-
1
-
-
84862869077
-
Fragment-Based Approaches in Drug Discovery and Chemical Biology
-
Scott, D. E.; Coyne, A. G.; Hudson, S. A.; Abell, C. Fragment-Based Approaches in Drug Discovery and Chemical Biology Biochemistry 2012, 51, 4990-5003
-
(2012)
Biochemistry
, vol.51
, pp. 4990-5003
-
-
Scott, D.E.1
Coyne, A.G.2
Hudson, S.A.3
Abell, C.4
-
2
-
-
0034662911
-
Site-directed ligand discovery
-
Erlanson, D. A.; Braisted, A. C.; Raphael, D. R.; Randal, M.; Stroud, R. M.; Gordon, E. M.; Wells, J. A. Site-directed ligand discovery Proc. Natl. Acad. Sci. U. S. A. 2000, 97, 9367-9372 (Pubitemid 30650781)
-
(2000)
Proceedings of the National Academy of Sciences of the United States of America
, vol.97
, Issue.17
, pp. 9367-9372
-
-
Erlanson, D.A.1
Braisted, A.C.2
Raphael, D.R.3
Randal, M.4
Stroud, R.M.5
Gordon, E.M.6
Wells, J.A.7
-
3
-
-
2542542373
-
Tethering: Fragment-based drug discovery
-
DOI 10.1146/annurev.biophys.33.110502.140409
-
Erlanson, D. A.; Wells, J. A.; Braisted, A. C. Tethering: fragment-based drug discovery Annu. Rev. Biophys. Biomol. Struct. 2004, 33, 199-223 (Pubitemid 38829958)
-
(2004)
Annual Review of Biophysics and Biomolecular Structure
, vol.33
, pp. 199-223
-
-
Erlanson, D.A.1
Wells, J.A.2
Braisted, A.C.3
-
4
-
-
84876016325
-
Electrophilic fragment-based design of reversible covalent kinase inhibitors
-
Miller, R. M.; Paavilainen, V. O.; Krishnan, S.; Serafimova, I. M.; Taunton, J. Electrophilic fragment-based design of reversible covalent kinase inhibitors J. Am. Chem. Soc. 2013, 135, 5298-5301
-
(2013)
J. Am. Chem. Soc.
, vol.135
, pp. 5298-5301
-
-
Miller, R.M.1
Paavilainen, V.O.2
Krishnan, S.3
Serafimova, I.M.4
Taunton, J.5
-
5
-
-
79953314480
-
The resurgence of covalent drugs
-
Singh, J.; Petter, R. C.; Baillie, T. A.; Whitty, A. The resurgence of covalent drugs Nature Rev. Drug Discovery 2011, 10, 307-317
-
(2011)
Nature Rev. Drug Discovery
, vol.10
, pp. 307-317
-
-
Singh, J.1
Petter, R.C.2
Baillie, T.A.3
Whitty, A.4
-
7
-
-
84870354792
-
Identification of Cys255 in HIF-1α as a novel site for development of covalent inhibitors of HIF-1α/ARNT PasB domain protein-protein interaction
-
Cardoso, R.; Love, R.; Nilsson, C. L.; Bergqvist, S.; Nowlin, D.; Yan, J.; Liu, K. K.; Zhu, J.; Chen, P.; Deng, Y. L.; Dyson, H. J.; Greig, M. J.; Brooun, A. Identification of Cys255 in HIF-1α as a novel site for development of covalent inhibitors of HIF-1α/ARNT PasB domain protein-protein interaction Protein Sci. 2012, 21, 1885-1896
-
(2012)
Protein Sci.
, vol.21
, pp. 1885-1896
-
-
Cardoso, R.1
Love, R.2
Nilsson, C.L.3
Bergqvist, S.4
Nowlin, D.5
Yan, J.6
Liu, K.K.7
Zhu, J.8
Chen, P.9
Deng, Y.L.10
Dyson, H.J.11
Greig, M.J.12
Brooun, A.13
-
8
-
-
78650078496
-
Quantitative reactivity profiling predicts functional cysteines in proteomes
-
Weerapana, E.; Wang, C.; Simon, G. M.; Richter, F.; Khare, S.; Dillon, M. B.; Bachovchin, D. A.; Mowen, K.; Baker, D.; Cravatt, B. F. Quantitative reactivity profiling predicts functional cysteines in proteomes Nature 2010, 468, 790-795
-
(2010)
Nature
, vol.468
, pp. 790-795
-
-
Weerapana, E.1
Wang, C.2
Simon, G.M.3
Richter, F.4
Khare, S.5
Dillon, M.B.6
Bachovchin, D.A.7
Mowen, K.8
Baker, D.9
Cravatt, B.F.10
-
9
-
-
84870260588
-
Kinetic Template-Guided Tethering of Fragments
-
Nonoo, R. H.; Armstrong, A.; Mann, D. J. Kinetic Template-Guided Tethering of Fragments ChemMedChem 2012, 7, 2082-2086
-
(2012)
ChemMedChem
, vol.7
, pp. 2082-2086
-
-
Nonoo, R.H.1
Armstrong, A.2
Mann, D.J.3
-
10
-
-
80053336043
-
Falcipains and other cysteine proteases of malaria parasites
-
Rosenthal, P. J. Falcipains and other cysteine proteases of malaria parasites Adv. Exp. Med. Biol. 2011, 712, 30-48
-
(2011)
Adv. Exp. Med. Biol.
