Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 24

1.

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.

Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S, Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM, Edwards MP, Ferre RA, Gajiwala KS, Hemkens M, Kania RS, Kath JC, Matthews J, Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin S, Zhang C, Lafontaine J.

J Med Chem. 2017 Apr 13;60(7):3002-3019. doi: 10.1021/acs.jmedchem.6b01894. Epub 2017 Mar 29.

PMID:
28287730
2.

Spectrum and Degree of CDK Drug Interactions Predicts Clinical Performance.

Chen P, Lee NV, Hu W, Xu M, Ferre RA, Lam H, Bergqvist S, Solowiej J, Diehl W, He YA, Yu X, Nagata A, VanArsdale T, Murray BW.

Mol Cancer Ther. 2016 Oct;15(10):2273-2281. Epub 2016 Aug 5.

3.

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.

Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC.

J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28.

PMID:
26756222
4.

Novel isoquinolone PDK1 inhibitors discovered through fragment-based lead discovery.

Johnson MC, Hu Q, Lingardo L, Ferre RA, Greasley S, Yan J, Kath J, Chen P, Ermolieff J, Alton G.

J Comput Aided Mol Des. 2011 Jul;25(7):689-98. doi: 10.1007/s10822-011-9456-7. Epub 2011 Jul 22.

PMID:
21779981
5.

Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation.

Vernier W, Chong W, Rewolinski D, Greasley S, Pauly T, Shaw M, Dinh D, Ferre RA, Meador JW 3rd, Nukui S, Ornelas M, Paz RL, Reyner E.

Bioorg Med Chem. 2010 May 1;18(9):3307-19. doi: 10.1016/j.bmc.2010.03.014. Epub 2010 Mar 11. Erratum in: Bioorg Med Chem. 2010 Oct 1;18(19):7144. Meador, James W 3rd [added]; Paz, Robert L [added].

PMID:
20363633
6.

The crystal structure of the RNA-dependent RNA polymerase from human rhinovirus: a dual function target for common cold antiviral therapy.

Love RA, Maegley KA, Yu X, Ferre RA, Lingardo LK, Diehl W, Parge HE, Dragovich PS, Fuhrman SA.

Structure. 2004 Aug;12(8):1533-44.

7.

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 8. Pharmacological optimization of orally bioavailable 2-pyridone-containing peptidomimetics.

Dragovich PS, Prins TJ, Zhou R, Johnson TO, Hua Y, Luu HT, Sakata SK, Brown EL, Maldonado FC, Tuntland T, Lee CA, Fuhrman SA, Zalman LS, Patick AK, Matthews DA, Wu EY, Guo M, Borer BC, Nayyar NK, Moran T, Chen L, Rejto PA, Rose PW, Guzman MC, Dovalsantos EZ, Lee S, McGee K, Mohajeri M, Liese A, Tao J, Kosa MB, Liu B, Batugo MR, Gleeson JP, Wu ZP, Liu J, Meador JW 3rd, Ferre RA.

J Med Chem. 2003 Oct 9;46(21):4572-85.

PMID:
14521419
8.

Structure of pteridine reductase (PTR1) from Leishmania tarentolae.

Zhao H, Bray T, Ouellette M, Zhao M, Ferre RA, Matthews D, Whiteley JM, Varughese KI.

Acta Crystallogr D Biol Crystallogr. 2003 Sep;59(Pt 9):1539-44. Epub 2003 Aug 19.

PMID:
12925782
9.

Structure-based design of a parallel synthetic array directed toward the discovery of irreversible inhibitors of human rhinovirus 3C protease.

Johnson TO, Hua Y, Luu HT, Brown EL, Chan F, Chu SS, Dragovich PS, Eastman BW, Ferre RA, Fuhrman SA, Hendrickson TF, Maldonado FC, Matthews DA, Meador JW 3rd, Patick AK, Reich SH, Skalitzky DJ, Worland ST, Yang M, Zalman LS.

J Med Chem. 2002 May 9;45(10):2016-23.

PMID:
11985469
10.

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics.

Dragovich PS, Prins TJ, Zhou R, Brown EL, Maldonado FC, Fuhrman SA, Zalman LS, Tuntland T, Lee CA, Patick AK, Matthews DA, Hendrickson TF, Kosa MB, Liu B, Batugo MR, Gleeson JP, Sakata SK, Chen L, Guzman MC, Meador JW 3rd, Ferre RA, Worland ST.

J Med Chem. 2002 Apr 11;45(8):1607-23.

PMID:
11931615
11.

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. Part 7: structure-activity studies of bicyclic 2-pyridone-containing peptidomimetics.

Dragovich PS, Prins TJ, Zhou R, Johnson TO, Brown EL, Maldonado FC, Fuhrman SA, Zalman LS, Patick AK, Matthews DA, Hou X, Meador JW, Ferre RA, Worland ST.

Bioorg Med Chem Lett. 2002 Mar 11;12(5):733-8.

PMID:
11858991
12.

Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors.

Webber SE, Marakovits JT, Dragovich PS, Prins TJ, Zhou R, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Srinivasan B, Moran T, Ford CE, Brothers MA, Harr JE, Meador JW 3rd, Ferre RA, Worland ST.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2683-6.

PMID:
11591501
13.

Substituted benzamide inhibitors of human rhinovirus 3C protease: structure-based design, synthesis, and biological evaluation.

