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Items: 1 to 50 of 129

1.

Identification and Optimization of Novel Small c-Abl Kinase Activators Using Fragment and HTS Methodologies.

Simpson GL, Bertrand SM, Borthwick JA, Campobasso N, Chabanet J, Chen S, Coggins J, Cottom J, Christensen SB, Dawson HC, Evans HL, Hobbs AN, Hong X, Mangatt B, Munoz-Muriedas J, Oliff A, Qin D, Scott-Stevens P, Ward P, Washio Y, Yang J, Young RJ.

J Med Chem. 2019 Feb 28;62(4):2154-2171. doi: 10.1021/acs.jmedchem.8b01872. Epub 2019 Feb 11.

PMID:
30689376
2.

Exploring the Potential of RET Kinase Inhibition for Irritable Bowel Syndrome: A Preclinical Investigation in Rodent Models of Colonic Hypersensitivity.

Russell JP, Mohammadi E, Ligon CO, Johnson AC, Gershon MD, Rao M, Shen Y, Chan CC, Eidam HS, DeMartino MP, Cheung M, Oliff AI, Kumar S, Greenwood-Van Meerveld B.

J Pharmacol Exp Ther. 2019 Feb;368(2):299-307. doi: 10.1124/jpet.118.252973. Epub 2018 Nov 9.

PMID:
30413627
3.

Enteric RET inhibition attenuates gastrointestinal secretion and motility via cholinergic signaling in rat colonic mucosal preparations.

Russell JP, Mohammadi E, Ligon C, Latorre R, Johnson AC, Hoang B, Krull D, Ho MW, Eidam HS, DeMartino MP, Cheung M, Oliff AI, Kumar S, Greenwood-Van Meerveld B.

Neurogastroenterol Motil. 2019 Apr;31(4):e13479. doi: 10.1111/nmo.13479. Epub 2018 Oct 12.

PMID:
30311722
4.

Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS.

Schenck Eidam H, Russell J, Raha K, DeMartino M, Qin D, Guan HA, Zhang Z, Zhen G, Yu H, Wu C, Pan Y, Joberty G, Zinn N, Laquerre S, Robinson S, White A, Giddings A, Mohammadi E, Greenwood-Van Meerveld B, Oliff A, Kumar S, Cheung M.

ACS Med Chem Lett. 2018 May 24;9(7):623-628. doi: 10.1021/acsmedchemlett.8b00035. eCollection 2018 Jul 12.

5.

TLR2 agonism reverses chemotherapy-induced neutropenia in Macaca fascicularis.

Laping NJ, DeMartino MP, Cottom JE, Axten JM, Emery JG, Guss JH, Burman M, Foley JJ, Cheung M, Oliff A, Kumar S.

Blood Adv. 2017 Dec 8;1(26):2553-2562. doi: 10.1182/bloodadvances.2017010611. eCollection 2017 Dec 12.

6.

Osteopathic Approach to the Diagnosis of Appendiceal Mucinous Cystadenocarcinoma Mimicking Primary Ovarian Malignant Neoplasm.

Martingano D, Gurm H, Oliff A, Martingano FX, Aglialoro G.

J Am Osteopath Assoc. 2016 Jul 1;116(7):480-4. doi: 10.7556/jaoa.2016.092.

PMID:
27367953
7.

Spinal Schwannoma presenting due to torsion and hemorrhage: case report and review of literature.

Jenkins AL 3rd, Ahuja A, Oliff AH, Sobotka S.

Spine J. 2015 Aug 1;15(8):e1-4. doi: 10.1016/j.spinee.2015.04.046. Epub 2015 May 6. Review.

PMID:
25957540
8.

Composite angioimmunoblastic T-cell and diffuse large B-cell lymphoma.

Alperovich A, Vlachostergios PJ, Binder A, Oliff AH, Balmiki RL, Dufresne F.

Hematol Oncol Stem Cell Ther. 2015 Sep;8(3):136-7. doi: 10.1016/j.hemonc.2015.04.006. Epub 2015 Apr 28. No abstract available.

9.

Gastric malakoplakia.

Ding X, Oliff A, Rando J, Harpaz N.

Gastrointest Endosc. 2014 Nov;80(5):903-4. doi: 10.1016/j.gie.2014.08.015. Epub 2014 Oct 15. No abstract available.

PMID:
25436401
10.

Development of a high-throughput screen to detect inhibitors of TRPS1 sumoylation.

Brandt M, Szewczuk LM, Zhang H, Hong X, McCormick PM, Lewis TS, Graham TI, Hung ST, Harper-Jones AD, Kerrigan JJ, Wang DY, Dul E, Hou W, Ho TF, Meek TD, Cheung MH, Johanson KO, Jones CS, Schwartz B, Kumar S, Oliff AI, Kirkpatrick RB.

