Wayne Grant
Overview
Explore the profile of Wayne Grant including associated specialties, affiliations and a list of published articles.
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Articles
21
Citations
603
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Recent Articles
1.
Choi J, Noguchi Y, Alburger J, Bayle S, Chung E, Grant W, et al.
J Med Chem
. 2023 May;
66(11):7162-7178.
PMID: 37204207
Specific inhibition of a single kinase isoform is a challenging task due to the highly conserved nature of ATP-binding sites. Casein kinase 1 (CK1) δ and ε share 97% sequence...
2.
Vena F, Bayle S, Nieto A, Quereda V, Aceti M, Frydman S, et al.
Mol Cancer Ther
. 2020 May;
19(8):1623-1635.
PMID: 32430484
Although gemcitabine is the cornerstone of care for pancreatic ductal adenocarcinoma (PDA), patients lack durable responses and relapse is inevitable. While the underlying mechanisms leading to gemcitabine resistance are likely...
3.
Nieto A, Hara M, Quereda V, Grant W, Saunders V, Xiao K, et al.
Cell Death Differ
. 2019 Sep;
27(4):1200-1213.
PMID: 31506606
Cellular DNA is constantly under threat from internal and external insults, consequently multiple pathways have evolved to maintain chromosomal fidelity. Our previous studies revealed that chronic stress, mediated by continuous...
4.
Monastyrskyi A, Nilchan N, Quereda V, Noguchi Y, Ruiz C, Grant W, et al.
Bioorg Med Chem
. 2018 Jan;
26(3):590-602.
PMID: 29289448
Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series...
5.
Monastyrskyi A, Bayle S, Quereda V, Grant W, Cameron M, Duckett D, et al.
Bioorg Med Chem Lett
. 2017 Dec;
28(3):400-404.
PMID: 29277458
The development of a new series of apoptosis signal-regulating kinase 1 (ASK1) inhibitors is described. Starting from purine, pyrimidine and quinazoline scaffolds identified by high throughput screening, we used tools...
6.
Wood S, Grant W, Adrados I, Choi J, Alburger J, Duckett D, et al.
ACS Med Chem Lett
. 2017 Dec;
8(12):1258-1263.
PMID: 29259744
We present the outcome of an high throughput screen (HTS) and optimization of a small molecule Unc-51-Like Kinase 1 (ULK1) inhibitor hit, , with an indazole core. Docking studies guided...
7.
Rosenberg L, Lafitte M, Quereda V, Grant W, Chen W, Bibian M, et al.
Sci Transl Med
. 2015 Dec;
7(318):318ra202.
PMID: 26676609
Identification of specific drivers of human cancer is required to instruct the development of targeted therapeutics. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that...
8.
Rosenberg L, Lafitte M, Grant W, Chen W, Cleveland J, Duckett D
J Biomol Screen
. 2015 Apr;
20(7):913-20.
PMID: 25851035
A rapidly accumulating body of work suggests the autophagy pathway is an attractive therapeutic target for neurodegenerative diseases and cancer. To validate autophagy as an anticancer strategy and to assess...
9.
Yin Y, Cameron M, Lin L, Khan S, Schroter T, Grant W, et al.
ACS Med Chem Lett
. 2014 Jun;
1(4):175-9.
PMID: 24900192
A series of urea-based Rho kinase (ROCK) inhibitors were designed and evaluated. The discovered compounds had excellent enzyme and cellular potency, high kinase selectivity, high aqueous solubility, good porcine corneal...
10.
Yin Y, Lin L, Ruiz C, Khan S, Cameron M, Grant W, et al.
J Med Chem
. 2013 Apr;
56(9):3568-81.
PMID: 23570561
RhoA and its downstream effector ROCK mediate stress fiber formation and cell contraction through their effects on the phosphorylation of myosin light chain (MLC). Inhibition of the RhoA/ROCK pathway has...