Blaise Lippa
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Explore the profile of Blaise Lippa including associated specialties, affiliations and a list of published articles.
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17
Citations
173
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Recent Articles
11.
Zhang J, Romero J, Chan A, Goss J, Stucka S, Cross J, et al.
Bioorg Med Chem Lett
. 2015 Jun;
25(17):3661-4.
PMID: 26117562
Inflammatory bowel disease, including Crohn's disease and ulcerative colitis, affects millions of people worldwide. CCR9 has been shown to be a key chemokine receptor mediating the local inflammatory responses in...
12.
Bhattacharya S, Aspnes G, Bagley S, Boehm M, Brosius A, Buckbinder L, et al.
Bioorg Med Chem Lett
. 2012 Nov;
22(24):7523-9.
PMID: 23153798
Previous drug discovery efforts identified classical PYK2 kinase inhibitors such as 2 and 3 that possess selectivity for PYK2 over its intra-family isoform FAK. Efforts to identify more kinome-selective chemical...
13.
Freeman-Cook K, Autry C, Borzillo G, Gordon D, Barbacci-Tobin E, Bernardo V, et al.
J Med Chem
. 2010 May;
53(12):4615-22.
PMID: 20481595
This paper describes the design and synthesis of novel, ATP-competitive Akt inhibitors from an elaborated 3-aminopyrrolidine scaffold. Key findings include the discovery of an initial lead that was modestly selective...
14.
Lippa B, Pan G, Corbett M, Li C, Kauffman G, Pandit J, et al.
Bioorg Med Chem Lett
. 2008 May;
18(11):3359-63.
PMID: 18456494
Based on a high throughput screening hit, pyrrolopyrimidine inhibitors of the Akt kinase are explored. X-ray co-crystal structures of two lead series results in the understanding of key binding interactions,...
15.
Lippa B, Kauffman G, Arcari J, Kwan T, Chen J, Hungerford W, et al.
Bioorg Med Chem Lett
. 2007 Apr;
17(11):3081-6.
PMID: 17398092
The synthesis and biological evaluation of potent and selective inhibitors of the erbB2 kinase is presented. Based on the 4-anilinoquinazoline chemotype, the syntheses of several new series of erbB2 inhibitors...
16.
Lippa B, Morris J, Corbett M, Kwan T, Noe M, Snow S, et al.
Bioorg Med Chem Lett
. 2006 Apr;
16(13):3444-8.
PMID: 16632359
The design, synthesis, and biological evaluation of potent inhibitors of the TrkA kinase is presented. A homology model is created to aid in the enhancement of potency and selectivity of...
17.
Borzillo G, Lippa B
Curr Top Med Chem
. 2005 Apr;
5(2):147-57.
PMID: 15853643
The Hedgehog (Hh) signaling pathway directs the development of multiple tissues during embryonic development, and contributes to tissue homeostasis in adults. Deficient Hh signaling results in defective embryogenesis; conversely, excessive...
18.
Wender P, Baryza J, Bennett C, Bi F, Brenner S, Clarke M, et al.
J Am Chem Soc
. 2002 Nov;
124(46):13648-9.
PMID: 12431074
Macrocycle 1 is a new highly potent analogue of bryostatin 1, a promising anti-cancer agent currently in human clinical trials. In vitro, 1 displays picomolar affinity for PKC and exhibits...