Reich SH, Johnson T, Wallace MB, Kephart SE, Fuhrman SA, Worland ST, Matthews DA, Hendrickson TF, Chan F, Meador J 3rd, Ferre RA, Brown EL, DeLisle DM, Patick AK, Binford SL, Ford CE.

J Med Chem. 2000 May 4;43(9):1670-83.

PMID:
10794684
14.

Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors.

Dragovich PS, Zhou R, Webber SE, Prins TJ, Kwok AK, Okano K, Fuhrman SA, Zalman LS, Maldonado FC, Brown EL, Meador JW 3rd, Patick AK, Ford CE, Brothers MA, Binford SL, Matthews DA, Ferre RA, Worland ST.

Bioorg Med Chem Lett. 2000 Jan 3;10(1):45-8.

PMID:
10636240
15.

Structure-assisted design of mechanism-based irreversible inhibitors of human rhinovirus 3C protease with potent antiviral activity against multiple rhinovirus serotypes.

Matthews DA, Dragovich PS, Webber SE, Fuhrman SA, Patick AK, Zalman LS, Hendrickson TF, Love RA, Prins TJ, Marakovits JT, Zhou R, Tikhe J, Ford CE, Meador JW, Ferre RA, Brown EL, Binford SL, Brothers MA, DeLisle DM, Worland ST.

Proc Natl Acad Sci U S A. 1999 Sep 28;96(20):11000-7.

16.

Structure-based design of irreversible, tripeptidyl human rhinovirus 3C protease inhibitors containing N-methyl amino acids.

Dragovich PS, Webber SE, Prins TJ, Zhou R, Marakovits JT, Tikhe JG, Fuhrman SA, Patick AK, Matthews DA, Ford CE, Brown EL, Binford SL, Meador JW 3rd, Ferre RA, Worland ST.

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2189-94.

PMID:
10465543
17.

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements.

Dragovich PS, Prins TJ, Zhou R, Webber SE, Marakovits JT, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Ford CE, Burke BJ, Rejto PA, Hendrickson TF, Tuntland T, Brown EL, Meador JW 3rd, Ferre RA, Harr JE, Kosa MB, Worland ST.

J Med Chem. 1999 Apr 8;42(7):1213-24.

PMID:
10197965
18.

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics.

Dragovich PS, Prins TJ, Zhou R, Fuhrman SA, Patick AK, Matthews DA, Ford CE, Meador JW 3rd, Ferre RA, Worland ST.

J Med Chem. 1999 Apr 8;42(7):1203-12.

PMID:
10197964
19.

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 2. Peptide structure-activity studies.

Dragovich PS, Webber SE, Babine RE, Fuhrman SA, Patick AK, Matthews DA, Reich SH, Marakovits JT, Prins TJ, Zhou R, Tikhe J, Littlefield ES, Bleckman TM, Wallace MB, Little TL, Ford CE, Meador JW 3rd, Ferre RA, Brown EL, Binford SL, DeLisle DM, Worland ST.

J Med Chem. 1998 Jul 16;41(15):2819-34.

PMID:
9667971
20.

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 1. Michael acceptor structure-activity studies.

Dragovich PS, Webber SE, Babine RE, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Reich SH, Prins TJ, Marakovits JT, Littlefield ES, Zhou R, Tikhe J, Ford CE, Wallace MB, Meador JW 3rd, Ferre RA, Brown EL, Binford SL, Harr JE, DeLisle DM, Worland ST.

J Med Chem. 1998 Jul 16;41(15):2806-18.

PMID:
9667970
21.

Tripeptide aldehyde inhibitors of human rhinovirus 3C protease: design, synthesis, biological evaluation, and cocrystal structure solution of P1 glutamine isosteric replacements.

Webber SE, Okano K, Little TL, Reich SH, Xin Y, Fuhrman SA, Matthews DA, Love RA, Hendrickson TF, Patick AK, Meador JW 3rd, Ferre RA, Brown EL, Ford CE, Binford SL, Worland ST.

J Med Chem. 1998 Jul 16;41(15):2786-805.

PMID:
9667969
22.

Design, synthesis, and evaluation of nonpeptidic inhibitors of human rhinovirus 3C protease.

Webber SE, Tikhe J, Worland ST, Fuhrman SA, Hendrickson TF, Matthews DA, Love RA, Patick AK, Meador JW, Ferre RA, Brown EL, DeLisle DM, Ford CE, Binford SL.

J Med Chem. 1996 Dec 20;39(26):5072-82.

PMID:
8978838
23.

Structure of human rhinovirus 3C protease reveals a trypsin-like polypeptide fold, RNA-binding site, and means for cleaving precursor polyprotein.

Matthews DA, Smith WW, Ferre RA, Condon B, Budahazi G, Sisson W, Villafranca JE, Janson CA, McElroy HE, Gribskov CL, et al.

Cell. 1994 Jun 3;77(5):761-71.

PMID:
7515772
24.

2.3 A crystal structure of the catalytic domain of DNA polymerase beta.

Davies JF 2nd, Almassy RJ, Hostomska Z, Ferre RA, Hostomsky Z.

Cell. 1994 Mar 25;76(6):1123-33.

PMID:
8137427

Supplemental Content

Loading ...
Support Center