Assay Drug Dev Technol. 2013 Jun;11(5):308-25. doi: 10.1089/adt.2012.501.

PMID:
23772552
11.

Secondary vascular alterations in diffuse and plexiform neurofibroma: an impressive yet little known morphologic change.

Pirola S, Oliff A.

Int J Surg Pathol. 2014 Feb;22(1):63-5. doi: 10.1177/1066896912436556. Epub 2012 Feb 15. No abstract available.

PMID:
22344173
12.

Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site.

Yang J, Campobasso N, Biju MP, Fisher K, Pan XQ, Cottom J, Galbraith S, Ho T, Zhang H, Hong X, Ward P, Hofmann G, Siegfried B, Zappacosta F, Washio Y, Cao P, Qu J, Bertrand S, Wang DY, Head MS, Li H, Moores S, Lai Z, Johanson K, Burton G, Erickson-Miller C, Simpson G, Tummino P, Copeland RA, Oliff A.

Chem Biol. 2011 Feb 25;18(2):177-86. doi: 10.1016/j.chembiol.2010.12.013.

13.

Synchronous renal malignancy presenting as recurrent urinary tract infections.

Dutta G, Silver D, Oliff A, Harrison A.

Case Rep Urol. 2011;2011:832673. doi: 10.1155/2011/832673. Epub 2011 Sep 18.

14.

Matrix metalloproteinase-activated doxorubicin prodrugs inhibit HT1080 xenograft growth better than doxorubicin with less toxicity.

Albright CF, Graciani N, Han W, Yue E, Stein R, Lai Z, Diamond M, Dowling R, Grimminger L, Zhang SY, Behrens D, Musselman A, Bruckner R, Zhang M, Jiang X, Hu D, Higley A, Dimeo S, Rafalski M, Mandlekar S, Car B, Yeleswaram S, Stern A, Copeland RA, Combs A, Seitz SP, Trainor GL, Taub R, Huang P, Oliff A.

Mol Cancer Ther. 2005 May;4(5):751-60.

15.

Farnesyl:protein transferase inhibitors as potential agents for the management of human prostate cancer.

Sepp-Lorenzino L, Tjaden G, Moasser MM, Timaul N, Ma Z, Kohl NE, Gibbs JB, Oliff A, Rosen N, Scher HI.

Prostate Cancer Prostatic Dis. 2001;4(1):33-43.

16.

A prostate-specific antigen (PSA)-activated vinblastine prodrug selectively kills PSA-secreting cells in vivo.

DeFeo-Jones D, Brady SF, Feng DM, Wong BK, Bolyar T, Haskell K, Kiefer DM, Leander K, McAvoy E, Lumma P, Pawluczyk JM, Wai J, Motzel SL, Keenan K, Van Zwieten M, Lin JH, Garsky VM, Freidinger R, Oliff A, Jones RE.

Mol Cancer Ther. 2002 May;1(7):451-9.

17.

Design and synthesis of a pro-drug of vinblastine targeted at treatment of prostate cancer with enhanced efficacy and reduced systemic toxicity.

Brady SF, Pawluczyk JM, Lumma PK, Feng DM, Wai JM, Jones R, DeFeo-Jones D, Wong BK, Miller-Stein C, Lin JH, Oliff A, Freidinger RM, Garsky VM.

J Med Chem. 2002 Oct 10;45(21):4706-15.

PMID:
12361397
18.

Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.

Lobell RB, Omer CA, Abrams MT, Bhimnathwala HG, Brucker MJ, Buser CA, Davide JP, deSolms SJ, Dinsmore CJ, Ellis-Hutchings MS, Kral AM, Liu D, Lumma WC, Machotka SV, Rands E, Williams TM, Graham SL, Hartman GD, Oliff AI, Heimbrook DC, Kohl NE.

Cancer Res. 2001 Dec 15;61(24):8758-68.

19.

The synthesis of a prodrug of doxorubicin designed to provide reduced systemic toxicity and greater target efficacy.

Garsky VM, Lumma PK, Feng DM, Wai J, Ramjit HG, Sardana MK, Oliff A, Jones RE, DeFeo-Jones D, Freidinger RM.

J Med Chem. 2001 Nov 22;44(24):4216-24.

PMID:
11708923
20.

Signaling pathways in apoptosis as potential targets for cancer therapy.

Huang P, Oliff A.

Trends Cell Biol. 2001 Aug;11(8):343-8. Review.

PMID:
11489640
21.

PSA-specific and non-PSA-specific conversion of a PSA-targeted peptide conjugate of doxorubicin to its active metabolites.

Wong BK, DeFeo-Jones D, Jones RE, Garsky VM, Feng DM, Oliff A, Chiba M, Ellis JD, Lin JH.

Drug Metab Dispos. 2001 Mar;29(3):313-8.

PMID:
11181501
22.

