- DIPEPTIDE ANALOGS AS TGF-BETA INHIBITORS
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The present disclosure is concerned with dipeptide analogs that are capable of inhibiting TGF-β and methods of treating cancers such as, for example, multiple myeloma and a hematologic malignancy, methods for immunotherapy, and methods of treating fibroti
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Paragraph 0457; 0489; 0493
(2019/05/15)
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- Multiple conformational states in crystals and in solution in αγ hybrid peptides. Fragility of the C12 helix in short sequences
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(Chemical Equation Presented) The conformational properties of foldamers generated from αγ hybrid peptide sequences have been probed in the model sequence Boc-Aib-Gpn-Aib-Gpn-NHMe. The choice of α-aminoisobutyryl (Aib) and gabapentin (Gpn) residues greatl
- Chatterjee, Sunanda,Vasudev, Prema G.,Ananda, Kuppanna,Raghothama, Srinivasarao,Shamala, Narayanaswamy,Balaram, Padmanabhan
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p. 6595 - 6606
(2008/12/22)
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- The photochemistry of N-p-toluenesulfonyl peptides: The peptide bond as an electron donor
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The scope of photobiological processes that involve absorbers within a protein matrix may be limited by the vulnerability of the peptide group to attack by highly reactive redox centers consequent upon electronic excitation. We have explored the nature of this vulnerability by undertaking comprehensive product analyses of aqueous photolysates of 12 N-p-toluene-sulfonyl peptides with systematically selected structures. The results indicate that degradation includes a major pathway that is initiated by intramolecular electron transfer in which the peptide bond serves as electron donor, and the data support the likelihood' of a relay process in dipeptide derivatives.
- Hill, Roger R.,Moore, Sharon A.,Roberts, David R.
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p. 1439 - 1446
(2008/02/01)
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- Contraste entre la phosphorylation des alcools et des amines par les 2-4 dioxo, oxa-1, aza-3 phospholanes-2
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Three new heterocycles 4 were synthesised either by reaction of the dichlorides 7 with the α hydroxyamide 8 in presence of two equivalents of silves tetrafluoroborate in pyridine (fig. 3), or by a hexamethyldisilazane promoted cyclization of the phosphoramide 12a (fig. 4), or by oxidation with Corey's reagent of the corresponding P(III) heterocycle 15 (fig. 5); phosphoranes 9 (fig. 3) and 16 (fig. 5) being formed as by products.Alcohols were easily phosphorylated with opening of the heterocycles 4 and rupture of the P2-N3 bond, after that of the exocyclic P-OPh bond in the case of 4b.Amines however, depending on the R1 substituent at phosphorus, either do not react (R1=Ph) or are axclusively phosphorylated with retention of the cyclic structure (R1=PhO).An explanation is proposed.
- Mulliez, Michel,Wolf, Robert
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p. 101 - 108
(2007/10/02)
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