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Response and determinants of cancer cell susceptibility to PI3K inhibitors: combined targeting of PI3K and Mek1 as an effective anticancer strategy.
Yu K, Toral-Barza L, Shi C, Zhang WG, Zask A. Yu K, et al. Among authors: zask a. Cancer Biol Ther. 2008 Feb;7(2):307-15. doi: 10.4161/cbt.7.2.5334. Epub 2007 Nov 21. Cancer Biol Ther. 2008. PMID: 18059185
In this report, we have studied anti-proliferative effects of the PI3K inhibitors WAY-266176 and WAY-266175 in a panel of histologically diverse cancer cells. ...A heightened PI3K/AKT/mTOR signaling was linked to the sensitive phenotype but did not generally predict …
In this report, we have studied anti-proliferative effects of the PI3K inhibitors WAY-266176 and WAY-266175 in a panel of histologica …
Molecular regulation of apoptotic machinery and lipid metabolism by mTORC1/mTORC2 dual inhibitors in preclinical models of HER2+/PIK3CAmut breast cancer.
Qian J, Chen Y, Meng T, Ma L, Meng L, Wang X, Yu T, Zask A, Shen J, Yu K. Qian J, et al. Among authors: zask a. Oncotarget. 2016 Oct 11;7(41):67071-67086. doi: 10.18632/oncotarget.11490. Oncotarget. 2016. PMID: 27563814 Free PMC article.
Hybrids of the hemiasterlin analogue taltobulin and the dolastatins are potent antimicrotubule agents.
Zask A, Kaplan J, Musto S, Loganzo F. Zask A, et al. J Am Chem Soc. 2005 Dec 21;127(50):17667-71. doi: 10.1021/ja053663v. J Am Chem Soc. 2005. PMID: 16351096
However, there is still a need for improved antimicrotubule agents. A number of seemingly structurally disparate peptidic natural products inhibit tubulin polymerization by binding to a region of the tubulin heterodimer close to the vinca binding site. ...The …
However, there is still a need for improved antimicrotubule agents. A number of seemingly structurally disparate peptidic natu …
PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors.
Yu K, Lucas J, Zhu T, Zask A, Gaydos C, Toral-Barza L, Gu J, Li F, Chaudhary I, Cai P, Lotvin J, Petersen R, Ruppen M, Fawzi M, Ayral-Kaloustian S, Skotnicki J, Mansour T, Frost P, Gibbons J. Yu K, et al. Among authors: zask a. Cancer Biol Ther. 2005 May;4(5):538-45. doi: 10.4161/cbt.4.5.1660. Epub 2005 May 28. Cancer Biol Ther. 2005. PMID: 15846106
While a strong rationale exists for pharmacological targeting of PI3K, only a few proof-of-principle in vivo efficacy studies are currently available. ...Finally, PWT-458 in combination with interferon-alpha (Intron-A) caused a dramatic regression of R …
While a strong rationale exists for pharmacological targeting of PI3K, only a few proof-of-principle in vivo efficacy studies …
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.
Venkatesan AM, Davis JM, Grosu GT, Baker J, Zask A, Levin JI, Ellingboe J, Skotnicki JS, Dijoseph JF, Sung A, Jin G, Xu W, McCarthy DJ, Barone D. Venkatesan AM, et al. Among authors: zask a. J Med Chem. 2004 Dec 2;47(25):6255-69. doi: 10.1021/jm040086x. J Med Chem. 2004. PMID: 15566296
A series of 4-alkynyloxy phenyl sulfanyl, sulfinyl and sulfony alkyl and piperidine-4-carboxylic acid hydroxamides were synthesized. ...The sulfonyl derivatives 20-24 carrying a 4-butynyloxy moiety were selective TACE inhibitors over the MMPs tested. The sulfinyl de
A series of 4-alkynyloxy phenyl sulfanyl, sulfinyl and sulfony alkyl and piperidine-4-carboxylic acid hydroxamides were synthesized.