, vol.712
, pp. 30-48
-
-
Rosenthal, P.J.1
-
11
-
-
0042352240
-
Elative rates of Michael reactions of 2-(phenethyl)thiol with vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides relevant to vinyl sulfonyl cysteine protease inhibitors
-
DOI 10.1021/ol034555l
-
Reddick, J. J.; Cheng, J.; Roush, W. R. Relative Rates of Michael Reactions of 2′-(Phenethyl)thiol with Vinyl Sulfones, Vinyl Sulfonate Esters, and Vinyl Sulfonamides Relevant to Vinyl Sulfonyl Cysteine Protease Inhibitors Org. Lett. 2003, 5, 1967-1970 (Pubitemid 37161970)
-
(2003)
Organic Letters
, vol.5
, Issue.11
, pp. 1967-1970
-
-
Reddick, J.J.1
Cheng, J.2
Roush, W.R.3
-
12
-
-
0038344159
-
Reactivity of functional groups on the protein surface: Development of epoxide probes for protein labeling
-
DOI 10.1021/ja034287m
-
Chen, G.; Heim, A.; Riether, D.; Yee, D.; Milgrom, Y.; Gawinowicz, M. A.; Sames, D. Reactivity of Functional Groups on the Protein Surface: Development of Epoxide Probes for Protein Labeling J. Am. Chem. Soc. 2003, 125, 8130-8133 (Pubitemid 36828576)
-
(2003)
Journal of the American Chemical Society
, vol.125
, Issue.27
, pp. 8130-8133
-
-
Chen, G.1
Heim, A.2
Riether, D.3
Yee, D.4
Milgrom, Y.5
Gawinowicz, M.A.6
Sames, D.7
-
13
-
-
0021260942
-
Vinylogous amino acid esters: A new class of inactivators for thiol proteases
-
Hanzlik, R. P.; Thompson, S. A. Vinylogous Amino Acid Esters: A New Class of Inactivators for Thiol Proteases J. Med. Chem. 1984, 27, 711-712 (Pubitemid 14082800)
-
(1984)
Journal of Medicinal Chemistry
, vol.27
, Issue.6
, pp. 711-712
-
-
Hanzlik, R.P.1
Thompson, S.A.2
-
14
-
-
64549114104
-
Novel Peptidomimetics Containing a Vinyl Ester Moiety as Highly Potent and Selective Falcipain-2 Inhibitors
-
Ettari, R.; Micale, N.; Schirmeister, T.; Gelhaus, C.; Leippe, M.; Nizi, E.; Di Francesco, M. E.; Grasso, S.; Zappalà, M. Novel Peptidomimetics Containing a Vinyl Ester Moiety as Highly Potent and Selective Falcipain-2 Inhibitors J. Med. Chem. 2009, 52, 2157-60
-
(2009)
J. Med. Chem.
, vol.52
, pp. 2157-2160
-
-
Ettari, R.1
Micale, N.2
Schirmeister, T.3
Gelhaus, C.4
Leippe, M.5
Nizi, E.6
Di Francesco, M.E.7
Grasso, S.8
Zappalà, M.9
-
15
-
-
21144432811
-
In vitro antiviral activity and single-dose pharmacokinetics in humans of a novel, orally bioavailable inhibitor of human rhinovirus 3C protease
-
DOI 10.1128/AAC.49.6.2267-2275.2005
-
Patick, A. K.; Brothers, M. A.; Maldonado, F.; Binford, S.; Maldonado, O.; Fuhrman, S.; Petersen, A.; Smith, G. J., III; Zalman, L. S.; Burns-Naas, L. A.; Tran, J. Q. In Vitro Antiviral Activity and Single-Dose Pharmacokinetics in Humans of a Novel, Orally Bioavailable Inhibitor of Human Rhinovirus 3C Protease Antimicrob. Agents Chemother. 2005, 49, 2267-2275 (Pubitemid 40734453)
-
(2005)
Antimicrobial Agents and Chemotherapy
, vol.49
, Issue.6
, pp. 2267-2275
-
-
Patick, A.K.1
Brothers, M.A.2
Maldonado, F.3
Binford, S.4
Maldonado, O.5
Fuhrman, S.6
Petersen, A.7
Smith III, G.J.8
Zalman, L.S.9
Burns-Naas, L.A.10
Tran, J.Q.11
-
16
-
-
0141726877
-
-
Congreve, M.; Carr, R.; Murray, C.; Jhoti, H. A. Drug Discovery Today 2003, 8, 876-877
-
(2003)
Drug Discovery Today
, vol.8
, pp. 876-877
-
-
Congreve, M.1
Carr, R.2
Murray, C.3
Jhoti, H.A.4
-
17
-
-
80053336043
-
Falcipains and other cysteine proteases of malaria parasites
-
Rosenthal, P. J. Falcipains and other cysteine proteases of malaria parasites Adv. Exp. Med. Biol. 2011, 712, 30-48
-
(2011)
Adv. Exp. Med. Biol.
