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Showing 1 to 12 of 808 entries
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A Positive Selection for Nucleoside Kinases in E. coli.

PloS one

Shelat NY, Parhi S, Ostermeier M.
PMID: 27677184
PLoS One. 2016 Sep 27;11(9):e0162921. doi: 10.1371/journal.pone.0162921. eCollection 2016.

Engineering heterologous nucleoside kinases inside E. coli is a difficult process due to the integral role nucleosides play in cell division and transcription. Nucleoside analogs are used in many kinase screens that depend on cellular metabolization of the analogs....

Study on fluorouracil-chitosan nanoparticle preparation and its antitumor effect.

Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society

Chen G, Gong R.
PMID: 27275110
Saudi Pharm J. 2016 May;24(3):250-3. doi: 10.1016/j.jsps.2016.04.008. Epub 2016 Apr 23.

To successfully prepare fluorouracil-chitosan nanoparticles, and further analyze its anti-tumor activity mechanism, this paper makes a comprehensive study of existing preparation prescription and makes a detailed analysis of fluorouracil-chitosan in vitro release and pharmacodynamic behavior of animals. Two-step synthesis...

Encapsulation of Pt(IV) Prodrugs within a Pt(II) Cage for Drug Delivery.

Chemical science

Zheng YR, Suntharalingam K, Johnstone TC, Lippard SJ.
PMID: 25621144
Chem Sci. 2015 Feb 01;6(2):1189-1193. doi: 10.1039/C4SC01892C.

This report presents a novel strategy that facilitates delivery of multiple, specific payloads of Pt(IV) prodrugs using a well-defined supramolecular system. This delivery system comprises a hexanuclear Pt(II) cage that can host four Pt(IV) prodrug guest molecules. Relying on...

Efficient activation of a visible light-activatable CA4 prodrug through intermolecular photo-unclick chemistry in mitochondria.

Chemical communications (Cambridge, England)

Bio M, Rajaputra P, Lim I, Thapa P, Tienabeso B, Hurst RE, You Y.
PMID: 28111669
Chem Commun (Camb). 2017 Feb 07;53(11):1884-1887. doi: 10.1039/c6cc09994g. Epub 2017 Jan 23.

Photo-unclick chemistry mediates visible and near IR-controlled drug release via a singlet oxygen (SO)-cleavable linker. Due to the limited diffusion distance of SO in biological systems, a photosensitizer and the SO-cleavable linker have been conjugated in one molecule or...

Macromolecular prodrugs of ribavirin: towards a treatment for co-infection with HIV and HCV.

Chemical science

Smith AAA, Zuwala K, Kryger MBL, Wohl BM, Guerrero-Sanchez C, Tolstrup M, Postma A, Zelikin AN.
PMID: 28580095
Chem Sci. 2015 Jan 01;6(1):264-269. doi: 10.1039/c4sc02754j. Epub 2014 Sep 16.

Human immunodeficiency virus (HIV) and hepatitis C virus (HCV) represent tremendous healthcare burdens with a large proportion of patients hosting the two viruses at the same time. An altered hepatic function and immunity as well as cross-interference of drugs...

Glutathione Transferase (GST)-Activated Prodrugs.

Pharmaceutics

Ruzza P, Calderan A.
PMID: 24300447
Pharmaceutics. 2013 Apr 02;5(2):220-31. doi: 10.3390/pharmaceutics5020220.

Glutathione transferase (formerly GST) catalyzes the inactivation of various electrophile-producing anticancer agents via conjugation to the tripeptide glutathione. Moreover, several data link the overexpression of some GSTs, in particular GSTP1-1, to both natural and acquired resistance to various structurally...

Glycosystems in nanotechnology: Gold glyconanoparticles as carrier for anti-HIV prodrugs.

Beilstein journal of organic chemistry

Chiodo F, Marradi M, Calvo J, Yuste E, Penadés S.
PMID: 24991287
Beilstein J Org Chem. 2014 Jun 12;10:1339-46. doi: 10.3762/bjoc.10.136. eCollection 2014.

The therapeutic approach for the treatment of HIV infection is based on the highly active antiretroviral therapy (HAART), a cocktail of antiretroviral drugs. Notwithstanding HAART has shown different drawbacks like toxic side effects and the emergence of viral multidrug...

Synthesis of phenylazonaphtol-β-D-O-glycosides, evaluation as substrates for beta-glycosidase activity and molecular studies.

Organic and medicinal chemistry letters

Brito-Arias M, Aguilar-Lemus C, Hurtado-Ponce PB, Martínez-Barrón G, Ibañez-Hernandez M.
PMID: 24995152
Org Med Chem Lett. 2014 May 17;4:2. doi: 10.1186/2191-2858-4-2. eCollection 2014.

BACKGROUND: Phenylazonaphtol-β-D-O-glycosides are alternative substrates for the detection of enzymatic activity of β-glycosidases which are involved in various important processes. These azoic compounds are currently exploited as prodrugs for colonic disease due the presence of β-glycosidase activity in the...

Maintenance of glutathione levels and its importance in epigenetic regulation.

Frontiers in pharmacology

García-Giménez JL, Pallardó FV.
PMID: 24847264
Front Pharmacol. 2014 May 05;5:88. doi: 10.3389/fphar.2014.00088. eCollection 2014.

No abstract available.

Intramolecular Rearrangement of α-Amino Acid Amide Derivatives of 2-Aminobenzothiazoles.

Tetrahedron letters

Pelletier JC, Velvadapu V, McDonnell ME, Wrobel JE, Reitz AB.
PMID: 25018567
Tetrahedron Lett. 2014 Jul 23;55(30):4193-4195. doi: 10.1016/j.tetlet.2014.05.046.

We have found that α-amino acid amide derivatives of 2-aminobenzothiazoles undergo a time-dependent, thermal rearrangement in which the amine group attacks the 2-position carbon of the thiazole ring to form a 5,5-spiro ring system. This is followed by sulfur...

An N-Acetyl Cysteine Ruthenium Tricarbonyl Conjugate Enables Simultaneous Release of CO and Ablation of Reactive Oxygen Species.

Chemistry (Weinheim an der Bergstrasse, Germany)

Seixas JD, Chaves-Ferreira M, Montes-Grajales D, Gonçalves AM, Marques AR, Saraiva LM, Olivero-Verbel J, Romão CC, Bernardes GJ.
PMID: 26316066
Chemistry. 2015 Oct 12;21(42):14708-12. doi: 10.1002/chem.201502474. Epub 2015 Aug 28.

We have designed and synthesised a [Ru(CO)3 Cl2 (NAC)] pro-drug that features an N-acetyl cysteine (NAC) ligand. This NAC carbon monoxide releasing molecule (CORM) conjugate is able to simultaneously release biologically active CO and to ablate the concurrent formation...

Targeting the PD-1/PD-L1 Immune Evasion Axis With DNA Aptamers as a Novel Therapeutic Strategy for the Treatment of Disseminated Cancers.

Molecular therapy. Nucleic acids

Prodeus A, Abdul-Wahid A, Fischer NW, Huang EH, Cydzik M, Gariépy J.
PMID: 25919090
Mol Ther Nucleic Acids. 2015 Apr 28;4:e237. doi: 10.1038/mtna.2015.11.

Blocking the immunoinhibitory PD-1:PD-L1 pathway using monoclonal antibodies has led to dramatic clinical responses by reversing tumor immune evasion and provoking robust and durable antitumor responses. Anti-PD-1 antibodies have now been approved for the treatment of melanoma, and are...

Showing 1 to 12 of 808 entries