Nanhua Yao
Overview
Explore the profile of Nanhua Yao including associated specialties, affiliations and a list of published articles.
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32
Citations
323
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Recent Articles
1.
Mondal K, Regnstrom K, Morishige W, Barbour R, Probst G, Xu Y, et al.
Biochem Biophys Res Commun
. 2013 Sep;
441(2):291-6.
PMID: 24070613
Alzheimer's disease (AD) is a devastating neurodegenerative disease affecting millions of people. β-Secretase-1 (BACE-1), an enzyme involved in the processing of the amyloid precursor protein (APP) to form Aβ, is...
2.
Ng R, Sun M, Bowers S, Hom R, Probst G, John V, et al.
Bioorg Med Chem Lett
. 2013 Jul;
23(16):4674-9.
PMID: 23856050
The structure activity relationship of the prime region of conformationally restricted hydroxyethylamine (HEA) BACE inhibitors is described. Variation of the P1' region provided selectivity over Cat-D with a series of...
3.
Aubele D, Hom R, Adler M, Galemmo Jr R, Bowers S, Truong A, et al.
ChemMedChem
. 2013 Jun;
8(8):1295-313.
PMID: 23794260
Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of α-synuclein in Lewy bodies, which are one of the hallmarks of Parkinson's disease neuropathology. Potent,...
4.
Xu Y, Yuan S, Bowers S, Hom R, Chan W, Sham H, et al.
Bioorg Med Chem Lett
. 2013 Apr;
23(10):3075-80.
PMID: 23570791
Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50=8nM) was made from a weak μM...
5.
Bowers S, Xu Y, Yuan S, Probst G, Hom R, Chan W, et al.
Bioorg Med Chem Lett
. 2013 Mar;
23(7):2181-6.
PMID: 23465612
The structure-activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described. Application of structure-based design to screening hit 1 yielded sub-micromolar inhibitors. Replacement of the carboxylic acid of 1...
6.
Bowers S, Truong A, Neitz R, Hom R, Sealy J, Probst G, et al.
Bioorg Med Chem Lett
. 2011 Aug;
21(18):5521-7.
PMID: 21813278
The SAR of a series of brain penetrant, trisubstituted thiophene based JNK inhibitors with improved pharmacokinetic properties is described. These compounds were designed based on information derived from metabolite identification...
7.
Bowers S, Truong A, Neitz R, Neitzel M, Probst G, Hom R, et al.
Bioorg Med Chem Lett
. 2011 Feb;
21(6):1838-43.
PMID: 21316234
The SAR of a series of tri-substituted thiophene JNK3 inhibitors is described. By optimizing both the N-aryl acetamide region of the inhibitor and the 4-position of the thiophene we obtained...
8.
Probst G, Bowers S, Sealy J, Truong A, Hom R, Galemmo Jr R, et al.
Bioorg Med Chem Lett
. 2010 Nov;
21(1):315-9.
PMID: 21112785
In this Letter, we describe the discovery of selective JNK2 and JNK3 inhibitors, such as 10, that routinely exhibit >10-fold selectivity over JNK1 and >1000-fold selectivity over related MAPKs, p38α...
9.
Hom R, Bowers S, Sealy J, Truong A, Probst G, Neitzel M, et al.
Bioorg Med Chem Lett
. 2010 Nov;
20(24):7303-7.
PMID: 21071223
From high throughput screening, we discovered compound 1, the prototype for a series of disubstituted thiophene inhibitors of JNK which is selective towards closely related MAP kinases p38 and Erk2....
10.
Probst G, Bowers S, Sealy J, Stupi B, Dressen D, Jagodzinska B, et al.
Bioorg Med Chem Lett
. 2010 Sep;
20(20):6034-9.
PMID: 20822903
The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with...