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Targeting protein-protein interactions for therapeutic intervention: a challenge for the future.
BACKGROUND Over the last two decades, an increasing research effort in academia and industry has focused on the modulation (both inhibition and stabilization) of protein-protein interactions (PPIs)Expand
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Chemistry and Pharmacology of Anticancer Drugs
INTRODUCTION TO CANCER Terminology Metastases Diagnosis and Screening Formation of Cancer Cells (Tumorigenesis) Mechanisms of Genomic Damage Treatments Discovery of Anticancer Drugs and PreclinicalExpand
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Advances in the Study of Pyrrolo[2,1-c] [1,4]benzodiazepine (PBD) Antitumour Antibiotics
There is growing interest in agents, such as the pyrrolo[2,1-c][1,4]benzodiazepines (PBDs), that can recognize and bond to specific sequences of DNA. They have potential as gene regulators withExpand
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The XPF-ERCC1 endonuclease and homologous recombination contribute to the repair of minor groove DNA interstrand crosslinks in mammalian cells produced by the pyrrolo[2,1-c][1,4]benzodiazepine dimer
SJG-136, a pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimer, is a highly efficient interstrand crosslinking agent that reacts with guanine bases in a 5′-GATC-3′ sequence in the DNA minor groove. SJG-136Expand
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Observation of unphosphorylated STAT3 core protein binding to target dsDNA by PEMSA and X‐ray crystallography
pSTAT3βtc and pSTAT3βtc bind by molecular sieving (View interaction)
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Pyrrolo[1,4]benzodiazepine antitumor antibiotics: relationship of DNA alkylation and sequence specificity to the biological activity of natural and synthetic compounds.
The DNA alkylation and sequence specificity of a group of natural and synthetic pyrrolo-[1,4]benzodiazepines [P(1,4)Bs] were evaluated by using an exonuclease III stop assay, and the results wereExpand
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Chemical approaches to the discovery and development of cancer therapies
The chemical sciences are essential for the process of anticancer-drug discovery, and a range of chemical research techniques is needed to develop clinically effective drugs. Improved understandingExpand
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SJG-136 (NSC 694501), a Novel Rationally Designed DNA Minor Groove Interstrand Cross-Linking Agent with Potent and Broad Spectrum Antitumor Activity
SJG-136 (NSC 694501) is a rationally designed pyrrolobenzodiazepine dimer that binds in the minor groove of DNA. It spans 6 bp with a preference for binding to purine-GATC-pyrimidine sequences. TheExpand
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O-Debenzylation of a Pyrrolo[2,1-c][1,4]benzodiazepine in the Presence of a Carbinolamine Functionality: Synthesis of DC-81
In contrast to other methods of reduction, catalytic transfer hydrogenation allows debenzylation of a phenolic hydroxyl in a carbinolamine-containing pyrolo[2,1-c][1,4]benzodiazepine, while leavingExpand
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Investigation of the protein alkylation sites of the STAT3:STAT3 inhibitor Stattic by mass spectrometry.
STAT3 (Signal Transducer and Activator of Transcription factor 3) is constitutively active in a wide range of human tumours. Stattic is one of the first non-peptidic small molecules reported toExpand
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