, vol.712
, pp. 30-48
-
-
Rosenthal, P.J.1
-
18
-
-
0026517333
-
Structure-activity relationships for inhibition of papain by peptide Michael acceptors
-
Liu, S.; Hanzlik, R. P. Structure-activity relationships for inhibition of papain by peptide Michael acceptors J. Med. Chem. 1992, 35, 1067-1075
-
(1992)
J. Med. Chem.
, vol.35
, pp. 1067-1075
-
-
Liu, S.1
Hanzlik, R.P.2
-
20
-
-
0036882396
-
Irreversible Inhibitors of Serine, Cysteine, and Threonine Proteases
-
Powers, J. C.; Asgian, J. L.; Ekici, O. D.; James, K. E. Irreversible Inhibitors of Serine, Cysteine, and Threonine Proteases Chem. Rev. 2002, 102, 4639-4750
-
(2002)
Chem. Rev.
, vol.102
, pp. 4639-4750
-
-
Powers, J.C.1
Asgian, J.L.2
Ekici, O.D.3
James, K.E.4
-
21
-
-
84874945035
-
Approaches for enhancing oral bioavailability of peptides and proteins
-
Renukuntla, J.; Vadlapudi, A. D.; Patel, A.; Boddu, S. H.; Mitra, A. K. Approaches for enhancing oral bioavailability of peptides and proteins Int. J. Pharm. 2013, 447, 75-93
-
(2013)
Int. J. Pharm.
, vol.447
, pp. 75-93
-
-
Renukuntla, J.1
Vadlapudi, A.D.2
Patel, A.3
Boddu, S.H.4
Mitra, A.K.5
-
22
-
-
84881137952
-
USP8 is a novel target for overcoming gefitinib-resistance in lung cancer
-
Byun, S.; Lee, S. Y.; Lee, J.; Jeong, C. H.; Farrand, L.; Lim, S.; Reddy, K.; Kim, J. Y.; Lee, M. H.; Lee, H. J.; Bode, A. M.; Lee, K. W.; Dong, Z. USP8 is a novel target for overcoming gefitinib-resistance in lung cancer Clin. Cancer Res. 2013, 19, 3894-904
-
(2013)
Clin. Cancer Res.
, vol.19
, pp. 3894-3904
-
-
Byun, S.1
Lee, S.Y.2
Lee, J.3
Jeong, C.H.4
Farrand, L.5
Lim, S.6
Reddy, K.7
Kim, J.Y.8
Lee, M.H.9
Lee, H.J.10
Bode, A.M.11
Lee, K.W.12
Dong, Z.13
-
23
-
-
63049130207
-
Novel control of S phase of the cell cycle by ubiquitin-conjugating enzyme H7
-
Whitcomb, E. A.; Dudek, E. J.; Liu, Q.; Taylor, A. Novel control of S phase of the cell cycle by ubiquitin-conjugating enzyme H7 Mol. Biol. Cell 2009, 20, 1-9
-
(2009)
Mol. Biol. Cell
, vol.20
, pp. 1-9
-
-
Whitcomb, E.A.1
Dudek, E.J.2
Liu, Q.3
Taylor, A.4
-
24
-
-
73649151319
-
Esters of Methanesulfonic Acid as Irreversible Inhibitors of Acetylcholinesterase
-
Kitz, R.; Wilson, I. B. Esters of Methanesulfonic Acid as Irreversible Inhibitors of Acetylcholinesterase J. Biol. Chem. 1962, 237, 3245-3249
-
(1962)
J. Biol. Chem.
, vol.237
, pp. 3245-3249
-
-
Kitz, R.1
Wilson, I.B.2
|