-
2
-
-
84866772206
-
Targeted covalent enzyme inhibitors
-
M.C. Noe, and A.M. Gilbert Targeted covalent enzyme inhibitors Annu. Rep. Med. Chem. 47 2012 413 439
-
(2012)
Annu. Rep. Med. Chem.
, vol.47
, pp. 413-439
-
-
Noe, M.C.1
Gilbert, A.M.2
-
3
-
-
17244362388
-
Mechanistic basis of enzyme-targeted drugs
-
J.G. Robertson Mechanistic basis of enzyme-targeted drugs Biochemistry 44 2005 5561 5571
-
(2005)
Biochemistry
, vol.44
, pp. 5561-5571
-
-
Robertson, J.G.1
-
4
-
-
79953314480
-
The resurgence of covalent drugs
-
J. Singh, and et al. The resurgence of covalent drugs Nat. Rev. Drug Discov. 10 2011 307 317
-
(2011)
Nat. Rev. Drug Discov.
, vol.10
, pp. 307-317
-
-
Singh, J.1
-
5
-
-
64349093749
-
Covalent modifiers: An orthogonal approach to drug design
-
M.H. Potashman, and M.E. Duggan Covalent modifiers: an orthogonal approach to drug design J. Med. Chem. 52 2009 1231 1246
-
(2009)
J. Med. Chem.
, vol.52
, pp. 1231-1246
-
-
Potashman, M.H.1
Duggan, M.E.2
-
6
-
-
77953631133
-
Strategies for discovering and derisking covalent, irreversible enzyme inhibitors
-
D.S. Johnson, and et al. Strategies for discovering and derisking covalent, irreversible enzyme inhibitors Future Med. Chem. 2 2010 949 964
-
(2010)
Future Med. Chem.
, vol.2
, pp. 949-964
-
-
Johnson, D.S.1
-
7
-
-
84862877720
-
Drug discovery for a new generation of covalent drugs
-
A.S. Kalgutkar, and D.K. Dalvie Drug discovery for a new generation of covalent drugs Expert Opin. Drug Discov. 7 2012 561 581
-
(2012)
Expert Opin. Drug Discov.
, vol.7
, pp. 561-581
-
-
Kalgutkar, A.S.1
Dalvie, D.K.2
-
8
-
-
84870190055
-
Reversible Michael additions: Covalent inhibitors and prodrugs
-
M.H. Johansson Reversible Michael additions: covalent inhibitors and prodrugs Mini-Rev. Med. Chem. 12 2012 1330 1344
-
(2012)
Mini-Rev. Med. Chem.
, vol.12
, pp. 1330-1344
-
-
Johansson, M.H.1
-
9
-
-
84885603664
-
Keap calm, and carry on covalently
-
A.J. Wilson, and et al. Keap calm, and carry on covalently J. Med. Chem. 56 2013 7463 7476
-
(2013)
J. Med. Chem.
, vol.56
, pp. 7463-7476
-
-
Wilson, A.J.1
-
10
-
-
84891496533
-
Drug discovery considerations in the development of covalent inhibitors
-
R. Mah Drug discovery considerations in the development of covalent inhibitors Bioorg. Med. Chem. Lett. 24 2014 33 39
-
(2014)
Bioorg. Med. Chem. Lett.
, vol.24
, pp. 33-39
-
-
Mah, R.1
-
11
-
-
0001299961
-
Acetylation of prostaglandin synthase by aspirin
-
G.J. Roth, and et al. Acetylation of prostaglandin synthase by aspirin Proc. Natl. Acad. Sci. U. S. A. 72 1975 3073 3076
-
(1975)
Proc. Natl. Acad. Sci. U. S. A.
, vol.72
, pp. 3073-3076
-
-
Roth, G.J.1
-
12
-
-
84905994821
-
The evolving role of chemical synthesis in antibacterial drug discovery
-
P.M. Wright, and et al. The evolving role of chemical synthesis in antibacterial drug discovery Angew. Chem. Int. Ed. 53 2014 8840 8869
-
(2014)
Angew. Chem. Int. Ed.
, vol.53
, pp. 8840-8869
-
-
Wright, P.M.1
-
13
-
-
0037313425
-
A proton-pump inhibitor expedition: The case histories of omeprazole and esomeprazole
-
L. Olbe, and et al. A proton-pump inhibitor expedition: the case histories of omeprazole and esomeprazole Nat. Rev. Drug Discov. 2 2003 132 139
-
(2003)
Nat. Rev. Drug Discov.
