Search Results - "Graziani, I"
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Mild Method for Succinimide Hydrolysis on ADCs: Impact on ADC Potency, Stability, Exposure, and Efficacy
Published in Bioconjugate chemistry (15-10-2014)“…The stability of the connection between the antibody and the toxin can have a profound impact on ADC safety and efficacy. There has been increasing evidence in…”
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2
Diversity oriented biosynthesis via accelerated evolution of modular gene clusters
Published in Nature communications (31-10-2017)“…Erythromycin, avermectin and rapamycin are clinically useful polyketide natural products produced on modular polyketide synthase multienzymes by an…”
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3
Sensitive, High Throughput Detection of Proteins in Individual, Surfactant-Stabilized Picoliter Droplets Using Nanoelectrospray Ionization Mass Spectrometry
Published in Analytical chemistry (Washington) (16-04-2013)“…Droplet-based fluidics is emerging as a powerful platform for single cell analysis, directed evolution of enzymes, and high throughput screening studies. Due…”
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Multivalent peptidic linker enables identification of preferred sites of conjugation for a potent thialanstatin antibody drug conjugate
Published in PloS one (30-05-2017)“…Antibody drug conjugates (ADCs) are no longer an unknown entity in the field of cancer therapy with the success of marketed ADCs like ADCETRIS and KADCYLA and…”
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Natural Product Bis-Intercalator Depsipeptides as a New Class of Payloads for Antibody–Drug Conjugates
Published in Bioconjugate chemistry (16-01-2019)“…A potent class of DNA-damaging agents, natural product bis-intercalator depsipeptides (NPBIDs), was evaluated as ultrapotent payloads for use in antibody–drug…”
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trans-Resveratrol induces apoptosis in human breast cancer cells MCF-7 by the activation of MAP kinases pathways
Published in Genes & nutrition (01-12-2007)“…Polyphenols represent a large class of plant-derived molecules with a general chemical structure that act as potent free radical scavengers. They have long…”
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7
Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities
Published in Proceedings of the National Academy of Sciences - PNAS (08-01-2008)“…Rapamycin is an immunosuppressive immunophilin ligand reported as having neurotrophic activity. We show that modification of rapamycin at the mammalian target…”
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Overcoming Amino-Nogo-induced Inhibition of Cell Spreading and Neurite Outgrowth by 12-O-Tetradecanoylphorbol-13-acetate-type Tumor Promoters
Published in The Journal of biological chemistry (26-02-2010)“…The N-terminal domain of NogoA, called amino-Nogo, inhibits axonal outgrowth and cell spreading via a largely unknown mechanism. In the present study, we show…”
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Amphotericin B, identified from a natural product screen, antagonizes CNS inhibitors to promote axon growth via activation of an Akt pathway in neurons
Published in Journal of neurochemistry (01-06-2010)“…J. Neurochem. (2010) 113, 1331-1342. One of the major barriers to successful axon regeneration in the adult CNS is the presence of inhibitory molecules that…”
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Recent advances in the chemistry, biosynthesis and pharmacology of rapamycin analogs
Published in Natural product reports (01-01-2009)“…Covering: 2003 to 2008. In the period 1998 to 2003, a number of reviews have appeared evaluating the potential of rapamycin and other immunophilin ligands as…”
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Septocylindrins A and B: Peptaibols Produced by the Terrestrial Fungus Septocylindrium sp. LL-Z1518
Published in Journal of natural products (Washington, D.C.) (01-03-2007)“…Two new peptaibols, septocylindrin A (1) and septocylindrin B (2), related to the well-studied membrane-channel-forming peptaibol alamethicin, were obtained…”
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12
Production of Novel Rapamycin Analogs by Precursor-Directed Biosynthesis
Published in Applied and Environmental Microbiology (01-04-2005)“…The natural product rapamycin, produced during fermentation by Streptomyces hygroscopicus, is known for its potent antifungal, immunosuppressive, and…”
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13
Unmasking the True Identity of Rapamycin’s Minor Conformer
Published in Journal of natural products (Washington, D.C.) (28-07-2023)“…Rapamycin, a well-known macrocyclic natural product with myriad biological activities, has been the subject of intense study since its first isolation and…”
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PF-06804103, A Site-specific Anti-HER2 Antibody–Drug Conjugate for the Treatment of HER2-expressing Breast, Gastric, and Lung Cancers
Published in Molecular cancer therapeutics (01-10-2020)“…The approval of ado-trastuzumab emtansine (T-DM1) in HER2+ metastatic breast cancer validated HER2 as a target for HER2-specific antibody–drug conjugates…”
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15
Mannopeptimycins, Novel Antibacterial Glycopeptides from Streptomyces hygroscopicus, LL-AC98
Published in Journal of the American Chemical Society (21-08-2002)“…A series of novel antibiotics with activity against methicillin-resistant staphylococci and vancomycin-resistant enterococci has been purified, and their…”
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Phaeochromycins A-E, anti-inflammatory polyketides isolated from the soil actinomycete Streptomyces phaeochromogenes LL-P018
Published in Journal of natural products (Washington, D.C.) (01-08-2005)“…Five new polyketide metabolites, phaeochromycins A-E (1-5), were isolated from an actinomycete designated Streptomyces phaeochromogenes LL-P018, cultured from…”
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3-Normeridamycin: A Potent Non-Immunosuppressive Immunophilin Ligand is Neuroprotective in Dopaminergic Neurons
Published in Journal of antibiotics (01-03-2006)“…3-Normeridamycin (1), isolated from fermentation extracts of the soil actinomycete Streptomyces sp. LL-C31037, demonstrated potent neuroprotective activity…”
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18
Natural Product Splicing Inhibitors: A New Class of Antibody–Drug Conjugate (ADC) Payloads
Published in Bioconjugate chemistry (17-08-2016)“…There is a considerable ongoing work to identify new cytotoxic payloads that are appropriate for antibody-based delivery, acting via mechanisms beyond DNA…”
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Site Selection: a Case Study in the Identification of Optimal Cysteine Engineered Antibody Drug Conjugates
Published in The AAPS journal (01-07-2017)“…As the antibody drug conjugate (ADC) community continues to shift towards site-specific conjugation technology, there is a growing need to understand how the…”
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Use of translational modeling and simulation for quantitative comparison of PF-06804103, a new generation HER2 ADC, with Trastuzumab-DM1
Published in Journal of pharmacokinetics and pharmacodynamics (01-10-2020)“…A modeling and simulation approach was used for quantitative comparison of a new generation HER2 antibody drug conjugate (ADC, PF-06804103) with…”
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