Target Actionability Review: a systematic evaluation of replication stress as a therapeutic target for paediatric solid malignancies

European Journal of Cancer ◽

10.1016/j.ejca.2021.11.030 ◽

2022 ◽

Vol 162 ◽

pp. 107-117

Author(s):

Kaylee M. Keller ◽

Sonja Krausert ◽

Apurva Gopisetty ◽

Dan Luedtke ◽

Jan Koster ◽

...

Keyword(s):

Therapeutic Target ◽

Replication Stress ◽

Systematic Evaluation ◽

Solid Malignancies

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Replication stress: Driver and therapeutic target in genomically instable cancers

DNA Repair - Advances in Protein Chemistry and Structural Biology ◽

10.1016/bs.apcsb.2018.10.006 ◽

2019 ◽

pp. 157-201 ◽

Cited By ~ 3

Author(s):

Pepijn M. Schoonen ◽

Sergi Guerrero Llobet ◽

Marcel A.T.M. van Vugt

Keyword(s):

Therapeutic Target ◽

Replication Stress

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P08.36 Radioresistance of glioblastoma stem-like cells is associated with DNA replication stress, which is a promising therapeutic target

Neuro-Oncology ◽

10.1093/neuonc/now188.169 ◽

2016 ◽

Vol 18 (suppl_4) ◽

pp. iv49-iv49

Author(s):

S. U. Ahmed ◽

R. Carruthers ◽

D. Biasoli ◽

N. Gomez-Roman ◽

L. Gilmour ◽

...

Keyword(s):

Dna Replication ◽

Therapeutic Target ◽

Replication Stress ◽

Promising Therapeutic Target ◽

Dna Replication Stress

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Image Analysis of Intramembrane Particles in Freeze-Fractured Biomembranes Using Computer Simulation Techniques

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100114694 ◽

1975 ◽

Vol 33 ◽

pp. 214-215

Author(s):

D.J. Benefiel ◽

R.S. Weinstein

Keyword(s):

Membrane Proteins ◽

Freeze Fracture ◽

Integral Membrane Proteins ◽

Systematic Evaluation ◽

Intramembrane Particles ◽

Modeling Methods ◽

Simulation Techniques ◽

Freeze Fracture Electron Microscopy ◽

Fracture Electron ◽

Computer Simulation Techniques

Intramembrane particles (IMP or MAP) are components of most biomembranes. They are visualized by freeze-fracture electron microscopy, and they probably represent replicas of integral membrane proteins. The presence of MAP in biomembranes has been extensively investigated but their detailed ultrastructure has been largely ignored. In this study, we have attempted to lay groundwork for a systematic evaluation of MAP ultrastructure. Using mathematical modeling methods, we have simulated the electron optical appearances of idealized globular proteins as they might be expected to appear in replicas under defined conditions. By comparing these images with the apearances of MAPs in replicas, we have attempted to evaluate dimensional and shape distortions that may be introduced by the freeze-fracture technique and further to deduce the actual shapes of integral membrane proteins from their freezefracture images.

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Memapsin 2, a drug target for Alzheimer's disease

Biochemical Society Symposium ◽

10.1042/bss0700213 ◽

2003 ◽

Vol 70 ◽

pp. 213-220 ◽

Cited By ~ 1

Author(s):

Gerald Koelsch ◽

Robert T. Turner ◽

Lin Hong ◽

Arun K. Ghosh ◽

Jordan Tang

Keyword(s):

Crystal Structure ◽

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Transition State ◽

Amyloid Precursor Protein ◽

Therapeutic Target ◽

Drug Target ◽

Aspartic Protease ◽

Precursor Protein ◽

Memapsin 2

Mempasin 2, a ϐ-secretase, is the membrane-anchored aspartic protease that initiates the cleavage of amyloid precursor protein leading to the production of ϐ-amyloid and the onset of Alzheimer's disease. Thus memapsin 2 is a major therapeutic target for the development of inhibitor drugs for the disease. Many biochemical tools, such as the specificity and crystal structure, have been established and have led to the design of potent and relatively small transition-state inhibitors. Although developing a clinically viable mempasin 2 inhibitor remains challenging, progress to date renders hope that memapsin 2 inhibitors may ultimately be useful for therapeutic reduction of ϐ-amyloid.

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