, vol.2
, pp. 132-139
-
-
Olbe, L.1
-
14
-
-
0033678468
-
Identification and biological activity of the active metabolite of clopidogrel
-
P. Savi, and et al. Identification and biological activity of the active metabolite of clopidogrel Thromb. Haemostasis 84 2000 891 896
-
(2000)
Thromb. Haemostasis
, vol.84
, pp. 891-896
-
-
Savi, P.1
-
15
-
-
24944450694
-
Protein-reactive natural products
-
C. Drahl, and et al. Protein-reactive natural products Angew. Chem. Int. Ed. 44 2005 5788 5809
-
(2005)
Angew. Chem. Int. Ed.
, vol.44
, pp. 5788-5809
-
-
Drahl, C.1
-
16
-
-
84877335817
-
Biotech's wellspring: The health of private biotech in 2012
-
B. Huggett Biotech's wellspring: the health of private biotech in 2012 Nat. Biotechnol. 31 2013 396 404
-
(2013)
Nat. Biotechnol.
, vol.31
, pp. 396-404
-
-
Huggett, B.1
-
17
-
-
84886568855
-
Principia biopharma
-
K. Garber Principia biopharma Nat. Biotechnol. 31 2013 377
-
(2013)
Nat. Biotechnol.
, vol.31
, pp. 377
-
-
Garber, K.1
-
18
-
-
84860434846
-
Covalent drugs form long-lived ties
-
L. Guterman Covalent drugs form long-lived ties Chem. Eng. News 89 2011 19 26
-
(2011)
Chem. Eng. News
, vol.89
, pp. 19-26
-
-
Guterman, L.1
-
19
-
-
0031726163
-
The metabolism of xenobiotics to reactive electrophiles in chemical carcinogenesis and mutagenesis: A collaboration with Elizabeth Cavert Miller and our associates
-
J.A. Miller The metabolism of xenobiotics to reactive electrophiles in chemical carcinogenesis and mutagenesis: a collaboration with Elizabeth Cavert Miller and our associates Drug Metab. Rev. 30 1998 645 674
-
(1998)
Drug Metab. Rev.
, vol.30
, pp. 645-674
-
-
Miller, J.A.1
-
20
-
-
0015754446
-
Acetaminophen-induced hepatic necrosis. II. Role of covalent binding in vivo
-
D.J. Jollow, and et al. Acetaminophen-induced hepatic necrosis. II. Role of covalent binding in vivo J. Pharmacol. Exp. Ther. 187 1973 195 202
-
(1973)
J. Pharmacol. Exp. Ther.
, vol.187
, pp. 195-202
-
-
Jollow, D.J.1
-
21
-
-
0034488213
-
Use of paracetamol (acetaminophen) for suicide and nonfatal poisoning: Worldwide patterns of use and misuse
-
D. Gunnell, and et al. Use of paracetamol (acetaminophen) for suicide and nonfatal poisoning: worldwide patterns of use and misuse Suicide Life-Threat. 30 2010 313 326
-
(2010)
Suicide Life-Threat.
, vol.30
, pp. 313-326
-
-
Gunnell, D.1
-
22
-
-
0036093183
-
Identification of seven proteins in the endoplasmic reticulum as targets for reactive metabolites of bromobenzene
-
Y.M. Koen, and R.P. Hanzlik Identification of seven proteins in the endoplasmic reticulum as targets for reactive metabolites of bromobenzene Chem. Res. Toxicol. 15 2002 699 706
-
(2002)
Chem. Res. Toxicol.
, vol.15
, pp. 699-706
-
-
Koen, Y.M.1
Hanzlik, R.P.2
-
23
-
-
0020359550
-
Contact sensitivity to urushiol: Role of covalent bond formation
-
I.S. Dunn, and et al. Contact sensitivity to urushiol: role of covalent bond formation Cell. Immunol. 74 1982 220 233
-
(1982)
Cell. Immunol.
, vol.74
, pp. 220-233
-
-
Dunn, I.S.1
-
24
-
-
0034043197
-
Repeated dose study of sucralose tolerance in human subjects
-
I.M. Baird, and et al. Repeated dose study of sucralose tolerance in human subjects Food Chem. Toxicol. 38 Suppl. 2 2000 S123 S129
-
(2000)
Food Chem. Toxicol.
