Hussein Hallak
Parke-Davis
23 Papers
339 Citations
Hussein Hallak is an academic researcher from Parke-Davis. The author has contributed to research in topics: Endothelin receptor & Medicine. The author has an hindex of 13, co-authored 20 publications.
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Papers
Matrix Metalloproteinase Inhibition Attenuates Left Ventricular Remodeling and Dysfunction in a Rat Model of Progressive Heart Failure
J. Thomas Peterson,Hussein Hallak,Linda S B Johnson,Hua Li,Patrick Michael O'brien,Drago Robert Sliskovic,Thomas M.A. Bocan,Mytsi L. Coker,Takuma Etoh,Francis G. Spinale +9 more
TL;DR: MMP activity contributes to LV dilation and progression to LV dysfunction in a rodent HF model, and direct MMP inhibition can attenuate this process.
332
Synthesis and Tyrosine Kinase Inhibitory Activity of a Series of 2-Amino-8H-pyrido[2,3-d]pyrimidines: Identification of Potent, Selective Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors
Diane H. Boschelli,Zhipei Wu,Sylvester Klutchko,H. D. Hollis Showalter,James Marino Hamby,Gina H. Lu,T C Major,Tawny K. Dahring,Brian L. Batley,Robert L. Panek,Joan A. Keiser,Brian G. Hartl,Alan J. Kraker,Wayne D. Klohs,Bill J. Roberts,Sandra J. Patmore,William L. Elliott,Randy Steinkampf,Laura A. Bradford,Hussein Hallak,Annette Marian Doherty +20 more
TL;DR: Variation of the aromatic group at C-6 and of the alkyl group at N-8 of the pyrido[2,3-d]pyrimidine core provided several analogues that retained potency, including derivatives that were biased toward inhibition of the TK activity of PDGFr.
140
•Journal Article
In Vitro Pharmacological Characterization of PD 166285, a New Nanomolar Potent and Broadly Active Protein Tyrosine Kinase Inhibitor
Robert L. Panek,Gina H. Lu,Sylvester Klutchko,Brian L. Batley,Tawny K. Dahring,James Marino Hamby,Hussein Hallak,Annette Marian Doherty,Joan A. Keiser +8 more
TL;DR: The potential therapeutic utility of this broadly acting inhibitor as an antiproliferative and antimigratory agent could extend to such diseases as cancer, atherosclerosis and restenosis, in which redundancies in protein kinase signaling pathways are known to exist.
126
Structure−Activity Relationships and Pharmacokinetic Analysis for a Series of Potent, Systemically Available Biphenylsulfonamide Matrix Metalloproteinase Inhibitors
Patrick Michael O'brien,Daniel F. Ortwine,Alexander Pavlovsky,Joseph Armand Picard,Drago Robert Sliskovic,Bruce D. Roth,Richard D. Dyer,Johnson Linda Lea,Chiu Fai Man,Hussein Hallak +9 more
TL;DR: Varying the lipophilicity of the alpha-position by replacing the isopropyl group of 11c with a variety of substituents, in general, maintained potency versus MMP-2, -3, and -13 but decreased the oral systemic availability, and 16a' afforded very low plasma concentrations following a single 5 mg/kg oral dose in rat.
104
Endothelin receptor antagonist increases cerebral perfusion and reduces ischaemic damage in feline focal cerebral ischaemia
Toshal R. Patel,Samuel Galbraith,David I. Graham,Hussein Hallak,Annette Marian Doherty,James McCulloch +5 more
TL;DR: The investigations indicate that endothelin receptor antagonism may be a new therapeutic strategy for the amelioration of focal ischaemic damage.
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