Gerald Koelsch
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Explore the profile of Gerald Koelsch including associated specialties, affiliations and a list of published articles.
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20
Citations
491
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Recent Articles
1.
Shirasuna K, Koelsch G, Seidel-Dugan C, Salmeron A, Steiner P, Winston W, et al.
Cancer Treat Res Commun
. 2021 Jul;
28:100433.
PMID: 34273876
The T-cell immunoreceptor with Ig and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT) is a validated immune checkpoint protein expressed on memory CD4T-cellls, Tregs, CD8T-cell and natural killer (NK) cells....
2.
Ghosh A, Shin D, Downs D, Koelsch G, Lin X, Ermolieff J, et al.
J Am Chem Soc
. 2018 Nov;
122(14):3522-3523.
PMID: 30443047
No abstract available.
3.
Koelsch G
Molecules
. 2017 Oct;
22(10).
PMID: 29027981
Alzheimer's disease (AD) is a fatal progressive neurodegenerative disorder characterized by increasing loss in memory, cognition, and function of daily living. Among the many pathologic events observed in the progression...
4.
Ghosh A, Brindisi M, Yen Y, Xu X, Huang X, Devasamudram T, et al.
Bioorg Med Chem Lett
. 2014 Dec;
25(3):668-72.
PMID: 25537272
We describe structure-based design, synthesis, and biological evaluation of a series of novel inhibitors bearing a pyrazole (compounds 3a-h) or a thiazole moiety (compounds 4a-e) as the P3 ligand. We...
5.
Chang W, Huang X, Downs D, Cirrito J, Koelsch G, Holtzman D, et al.
FASEB J
. 2010 Nov;
25(2):775-84.
PMID: 21059748
Alzheimer disease is intimately linked to an excess amount of amyloid-β (Aβ) in the brain. Thus, therapeutic inhibition of Aβ production is an attractive clinical approach to treat this disease....
6.
Ghosh A, Kumaragurubaran N, Hong L, Kulkarni S, Xu X, Miller H, et al.
Bioorg Med Chem Lett
. 2008 Jan;
18(3):1031-6.
PMID: 18180160
Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic beta-secretase inhibitors incorporating hydroxyethylamine isosteres are described. We have identified inhibitor 24 which has shown exceedingly potent activity in...
7.
Ghosh A, Bilcer G, Hong L, Koelsch G, Tang J
Curr Alzheimer Res
. 2007 Oct;
4(4):418-22.
PMID: 17908045
A major strategy for the development of a disease-modifying therapy against Alzheimer's disease is pharmacological intervention designed to reduce levels of beta-amyloid in the brain. Among various ways of reducing...
8.
Ghosh A, Kumaragurubaran N, Hong L, Kulkarni S, Xu X, Chang W, et al.
J Med Chem
. 2007 Apr;
50(10):2399-407.
PMID: 17432843
Structure-based design and synthesis of a number of potent and selective memapsin 2 inhibitors are described. These inhibitors were designed based upon the X-ray structure of memapsin 2-bound inhibitor 3...
9.
Ghosh A, Kumaragurubaran N, Hong L, Lei H, Hussain K, Liu C, et al.
J Am Chem Soc
. 2006 Apr;
128(16):5310-1.
PMID: 16620080
Structure-based design, synthesis, and X-ray structure of protein-ligand complexes of memapsin 2 are described. The inhibitors are designed specifically to interact with S2- and S3-active site residues to provide selectivity...
10.
Turner 3rd R, Hong L, Koelsch G, Ghosh A, Tang J
Biochemistry
. 2005 Jan;
44(1):105-12.
PMID: 15628850
Memapsin 2 (beta-secretase) is the membrane-anchored aspartic protease that initiates the cleavage of beta-amyloid precursor protein (APP), leading to the production of amyloid-beta (Abeta), a major factor in the pathogenesis...