Cells resistant to HTI-286 do not overexpress P-glycoprotein but have reduced drug accumulation and a point mutation in alpha-tubulin.
Loganzo F, Hari M, Annable T, Tan X, Morilla DB, Musto S, Zask A, Kaplan J, Minnick AA Jr, May MK, Ayral-Kaloustian S, Poruchynsky MS, Fojo T, Greenberger LM. Loganzo F, et al. Among authors: zask a. Mol Cancer Ther. 2004 Oct;3(10):1319-27. Mol Cancer Ther. 2004. PMID: 15486199
HTI-286, a synthetic analogue of hemiasterlin, depolymerizes microtubules and is proposed to bind at the Vinca peptide site in tubulin. ...However, 4.0 nmol/L HTI-286-selected cells had a point mutation in alpha-tubulin that substitutes Ser for Ala(12) near the none …
HTI-286, a synthetic analogue of hemiasterlin, depolymerizes microtubules and is proposed to bind at the Vinca peptide site in tubuli …
Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: modification of the A segment.
Yamashita A, Norton EB, Kaplan JA, Niu C, Loganzo F, Hernandez R, Beyer CF, Annable T, Musto S, Discafani C, Zask A, Ayral-Kaloustian S. Yamashita A, et al. Among authors: zask a. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5317-22. doi: 10.1016/j.bmcl.2004.08.024. Bioorg Med Chem Lett. 2004. PMID: 15454219
The structure-activity relationships related to stereo- and regio-chemical effects of substituents on the aromatic ring in the A segment were studied. Analogs, which carry a meta-substituted phenyl ring in the A segment show comparable activity for inhibition …
The structure-activity relationships related to stereo- and regio-chemical effects of substituents on the aromatic ring in the A segm …
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).
Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Suayan R, Yamashita A, Cole D, Tang Z, Krishnamurthy G, Williamson R, Khafizova G, Musto S, Hernandez R, Annable T, Yang X, Discafani C, Beyer C, Greenberger LM, Loganzo F, Ayral-Kaloustian S. Zask A, et al. J Med Chem. 2004 Sep 9;47(19):4774-86. doi: 10.1021/jm040056u. J Med Chem. 2004. PMID: 15341492
Hemiasterlin, a tripeptide isolated from marine sponges, induces microtubule depolymerization and mitotic arrest in cells. HTI-286, an analogue from an initial study of the hemiasterlins, is presently in clinical trials. ...
Hemiasterlin, a tripeptide isolated from marine sponges, induces microtubule depolymerization and mitotic arrest in cells. HTI-286, a …
D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors.
Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Yamashita A, Beyer C, Krishnamurthy G, Greenberger LM, Loganzo F, Ayral-Kaloustian S. Zask A, et al. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4353-8. doi: 10.1016/j.bmcl.2004.05.005. Bioorg Med Chem Lett. 2004. PMID: 15261301
Synthetic modifications of the carboxylic acid could be carried out selectively using a wide range of synthetic reagents. Proline analog 3 was found to be effective in a human xenograft model in athymic mice....
Synthetic modifications of the carboxylic acid could be carried out selectively using a wide range of synthetic reagents. Proline ana …
HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
Loganzo F, Discafani CM, Annable T, Beyer C, Musto S, Hari M, Tan X, Hardy C, Hernandez R, Baxter M, Singanallore T, Khafizova G, Poruchynsky MS, Fojo T, Nieman JA, Ayral-Kaloustian S, Zask A, Andersen RJ, Greenberger LM. Loganzo F, et al. Among authors: zask a. Cancer Res. 2003 Apr 15;63(8):1838-45. Cancer Res. 2003. PMID: 12702571
Hemiasterlin is a natural product derived from marine sponges that, like other structurally diverse peptide-like molecules, binds to the Vinca-peptide site in tubulin, disrupts normal microtubule dynamics, and, at stoichiometric amounts, depolymerizes microtubules. ...Thes …
Hemiasterlin is a natural product derived from marine sponges that, like other structurally diverse peptide-like molecules, binds to …
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