Farnesyltransferase inhibitors: antineoplastic properties, mechanisms of action, and clinical prospects.

Prendergast GC, Oliff A.

Semin Cancer Biol. 2000 Dec;10(6):443-52. Review.

PMID:
11170866
23.

Drug-targeting strategies in cancer therapy.

Huang PS, Oliff A.

Curr Opin Genet Dev. 2001 Feb;11(1):104-10. Review.

PMID:
11163159
24.

A peptide-doxorubicin 'prodrug' activated by prostate-specific antigen selectively kills prostate tumor cells positive for prostate-specific antigen in vivo.

DeFeo-Jones D, Garsky VM, Wong BK, Feng DM, Bolyar T, Haskell K, Kiefer DM, Leander K, McAvoy E, Lumma P, Wai J, Senderak ET, Motzel SL, Keenan K, Van Zwieten M, Lin JH, Freidinger R, Huff J, Oliff A, Jones RE.

Nat Med. 2000 Nov;6(11):1248-52.

PMID:
11062536
25.

Farnesyltransferase inhibitors potentiate the antitumor effect of radiation on a human tumor xenograft expressing activated HRAS.

Cohen-Jonathan E, Muschel RJ, Gillies McKenna W, Evans SM, Cerniglia G, Mick R, Kusewitt D, Sebti SM, Hamilton AD, Oliff A, Kohl N, Gibbs JB, Bernhard EJ.

Radiat Res. 2000 Aug;154(2):125-32.

PMID:
10931682
26.

Mouse mammary tumor virus-Ki-rasB transgenic mice develop mammary carcinomas that can be growth-inhibited by a farnesyl:protein transferase inhibitor.

Omer CA, Chen Z, Diehl RE, Conner MW, Chen HY, Trumbauer ME, Gopal-Truter S, Seeburger G, Bhimnathwala H, Abrams MT, Davide JP, Ellis MS, Gibbs JB, Greenberg I, Koblan KS, Kral AM, Liu D, Lobell RB, Miller PJ, Mosser SD, O'Neill TJ, Rands E, Schaber MD, Senderak ET, Oliff A, Kohl NE.

Cancer Res. 2000 May 15;60(10):2680-8.

27.

Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.

Dinsmore CJ, Williams TM, O'Neill TJ, Liu D, Rands E, Culberson JC, Lobell RB, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD.

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3301-6.

PMID:
10612589
28.

Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.

Anthony NJ, Gomez RP, Schaber MD, Mosser SD, Hamilton KA, O'Neil TJ, Koblan KS, Graham SL, Hartman GD, Shah D, Rands E, Kohl NE, Gibbs JB, Oliff AI.

J Med Chem. 1999 Aug 26;42(17):3356-68.

PMID:
10464022
29.

Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.

Ciccarone TM, MacTough SC, Williams TM, Dinsmore CJ, O'Neill TJ, Shah D, Culberson JC, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD.

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1991-6.

PMID:
10450968
30.

Farnesyltransferase inhibitors: targeting the molecular basis of cancer.

Oliff A.

Biochim Biophys Acta. 1999 May 31;1423(3):C19-30. Review. No abstract available.

PMID:
10382537
31.

Treatment with farnesyl-protein transferase inhibitor induces regression of mammary tumors in transforming growth factor (TGF) alpha and TGF alpha/neu transgenic mice by inhibition of mitogenic activity and induction of apoptosis.

Nørgaard P, Law B, Joseph H, Page DL, Shyr Y, Mays D, Pietenpol JA, Kohl NE, Oliff A, Coffey RJ Jr, Poulsen HS, Moses HL.

Clin Cancer Res. 1999 Jan;5(1):35-42.

32.

Biochemical and biological analyses of farnesyl-protein transferase inhibitors.

Kohl NE, Koblan KS, Omer CA, Oliff A, Gibbs JB.

Methods Mol Biol. 1998;84:283-91.

PMID:
9666457
33.

N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase.

deSolms SJ, Giuliani EA, Graham SL, Koblan KS, Kohl NE, Mosser SD, Oliff AI, Pompliano DL, Rands E, Scholz TH, Wiscount CM, Gibbs JB, Smith RL.

J Med Chem. 1998 Jul 2;41(14):2651-6.

PMID:
9651171
34.

Therapeutic intervention and signaling.

Heimbrook DC, Oliff A.

Curr Opin Cell Biol. 1998 Apr;10(2):284-8. Review.

PMID:
9561854
35.

Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.

Mangues R, Corral T, Kohl NE, Symmans WF, Lu S, Malumbres M, Gibbs JB, Oliff A, Pellicer A.

Cancer Res. 1998 Mar 15;58(6):1253-9.

36.

Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones.

Moasser MM, Sepp-Lorenzino L, Kohl NE, Oliff A, Balog A, Su DS, Danishefsky SJ, Rosen N.