, vol.38
, pp. S123-S129
-
-
Baird, I.M.1
-
25
-
-
84882625055
-
Covalent adduction of nitrogen mustards to model protein nucleophiles
-
V.R. Thompson, and A.P. DeCaprio Covalent adduction of nitrogen mustards to model protein nucleophiles Chem. Res. Toxicol. 26 2013 1263 1271
-
(2013)
Chem. Res. Toxicol.
, vol.26
, pp. 1263-1271
-
-
Thompson, V.R.1
DeCaprio, A.P.2
-
26
-
-
70349103856
-
A zone classification system for risk assessment of idiosyncratic drug toxicity using daily dose and covalent binding
-
S. Nakayama, and et al. A zone classification system for risk assessment of idiosyncratic drug toxicity using daily dose and covalent binding Drug Metab. Dispos. 37 2009 1970 1977
-
(2009)
Drug Metab. Dispos.
, vol.37
, pp. 1970-1977
-
-
Nakayama, S.1
-
27
-
-
33845491064
-
Chemical toxicology: Reactive intermediates and their role in pharmacology and toxicology
-
J.C.L. Erve Chemical toxicology: reactive intermediates and their role in pharmacology and toxicology Expert Opin. Metab. Toxicol. 2 2006 923 946
-
(2006)
Expert Opin. Metab. Toxicol.
, vol.2
, pp. 923-946
-
-
Erve, J.C.L.1
-
28
-
-
18844373318
-
Role of metabolism in drug-induced idiosyncratic hepatotoxicity
-
J.L. Walgren, and et al. Role of metabolism in drug-induced idiosyncratic hepatotoxicity Crit. Rev. Toxicol. 35 2005 325 361
-
(2005)
Crit. Rev. Toxicol.
, vol.35
, pp. 325-361
-
-
Walgren, J.L.1
-
29
-
-
46249118651
-
Relationship between daily dose of oral medications and idiosyncratic drug-induced liver injury: Search for signals
-
C. Lammert, and et al. Relationship between daily dose of oral medications and idiosyncratic drug-induced liver injury: search for signals Hepatology 47 2008 2003 2009
-
(2008)
Hepatology
, vol.47
, pp. 2003-2009
-
-
Lammert, C.1
-
30
-
-
0032789796
-
New concepts in immunology relevant to idiosyncratic drug reactions. The 'danger hypothesis' and innate immune system
-
J.P. Uetrecht New concepts in immunology relevant to idiosyncratic drug reactions. The 'danger hypothesis' and innate immune system Chem. Res. Toxicol. 12 1999 387 395
-
(1999)
Chem. Res. Toxicol.
, vol.12
, pp. 387-395
-
-
Uetrecht, J.P.1
-
31
-
-
4344645978
-
Can the pharmaceutical industry reduce attrition rates?
-
I. Kola, and J. Landis Can the pharmaceutical industry reduce attrition rates? Nat. Rev. Drug Discov. 3 2004 711 715
-
(2004)
Nat. Rev. Drug Discov.
, vol.3
, pp. 711-715
-
-
Kola, I.1
Landis, J.2
-
32
-
-
0037264608
-
A guide to drug discovery: Target selection in drug discovery
-
J. Knowles, and G. Gromo A guide to drug discovery: target selection in drug discovery Nat. Rev. Drug Discov. 2 2003 63 69
-
(2003)
Nat. Rev. Drug Discov.
, vol.2
, pp. 63-69
-
-
Knowles, J.1
Gromo, G.2
-
33
-
-
4544381198
-
Biochemical mechanisms of drug action: What does it take for success?
-
D.C. Swinney Biochemical mechanisms of drug action: what does it take for success? Nat. Rev. Drug Discov. 3 2004 801 808
-
(2004)
Nat. Rev. Drug Discov.
, vol.3
, pp. 801-808
-
-
Swinney, D.C.1
-
34
-
-
33646122469
-
Biochemical mechanisms of new molecular entities (NMEs) approved by United States FDA during 2001-2004
-
D.C. Swinney Biochemical mechanisms of new molecular entities (NMEs) approved by United States FDA during 2001-2004 Curr. Top. Med. Chem. 6 2006 461 478
-
(2006)
Curr. Top. Med. Chem.
