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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
Chemistry and Pharmacology of Anticancer Drugs
- D. Thurston
- 22 November 2006
INTRODUCTION TO CANCER Terminology Metastases Diagnosis and Screening Formation of Cancer Cells (Tumorigenesis) Mechanisms of Genomic Damage Treatments Discovery of Anticancer Drugs and Preclinical… Expand
Advances in the Study of Pyrrolo[2,1-c] [1,4]benzodiazepine (PBD) Antitumour Antibiotics
- D. Thurston
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 with… Expand
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-136… Expand
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)
Pyrrolo[1,4]benzodiazepine antitumor antibiotics: relationship of DNA alkylation and sequence specificity to the biological activity of natural and synthetic compounds.
- L. Hurley, T. Reck, +7 authors S. Mong
- Chemistry, Medicine
- Chemical research in toxicology
- 1 September 1988
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 were… Expand
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 understanding… Expand
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. The… Expand
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 leaving… Expand
Investigation of the protein alkylation sites of the STAT3:STAT3 inhibitor Stattic by mass spectrometry.
- S. Heidelberger, G. Zinzalla, +9 authors D. Thurston
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 15 August 2013
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 to… Expand