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Items: 26

1.

Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII).

Koltun DO, Parkhill EQ, Kalla R, Perry TD, Elzein E, Li X, Simonovich SP, Ziebenhaus C, Hansen TR, Marchand B, Hung WK, Lagpacan L, Hung M, Aoyama RG, Murray BP, Perry JK, Somoza JR, Villaseñor AG, Pagratis N, Zablocki JA.

Bioorg Med Chem Lett. 2018 Feb 1;28(3):541-546. doi: 10.1016/j.bmcl.2017.10.040. Epub 2017 Oct 20.

PMID:
29254643
2.

Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.

Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC.

J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3.

PMID:
27690427
3.

Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.

Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Notte GT, Kalla R, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Smith-Maxwell C, Dhalla AK, Rajamani S, Stafford B, Tang J, Mollova N, Belardinelli L, Zablocki JA.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3202-3206. doi: 10.1016/j.bmcl.2016.03.101. Epub 2016 Mar 30.

PMID:
27080178
4.

Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.

Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Hirakawa R, Smith-Maxwell C, Wu L, Dhalla AK, Rajamani S, Mollova N, Stafford B, Tang J, Belardinelli L, Zablocki JA.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3207-3211. doi: 10.1016/j.bmcl.2016.03.096. Epub 2016 Mar 26.

PMID:
27038498
5.

Differing health care visions.

Zablocki JA.

Am J Nurs. 2013 Jan;113(1):13. doi: 10.1097/01.NAJ.0000425731.37989.06. No abstract available.

PMID:
23271229
6.

CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.

Elzein E, Ibrahim P, Koltun DO, Rehder K, Shenk KD, Marquart TA, Jiang B, Li X, Natero R, Li Y, Nguyen M, Kerwar S, Chu N, Soohoo D, Hao J, Maydanik VY, Lustig DA, Zeng D, Leung K, Zablocki JA.

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6017-21.

PMID:
15546720
7.

Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents.

Morrison CF, Elzein E, Jiang B, Ibrahim PN, Marquart T, Palle V, Shenk KD, Varkhedkar V, Maa T, Wu L, Wu Y, Zeng D, Fong I, Lustig D, Leung K, Zablocki JA.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3793-7.

PMID:
15203164
8.
9.

New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological properties.

Koltun DO, Marquart TA, Shenk KD, Elzein E, Li Y, Nguyen M, Kerwar S, Zeng D, Chu N, Soohoo D, Hao J, Maydanik VY, Lustig DA, Ng KJ, Fraser H, Zablocki JA.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):549-52.

PMID:
14698201
10.

Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).

Palle VP, Varkhedkar V, Ibrahim P, Ahmed H, Li Z, Gao Z, Ozeck M, Wu Y, Zeng D, Wu L, Leung K, Chu N, Zablocki JA.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):535-9.

PMID:
14698198
11.

Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.

Palle VP, Elzein EO, Gothe SA, Li Z, Gao Z, Meyer S, Blackburn B, Zablocki JA.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2935-9.

PMID:
12270178
12.

Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists.

Gao Z, Li Z, Baker SP, Lasley RD, Meyer S, Elzein E, Palle V, Zablocki JA, Blackburn B, Belardinelli L.

J Pharmacol Exp Ther. 2001 Jul;298(1):209-18.

PMID:
11408544
13.

A partial agonist of the A(1)-adenosine receptor selectively slows AV conduction in guinea pig hearts.

Wu L, Belardinelli L, Zablocki JA, Palle V, Shryock JC.

Am J Physiol Heart Circ Physiol. 2001 Jan;280(1):H334-43.

14.

Only full support needed.

Zablocki JA.

Can Fam Physician. 1998 Nov;44:2375. No abstract available.

15.

Breastfeeding and mastitis.

Zablocki JA.

Can Fam Physician. 1997 Oct;43:1711, 1713. No abstract available.

16.

The amino-terminal one-third of alpha IIb defines the ligand recognition specificity of integrin alpha IIb beta 3.

Loftus JC, Halloran CE, Ginsberg MH, Feigen LP, Zablocki JA, Smith JW.

J Biol Chem. 1996 Jan 26;271(4):2033-9.

17.

Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.

Zablocki JA, Rico JG, Garland RB, Rogers TE, Williams K, Schretzman LA, Rao SA, Bovy PR, Tjoeng FS, Lindmark RJ, et al.

J Med Chem. 1995 Jun 23;38(13):2378-94.

PMID:
7608903
18.

A novel series of orally active antiplatelet agents.

Zablocki JA, Tjoeng FS, Bovy PR, Miyano M, Garland RB, Williams K, Schretzman L, Zupec ME, Rico JG, Lindmark RJ, et al.

Bioorg Med Chem. 1995 May;3(5):539-51.

PMID:
7648203
19.

SC-54684A: an orally active inhibitor of platelet aggregation.

Nicholson NS, Panzer-Knodle SG, Salyers AK, Taite BB, Szalony JA, Haas NF, King LW, Zablocki JA, Keller BT, Broschat K, et al.

Circulation. 1995 Jan 15;91(2):403-10.

PMID:
7805244
20.

Characterization of Binding of an RGD Mimetic, [(3)H]-SC-52012, to Platelet GPIIb/IIIa.

Panzer-Knodle SG, Jacqmin P, Page JD, Nicholson NS, Zablocki JA, Engleman VW, Feigen LP.

Platelets. 1995;6(5):288-95. doi: 10.3109/09537109509023569.

PMID:
21043715
21.

Design of orally active, non-peptide fibrinogen receptor antagonists. An evolutionary process from the RGD sequence to novel anti-platelet aggregation agents.

Bovy PR, Tjoeng FS, Rico JG, Rogers TE, Lindmark RJ, Zablocki JA, Garland RB, McMackins DE, Dayringer H, Tóth MV, et al.

Bioorg Med Chem. 1994 Sep;2(9):881-95.

PMID:
7712124
22.

Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Arg-guanidine of RGDX mimetics and the platelet GP IIb-IIIa receptor.

Zablocki JA, Miyano M, Garland RB, Pireh D, Schretzman L, Rao SN, Lindmark RJ, Panzer-Knodle SG, Nicholson NS, Taite BB, et al.

J Med Chem. 1993 Jun 25;36(13):1811-9.

PMID:
8515420
23.
24.

Ketononestrol aziridine, an agonistic estrogen receptor affinity label: study of its bioactivity and estrogen receptor covalent labeling.

Elliston JF, Zablocki JA, Katzenellenbogen BS, Katzenellenbogen JA.

Endocrinology. 1987 Aug;121(2):667-76.

PMID:
3595536
25.

Estrogenic affinity labels: synthesis, irreversible receptor binding, and bioactivity of aziridine-substituted hexestrol derivatives.

Zablocki JA, Katzenellenbogen JA, Carlson KE, Norman MJ, Katzenellenbogen BS.

J Med Chem. 1987 May;30(5):829-38.

PMID:
3033242

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