, vol.6
, pp. 461-478
-
-
Swinney, D.C.1
-
35
-
-
84864246491
-
Irreversible kinase inhibitors: Balancing the benefits and risks
-
T. Barf, and A. Kaptein Irreversible kinase inhibitors: balancing the benefits and risks J. Med. Chem. 55 2012 6243 6262
-
(2012)
J. Med. Chem.
, vol.55
, pp. 6243-6262
-
-
Barf, T.1
Kaptein, A.2
-
36
-
-
0033621044
-
The maximal affinity of ligands
-
I.D. Kuntz, and et al. The maximal affinity of ligands Proc. Natl. Acad. Sci. U. S. A. 96 1999 9997 10002
-
(1999)
Proc. Natl. Acad. Sci. U. S. A.
, vol.96
, pp. 9997-10002
-
-
Kuntz, I.D.1
-
37
-
-
60449094541
-
Beyond picomolar affinities: Quantitative aspects of noncovalent and covalent binding of drugs to proteins
-
A.J.T. Smith, and et al. Beyond picomolar affinities: quantitative aspects of noncovalent and covalent binding of drugs to proteins J. Med. Chem. 52 2009 225 233
-
(2009)
J. Med. Chem.
, vol.52
, pp. 225-233
-
-
Smith, A.J.T.1
-
38
-
-
0031718551
-
Clinical pharmacology of rivastigmine: A new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease
-
R.J. Polinsky Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease Clin. Ther. 20 1998 634 647
-
(1998)
Clin. Ther.
, vol.20
, pp. 634-647
-
-
Polinsky, R.J.1
-
39
-
-
0034871011
-
A systematic review of the associations between dose regimens and medication compliance
-
A.J. Claxton, and et al. A systematic review of the associations between dose regimens and medication compliance Clin. Ther. 23 2001 1296 1310
-
(2001)
Clin. Ther.
, vol.23
, pp. 1296-1310
-
-
Claxton, A.J.1
-
40
-
-
84925446013
-
A proposed screening paradigm for discovery of covalent inhibitor drugs
-
M.F. Moghaddam, and et al. A proposed screening paradigm for discovery of covalent inhibitor drugs Drug Metab. Lett. 8 2014 19 30
-
(2014)
Drug Metab. Lett.
, vol.8
, pp. 19-30
-
-
Moghaddam, M.F.1
-
41
-
-
40049099220
-
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
-
C-H. Yun, and et al. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP Proc. Natl. Acad. Sci. U. S. A. 105 2008 2070 2075
-
(2008)
Proc. Natl. Acad. Sci. U. S. A.
, vol.105
, pp. 2070-2075
-
-
Yun, C.-H.1
-
42
-
-
84874301754
-
Developing irreversible inhibitors of the protein kinase cysteinome
-
Q. Liu, and et al. Developing irreversible inhibitors of the protein kinase cysteinome Chem. Biol. 20 2013 146 159
-
(2013)
Chem. Biol.
, vol.20
, pp. 146-159
-
-
Liu, Q.1
-
43
-
-
84887497121
-
The quest to overcome resistance to EGFR-targeted therapies in cancer
-
C.R. Chong, and P.A. Jänne The quest to overcome resistance to EGFR-targeted therapies in cancer Nat. Med. 19 2013 1389 1400
-
(2013)
Nat. Med.
, vol.19
, pp. 1389-1400
-
-
Chong, C.R.1
Jänne, P.A.2
-
44
-
-
0038058949
-
Elucidation of HIV-1 protease resistance by characterization of interaction kinetics between inhibitors and enzyme variants
-
C.F. Shuman, and et al. Elucidation of HIV-1 protease resistance by characterization of interaction kinetics between inhibitors and enzyme variants Antiviral Res. 58 2003 235 242
-
(2003)
Antiviral Res.
, vol.58
, pp. 235-242
-
-
Shuman, C.F.1
-
45
-
-
78650513897
-
Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine
-
M. Hagel, and et al. Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine Nat. Chem. Biol. 7 2011 22 24
-
(2011)
Nat. Chem. Biol.
