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1.
Chem Commun (Camb) ; 55(2): 253-256, 2018 Dec 20.
Artigo em Inglês | MEDLINE | ID: mdl-30534737

RESUMO

We describe the preparation of a cancer vaccine candidate by conjugating a MUC1 peptide antigen to the ß-glucan polysaccharide, which serves both as a carrier and an immune activator. In contrast to amorphous polysaccharides, peptide-ß-glucan conjugates form uniform nanoparticles that facilitate the delivery of antigens and binding to myeloid cells, thus leading to the activation of both innate and adaptive immunity.


Assuntos
Adenocarcinoma/imunologia , Vacinas Anticâncer/imunologia , Portadores de Fármacos/química , Mucina-1/imunologia , Fragmentos de Peptídeos/imunologia , beta-Glucanas/química , Imunidade Adaptativa/imunologia , Sequência de Aminoácidos , Animais , Vacinas Anticâncer/síntese química , Vacinas Anticâncer/química , Humanos , Imunidade Ativa/imunologia , Imunoglobulina G/imunologia , Imunoglobulina G/metabolismo , Imunoglobulina M/imunologia , Imunoglobulina M/metabolismo , Interferon gama/metabolismo , Interleucina-6/metabolismo , Células MCF-7 , Camundongos Endogâmicos C57BL , Mucina-1/química , Fragmentos de Peptídeos/química , Vacinas de Subunidades/síntese química , Vacinas de Subunidades/química , Vacinas de Subunidades/imunologia , Vacinas Sintéticas/química , Vacinas Sintéticas/imunologia
2.
Chem Sci ; 9(7): 1940-1946, 2018 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-29675240

RESUMO

Peptidyl thioesters or their surrogates with C-terminal ß-branched hydrophobic amino acid residues usually exhibit poor reactivities in ligation reactions. Thus, activation using exogenous additives is required to ensure an acceptable reaction efficiency. Herein, we report a traceless ligation at Val-Xaa sites under mild thiol additive-free reaction conditions, whereby the introduction of ß-mercaptan on the C-terminal valine residue effectively activates the otherwise unreactive N-acyl-benzimidazolinone (Nbz), and enables the use of a one-pot ligation-desulfurization strategy to generate the desired peptide products. The orthogonality between ß-thiovaline-Nbz and a conventional alkyl thioester, as well as the convenient access to the former from readily available penicillamine, also allowed expedited assembly of the peptidic hormone ß-LPH and hPTH analogues, based on a kinetically controlled one-pot three-segment ligation and desulfurization strategy.

3.
Org Lett ; 18(3): 624-7, 2016 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-26812626

RESUMO

A concise, asymmetric total synthesis of (+)-fusarisetin A, a hybrid natural product, has been achieved. A one-pot four-reaction process efficiently delivered the tetracycle 2 which served as a key intermediate for the synthesis of the title natural product and its analogues through amino acid incorporation.


Assuntos
Antineoplásicos/síntese química , Produtos Biológicos/síntese química , Compostos Heterocíclicos de 4 ou mais Anéis/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Fusarium/química , Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Estrutura Molecular , Microbiologia do Solo , Estereoisomerismo
4.
Org Lett ; 17(21): 5480-3, 2015 Nov 06.
Artigo em Inglês | MEDLINE | ID: mdl-26509873

RESUMO

A concise, protecting-group-free total synthesis of (-)-jiadifenolide, a synthetically challenging seco-prezizaane sesquiterpene with potent neurotrophic activity, is reported. The convergent route features a SmI2/H2O-mediated stereoselective reductive cyclization, an unprecedented formal [4 + 1] annulative tetrahydrofuran-forming reaction and programmed redox manipulations. The newly developed annulation of ß-hydroxy aldehydes or ketones with lithium trimethylsilyldiazomethane provides access to a diverse array of multisubstituted tetrahydrofurans. The synthetic jiadifenolide exhibited weak cytotoxicity against five human cancer cell lines.


Assuntos
Antineoplásicos/síntese química , Furanos/química , Sesquiterpenos/síntese química , Aldeídos , Antineoplásicos/química , Antineoplásicos/farmacologia , Ciclização , Illicium/química , Estrutura Molecular , Oxirredução , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Estereoisomerismo
5.
Fish Shellfish Immunol ; 23(1): 52-61, 2007 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-17350861

RESUMO

ISG15 is one of the most strongly induced genes upon viral infection, interferon (IFN) stimulation, and lipopolysaccharide (LPS) stimulation, and only one copy has been found in mammals so far. Here two fish ISG15 genes, termed CaISG15-1 and CaISG15-2, have been cloned and sequenced from UV-inactivated GCHV (grass carp haemorrhagic virus)-infected and IFN-produced CAB cells (crucian carp Carassius auratus blastulae embryonic cells) by suppression subtractive hybridization. The full-length cDNA sequences of two crucian carp ISG15 encode a 155-amino-acid protein and a 161-amino-acid protein, both of which show 78.9% identity overall and possess the characteristic structures of mammalian ISG15 proteins including two tandem ubiquitin-like domains and the C-terminal canonical LRLRGG motif. In CAB cells treated with different stimuli including active virus, UV-inactivated GCHV and IFN containing supernatant (ICS), the expression of both CaISG15-1 and CaISG15-2 was upregulated but displayed different kinetics. Poly I:C and LPS were also able to induce an increase in mRNA for both genes. In CAB cells responsive to active GCHV, UV-inactivated GCHV, CAB ICS, Poly I:C and LPS, CaISG15-1 was upregulated more significantly than CaISG15-2. These results suggest that there are two ISG15 homologues in crucian carp, both of which might play distinct roles in innate immunity against viral and bacterial infection.


Assuntos
Carpas/genética , Citocinas/genética , Filogenia , Ubiquitinas/genética , Sequência de Aminoácidos , Animais , Sequência de Bases , Carpas/imunologia , Análise por Conglomerados , Citocinas/metabolismo , Primers do DNA , Imunidade Inata , Dados de Sequência Molecular , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Alinhamento de Sequência , Análise de Sequência de DNA , Ubiquitinas/metabolismo
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