A5101944189- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- DNA and Nucleic Acid Chemistry
- Enzyme function and inhibition
- Biochemical and Molecular Research
- Enzyme Structure and Function
- Beetle Biology and Toxicology Studies
- Skin and Cellular Biology Research
- Innovations in Medical Education
- Advanced biosensing and bioanalysis techniques
- Cancer therapeutics and mechanisms
- NF-κB Signaling Pathways
- Phosphodiesterase function and regulation
- Cell death mechanisms and regulation
- Phagocytosis and Immune Regulation
- Lanthanide and Transition Metal Complexes
- Healthcare Policy and Management
- interferon and immune responses
- Immune cells in cancer
- RNA Interference and Gene Delivery
- RNA and protein synthesis mechanisms
- Cytokine Signaling Pathways and Interactions
- Drug-Induced Ocular Toxicity
- Medical Education and Admissions
- HIV/AIDS drug development and treatment
- Peptidase Inhibition and Analysis
GlaxoSmithKline (United Kingdom)
2005-2021
GlaxoSmithKline (India)
2019
South College
2018
GlaxoSmithKline (United States)
2018
Kansas City University
2013
University of Reading
1999-2004
University of Auckland
1999-2000
Cancer Society of New Zealand
1999-2000
Trinity College Dublin
1999
University College Dublin
1999
RIP1 regulates cell death and inflammation is believed to play an important role in contributing a variety of human pathologies, including immune-mediated inflammatory diseases cancer. While small-molecule inhibitors kinase have been advanced the clinic for CNS indications, oncology indications yet be described. Herein we report on discovery profile GSK3145095 (compound 6). Compound 6 potently binds with exquisite specificity has excellent activity blocking kinase-dependent cellular...
RIP1 kinase regulates necroptosis and inflammation may play an important role in contributing to a variety of human pathologies, including inflammatory neurological diseases. Currently, inhibitors have advanced into early clinical trials for evaluation diseases such as psoriasis, rheumatoid arthritis, ulcerative colitis amyotrophic lateral sclerosis Alzheimer's disease. In this paper, we report on the design potent highly selective dihydropyrazole (DHP) starting from high-throughput screen...
ADVERTISEMENT RETURN TO ISSUEPREVLetterNEXTMajor Groove Binding and 'DNA-Induced' Fit in the Intercalation of a Derivative Mixed Topoisomerase I/II Poison N-(2-(Dimethylamino)ethyl)acridine-4- carboxamide (DACA) into DNA: X-ray Structure Complexed to d(CG(5-BrU)ACG)2 at 1.3-Å ResolutionAlan K. Todd, Adrienne Adams, James H. Thorpe, William A. Denny, Laurence P. G. Wakelin, Christine J. CardinView Author Information Chemistry Department, University Reading, Whiteknights, Reading RG6 6AD,...
The structure of the duplex d[CG(5-BrU)ACG](2) bound to 9-bromophenazine-4-carboxamide has been solved through MAD phasing at 2.0 A resolution. It shows an unexpected and previously unreported intercalation cavity stabilized by drug novel binding modes Co(2+) ions certain guanine N7 sites. For terminal cytosine is rotated pair with a symmetry-related create pseudo-Holliday junction geometry, two such cavities linked minor groove interactions N2/N3 sites angle 40 degrees, creating...
DNA-strand exchange is a vital step in the recombination process, of which key intermediate four-way DNA Holliday junction formed transiently most living organisms. Here, single-crystal structure at resolution 2.35 A such by d(CCGGTACCGG)(2), has crystallized more highly symmetrical packing mode to that previously observed for same sequence, presented. In this case, isomorphous mismatch sequence d(CCGGGACCGG)(2), reveals roles both lattice and determining geometry. The helices cross larger...
Initial Experience with and Potential of Data Processing Computer Technics in a Hospital Clinical Laboratory Get access E. R. Gabiueli, Gabiueli Search for other works by this author on: Oxford Academic Google Scholar V. Pessin, Pessin J. Thorpe, Thorpe C. Palmer American Journal Pathology, Volume 47, Issue 1, 1 January 1967, Pages 60–68, https://doi.org/10.1093/ajcp/47.1.60 Published: 01 1967 Article history Received: 18 February 1966
The inhibition of kallikrein 5 (KLK5) has been identified as a potential strategy for treatment the genetic skin disorder Netherton syndrome, in which loss-of-function mutations SPINK5 gene lead to down-regulation endogenous inhibitor LEKTI-1 and profound skin-barrier defects with severe allergic manifestations. To aid development medicine this target, an X-ray crystallographic system was developed facilitate fragment-guided chemistry knowledge-based drug-discovery approaches. Here,...
Direct soaking of protein crystals with small-molecule fragments grouped into complementary clusters is a useful technique when assessing the potential new crystal system to support structure-guided drug discovery. It provides robustness check prior any extensive screening, double for assay binding cutoffs and structural data pockets that may or not be picked out in measurements. The output from this three novel fragment molecules identified bind antibacterial target Acinetobacter baumannii...
A four-wavelength MAD experiment on a new brominated octanucleotide is reported here. d[ACGTACG(5-BrU)], C 77 H 81 BrN 30 O 32 P 7 , M_r (DNA) = 2235, tetragonal, 4 3 2 1 (No. 96), 43.597, c 26.268 Å, V 49927.5 Å Z 8, T 100 K, R 10.91% for 4312 reflections between 15.0 and 1.46 resolution. The self-complementary d[ACGTACG(5-BrU)] has been crystallized data measured to 1.45 at both 293 K second crystal flash frozen K. latter collection was carried out the same resolution four wavelengths...