Dave Lugo
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Explore the profile of Dave Lugo including associated specialties, affiliations and a list of published articles.
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10
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1423
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Recent Articles
1.
Shah V, Giotopoulos G, Osaki H, Meyerhofer M, Meduri E, Gallego-Crespo A, et al.
Blood
. 2024 Dec;
145(7):748-764.
PMID: 39651888
Initial clinical trials with drugs targeting epigenetic modulators, such as bromodomain and extraterminal protein (BET) inhibitors, demonstrate modest results in acute myeloid leukemia (AML). A major reason for this involves...
2.
Wellaway C, Amans D, Bamborough P, Barnett H, Bit R, Brown J, et al.
J Med Chem
. 2020 Jan;
63(2):714-746.
PMID: 31904959
The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize -acetyl lysine (KAc) post-translational modifications on histone tails. These interactions...
3.
Tyler D, Vappiani J, Caneque T, Lam E, Ward A, Gilan O, et al.
Science
. 2017 Jun;
356(6345):1397-1401.
PMID: 28619718
The success of new therapies hinges on our ability to understand their molecular and cellular mechanisms of action. We modified BET bromodomain inhibitors, an epigenetic-based therapy, to create functionally conserved...
4.
Garton N, Barker M, Davis R, Douault C, Hooper-Greenhill E, Jones E, et al.
Bioorg Med Chem Lett
. 2016 Sep;
26(19):4606-4612.
PMID: 27578246
The optimisation of the azanaphthyridine series of Spleen Tyrosine Kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient...
5.
Gilan O, Lam E, Becher I, Lugo D, Cannizzaro E, Joberty G, et al.
Nat Struct Mol Biol
. 2016 Jun;
23(7):673-81.
PMID: 27294782
Targeted therapies against disruptor of telomeric silencing 1-like (DOT1L) and bromodomain-containing protein 4 (BRD4) are currently being evaluated in clinical trials. However, the mechanisms by which BRD4 and DOT1L regulate...
6.
Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, et al.
Cancer Res
. 2015 Nov;
75(23):5106-5119.
PMID: 26552700
The histone acetyltransferases CBP/p300 are involved in recurrent leukemia-associated chromosomal translocations and are key regulators of cell growth. Therefore, efforts to generate inhibitors of CBP/p300 are of clinical value. We...
7.
Fong C, Gilan O, Lam E, Rubin A, Ftouni S, Tyler D, et al.
Nature
. 2015 Sep;
525(7570):538-42.
PMID: 26367796
Bromodomain and extra terminal protein (BET) inhibitors are first-in-class targeted therapies that deliver a new therapeutic opportunity by directly targeting bromodomain proteins that bind acetylated chromatin marks. Early clinical trials...
8.
Alsarraj J, Faraji F, Geiger T, Mattaini K, Williams M, Wu J, et al.
PLoS One
. 2013 Nov;
8(11):e80746.
PMID: 24260471
Recent studies suggest that BET inhibitors are effective anti-cancer therapeutics. Here we show that BET inhibitors are effective against murine primary mammary tumors, but not pulmonary metastases. BRD4, a target...
9.
van Bree S, Gomez-Pinilla P, van de Bovenkamp F, Di Giovangiulio M, Farro G, Nemethova A, et al.
Gut
. 2012 Dec;
62(11):1581-90.
PMID: 23242119
Objective: Intestinal inflammation resulting from manipulation-induced mast cell activation is a crucial mechanism in the pathophysiology of postoperative ileus (POI). Recently it has been shown that spleen tyrosine kinase (Syk)...
10.
Dawson M, Prinjha R, Dittmann A, Giotopoulos G, Bantscheff M, Chan W, et al.
Nature
. 2011 Oct;
478(7370):529-33.
PMID: 21964340
Recurrent chromosomal translocations involving the mixed lineage leukaemia (MLL) gene initiate aggressive forms of leukaemia, which are often refractory to conventional therapies. Many MLL-fusion partners are members of the super...