Proc Natl Acad Sci U S A. 1998 Feb 17;95(4):1369-74.

37.

Emerging uses for genomic information in drug discovery.

Friend SH, Oliff A.

N Engl J Med. 1998 Jan 8;338(2):125-6. No abstract available.

PMID:
9420347
38.

A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis.

Barrington RE, Subler MA, Rands E, Omer CA, Miller PJ, Hundley JE, Koester SK, Troyer DA, Bearss DJ, Conner MW, Gibbs JB, Hamilton K, Koblan KS, Mosser SD, O'Neill TJ, Schaber MD, Senderak ET, Windle JJ, Oliff A, Kohl NE.

Mol Cell Biol. 1998 Jan;18(1):85-92.

39.

Farnesyltransferase inhibitors versus Ras inhibitors.

Gibbs JB, Graham SL, Hartman GD, Koblan KS, Kohl NE, Omer CA, Oliff A.

Curr Opin Chem Biol. 1997 Aug;1(2):197-203. Review.

PMID:
9667853
40.

Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth.

Omer CA, Anthony NJ, Buser-Doepner CA, Burkhardt AL, deSolms SJ, Dinsmore CJ, Gibbs JB, Hartman GD, Koblan KS, Lobell RB, Oliff A, Williams TM, Kohl NE.

Biofactors. 1997;6(3):359-66. Review.

PMID:
9288406
41.

The potential of farnesyltransferase inhibitors as cancer chemotherapeutics.

Gibbs JB, Oliff A.

Annu Rev Pharmacol Toxicol. 1997;37:143-66. Review.

PMID:
9131250
42.

Cloning and mutagenesis of the p110 alpha subunit of human phosphoinositide 3'-hydroxykinase.

Stirdivant SM, Ahern J, Conroy RR, Barnett SF, Ledder LM, Oliff A, Heimbrook DC.

Bioorg Med Chem. 1997 Jan;5(1):65-74.

PMID:
9043658
43.

Selection of potent inhibitors of farnesyl-protein transferase from a synthetic tetrapeptide combinatorial library.

Wallace A, Koblan KS, Hamilton K, Marquis-Omer DJ, Miller PJ, Mosser SD, Omer CA, Schaber MD, Cortese R, Oliff A, Gibbs JB, Pessi A.

J Biol Chem. 1996 Dec 6;271(49):31306-11.

44.

New molecular targets for cancer therapy.

Oliff A, Gibbs JB, McCormick F.

Sci Am. 1996 Sep;275(3):144-9. Review. No abstract available.

PMID:
8701284
45.

Farnesyltransferase inhibitors: a new class of cancer chemotherapeutics.

Koblan KS, Kohl NE, Omer CA, Anthony NJ, Conner MW, deSolms SJ, Williams TM, Graham SL, Hartman GD, Oliff A, Gibbs JB.

Biochem Soc Trans. 1996 Aug;24(3):688-92. Review. No abstract available.

PMID:
8878827
46.

2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.

Williams TM, Ciccarone TM, MacTough SC, Bock RL, Conner MW, Davide JP, Hamilton K, Koblan KS, Kohl NE, Kral AM, Mosser SD, Omer CA, Pompliano DL, Rands E, Schaber MD, Shah D, Wilson FR, Gibbs JB, Graham SL, Hartman GD, Oliff AI, Smith RL.

J Med Chem. 1996 Mar 29;39(7):1345-8. No abstract available.

PMID:
8691462
47.

Farnesyltransferase inhibitors and anti-Ras therapy.

Gibbs JB, Kohl NE, Koblan KS, Omer CA, Sepp-Lorenzino L, Rosen N, Anthony NJ, Conner MW, deSolms SJ, Williams TM, Graham SL, Hartman GD, Oliff A.

Breast Cancer Res Treat. 1996;38(1):75-83. Review.

PMID:
8825125
48.

A peptidomimetic inhibitor of farnesyl:protein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines.

Sepp-Lorenzino L, Ma Z, Rands E, Kohl NE, Gibbs JB, Oliff A, Rosen N.

Cancer Res. 1995 Nov 15;55(22):5302-9.

49.

Pseudodipeptide inhibitors of protein farnesyltransferase.

deSolms SJ, Deana AA, Giuliani EA, Graham SL, Kohl NE, Mosser SD, Oliff AI, Pompliano DL, Rands E, Scholz TH, et al.

J Med Chem. 1995 Sep 29;38(20):3967-71.

PMID:
7562930
50.

An SH3 domain is required for the mitogenic activity of microinjected phospholipase C-gamma 1.

Huang PS, Davis L, Huber H, Goodhart PJ, Wegrzyn RE, Oliff A, Heimbrook DC.

FEBS Lett. 1995 Jan 30;358(3):287-92.

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