The key structural features for binding are the α-amino acid function, having the (R) absolute stereochemistry, the 3,5-diiodo substituted aromatic ring and a lipophilic group attached at the phenolic oxygen of the tyrosine moiety. Copyright
- Curtis, Neil R.,Kulagowski, Janusz J.,Leeson, Paul D.,Mawer, Ian M.,Ridgill, Mark P.,Rowley, Michael,Grimwood, Sarah,Marshall, George R.
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p. 1145 - 1150
(2007/10/03)
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