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Stefan Hart

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Articles 21
Citations 837
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Recent Articles
1.
Mustafa N, Lee J, Adina Nee H, Bi C, Chung T, Hart S, et al.
Oncotarget . 2017 Dec; 8(60):101847-101864. PMID: 29254208
The PI3K/mTOR/AKT pathway is an integral regulator of survival and drug resistance in multiple myeloma (MM). VS-5584 was synthesized with dual-specific and equipotent activity against mTORC1/2 and all four Class...
2.
Bessho H, Wong B, Huang D, Tan J, Ong C, Iwamura M, et al.
Cancer Invest . 2015 Jun; 33(8):378-86. PMID: 26115098
The blockade of VEGF pathway has been clinically validated as an initial treatment for renal cell carcinoma (RCC). Angiopoietin-2 (Ang-2) has been indicated as a key regulator for angiogenesis escape....
3.
Poulsen A, Nagaraj H, Lee A, Blanchard S, Soh C, Chen D, et al.
J Chem Inf Model . 2014 Oct; 54(11):3238-50. PMID: 25317974
Phosphoinositide 3-kinases (PI3Ks) and the mammalian target of rapamycin (mTOR) act as critical effectors in a commonly deregulated cell signaling pathway in human cancers. The abnormal activation of the PI3K/mTOR...
4.
Ananthanarayanan A, Nugraha B, Triyatni M, Hart S, Sankuratri S, Yu H
Mol Pharm . 2014 Apr; 11(7):2106-14. PMID: 24761996
Developing effective new drugs against hepatitis C (HCV) virus has been challenging due to the lack of appropriate small animal and in vitro models recapitulating the entire life cycle of...
5.
Tan A, Hoang L, Chin D, Rasmussen E, Lopatin U, Hart S, et al.
J Hepatol . 2013 Sep; 60(1):54-61. PMID: 23994382
Background & Aims: The interaction between HBV replication and immune modulatory effects mediated by IFNα therapy is not well understood. We characterized the impact of HBV DNA replication on the...
6.
Hart S, Novotny-Diermayr V, Goh K, Williams M, Tan Y, Ong L, et al.
Mol Cancer Ther . 2012 Dec; 12(2):151-61. PMID: 23270925
Dysregulation of the PI3K/mTOR pathway, either through amplifications, deletions, or as a direct result of mutations, has been closely linked to the development and progression of a wide range of...
7.
Younes A, Romaguera J, Fanale M, McLaughlin P, Hagemeister F, Copeland A, et al.
J Clin Oncol . 2012 Sep; 30(33):4161-7. PMID: 22965964
Purpose: The Janus kinase 2/signal transducers and activators of transcription (JAK2/STAT) pathway plays an important role in the pathogenesis of hematologic malignancies. We conducted a phase I dose-finding and pharmacokinetic/pharmacodynamic...
8.
Madan B, Goh K, Hart S, William A, Jayaraman R, Ethirajulu K, et al.
J Immunol . 2012 Sep; 189(8):4123-34. PMID: 22962687
SB1578 is a novel, orally bioavailable JAK2 inhibitor with specificity for JAK2 within the JAK family and also potent activity against FLT3 and c-Fms. These three tyrosine kinases play a...
9.
William A, Lee A, Poulsen A, Goh K, Madan B, Hart S, et al.
J Med Chem . 2012 Feb; 55(6):2623-40. PMID: 22339472
Herein, we describe the synthesis and SAR of a series of small molecule macrocycles that selectively inhibit JAK2 kinase within the JAK family and FLT3 kinase. Following a multiparameter optimization...
10.
William A, Lee A, Blanchard S, Poulsen A, Teo E, Nagaraj H, et al.
J Med Chem . 2011 May; 54(13):4638-58. PMID: 21604762
Discovery of the activating mutation V617F in Janus Kinase 2 (JAK2(V617F)), a tyrosine kinase critically involved in receptor signaling, recently ignited interest in JAK2 inhibitor therapy as a treatment for...