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Larry R McLean

Explore the profile of Larry R McLean including associated specialties, affiliations and a list of published articles. Areas
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Articles 7
Citations 113
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Recent Articles
1.
Vaz R, Li Y, Chellaraj V, Reiling S, Kuntzweiler T, Yang D, et al.
Bioorg Med Chem Lett . 2018 Aug; 28(19):3194-3196. PMID: 30146095
This work describes the rational amelioration of Cytochrome P450 4/5 (CYP3A4/5) induction through the Pregnane-X Receptor (PXR) pathway in a series of compounds that modulate the metabotropic glutamate Receptor 2...
2.
Deng G, Shen J, Yin M, McManus J, Mathieu M, Gee P, et al.
J Biol Chem . 2014 Nov; 290(2):762-74. PMID: 25391653
Cancer-associated point mutations in isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) confer a neomorphic enzymatic activity: the reduction of α-ketoglutarate to d-2-hydroxyglutaric acid, which is proposed to act as...
3.
Liang G, Chen X, Aldous S, Pu S, Mehdi S, Powers E, et al.
ACS Med Chem Lett . 2014 Jun; 3(2):159-64. PMID: 24900446
A series of compounds with an amidinothiophene P1 group and a pyrrolidinone-sulphonamide scaffold linker was identified as potent inhibitors of human kallikrein 6 by structure-based virtual screening based on the...
4.
McLean L, Zhang Y, Zaidi N, Bi X, Wang R, Dharanipragada R, et al.
Bioorg Med Chem Lett . 2012 Apr; 22(9):3296-300. PMID: 22464456
Beginning with a screening hit, unique thienopyrazole-indole inhibitors of Itk (interleukin-2-inducible tyrosine kinase) were designed, synthesized, and crystallized in the target kinase. Although initial compounds were highly active in Itk,...
5.
McLean L, Zhang Y, Li H, Choi Y, Han Z, Vaz R, et al.
Bioorg Med Chem Lett . 2010 Feb; 20(6):1821-4. PMID: 20185308
In the course of a fragment screening campaign by in silico docking followed by X-ray crystallography, a novel binding site for migration inhibitory factor (MIF) inhibitors was demonstrated. The site...
6.
McLean L, Zhang Y, Degnen W, Peppard J, Cabel D, Zou C, et al.
Bioorg Med Chem Lett . 2010 Feb; 20(6):1981-4. PMID: 20153645
Amino-benzoic acid derivatives 1-4 were found to be inhibitors for DHODH by virtual screening, biochemical, and X-ray crystallographic studies. X-ray structures showed that 1 and 2 bind to DHODH as...
7.
McLean L, Zhang Y, Li H, Li Z, Lukasczyk U, Choi Y, et al.
Bioorg Med Chem Lett . 2009 Oct; 19(23):6717-20. PMID: 19836948
Biochemical and X-ray crystallographic studies confirmed that hydroxyquinoline derivatives identified by virtual screening were actually covalent inhibitors of the MIF tautomerase. Adducts were formed by N-alkylation of the Pro-1 at...