, vol.7
, pp. 22-24
-
-
Hagel, M.1
-
46
-
-
65249117514
-
Identifying and characterizing binding sites and assessing druggability
-
T.A. Halgren Identifying and characterizing binding sites and assessing druggability J. Chem. Inf. Model. 49 2009 377 389
-
(2009)
J. Chem. Inf. Model.
, vol.49
, pp. 377-389
-
-
Halgren, T.A.1
-
47
-
-
85050577226
-
The year in new drugs
-
L.M. Jarvis The year in new drugs Chem. Eng. News 92 2014 10 13
-
(2014)
Chem. Eng. News
, vol.92
, pp. 10-13
-
-
Jarvis, L.M.1
-
48
-
-
84861760527
-
Differential sensitivity of glioma- versus lung cancer-specific EGFR mutations to EGFR kinase inhibitors
-
I. Vivanco, and et al. Differential sensitivity of glioma- versus lung cancer-specific EGFR mutations to EGFR kinase inhibitors Cancer Discov. 2 2012 459 471
-
(2012)
Cancer Discov.
, vol.2
, pp. 459-471
-
-
Vivanco, I.1
-
49
-
-
84891946419
-
Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance
-
P.A. Schwartz, and et al. Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance Proc. Natl. Acad. Sci. U. S. A. 111 2014 173 178
-
(2014)
Proc. Natl. Acad. Sci. U. S. A.
, vol.111
, pp. 173-178
-
-
Schwartz, P.A.1
-
50
-
-
57349141390
-
BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors
-
N. Minkovsky, and A. Berezov BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors Curr. Opin. Investig. Drugs 9 2008 1336 1346
-
(2008)
Curr. Opin. Investig. Drugs
, vol.9
, pp. 1336-1346
-
-
Minkovsky, N.1
Berezov, A.2
-
51
-
-
84858669035
-
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): A better mousetrap? A review of the clinical evidence
-
S-H.I. Ou Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence Crit. Rev. Oncol. Hematol. 83 2012 47 421
-
(2012)
Crit. Rev. Oncol. Hematol.
, vol.83
, pp. 47-421
-
-
Ou, S.-H.I.1
-
52
-
-
84896732823
-
Bruton's tyrosine kinase (BTK) inhibitors in clinical trials
-
J.A. Burger Bruton's tyrosine kinase (BTK) inhibitors in clinical trials Curr. Hematol. Malig. Rep. 9 2014 44 49
-
(2014)
Curr. Hematol. Malig. Rep.
, vol.9
, pp. 44-49
-
-
Burger, J.A.1
-
53
-
-
77955625479
-
The bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy
-
L.A. Honigberg, and et al. The bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy Proc. Natl. Acad. Sci. U. S. A. 107 2010 13075 13080
-
(2010)
Proc. Natl. Acad. Sci. U. S. A.
, vol.107
, pp. 13075-13080
-
-
Honigberg, L.A.1
-
54
-
-
84883160397
-
Ibrutinib and novel BTK inhibitors in clinical development
-
A. Akinleye, and et al. Ibrutinib and novel BTK inhibitors in clinical development J. Hemat. Oncol. 6 2013 59 67
-
(2013)
J. Hemat. Oncol.
, vol.6
, pp. 59-67
-
-
Akinleye, A.1
-
55
-
-
84903537320
-
The clinical development of MEK inhibitors
-
Y. Zhao, and A.A. Adjei The clinical development of MEK inhibitors Nat. Rev. Clin. Oncol. 11 2014 385 400
-
(2014)
Nat. Rev. Clin. Oncol.
, vol.11
, pp. 385-400
-
-
Zhao, Y.1
Adjei, A.A.2
-
56
-
-
77952109517
-
Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III
-
Y. Shen, and et al. Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III Bioorg. Med. Chem. Lett. 20 2010 3155 3157
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 3155-3157
-
-
Shen, Y.1
-
57
-
-
84928884201
-
Mechanism of action of the anti-cancer agent, Triptolide
-
F.H. Sarkar, Springer
-
V. Sangwan, and A.K. Saluja Mechanism of action of the anti-cancer agent, Triptolide F.H. Sarkar, Nutraceuticals and Cancer 2012 Springer 135 150
-
(2012)
Nutraceuticals and Cancer
, pp. 135-150
-
-
Sangwan, V.1
Saluja, A.K.2
-
58
-
-
34547203981
-
Triptolide binds covalently to a 90 kDa nuclear protein. Role of epoxides in binding and activity
-
C. McCallum, and et al. Triptolide binds covalently to a 90 kDa nuclear protein. Role of epoxides in binding and activity Immunobiology 212 2007 549 556
-
(2007)
Immunobiology
, vol.212
, pp. 549-556
-
-
McCallum, C.1
-
59
-
-
4444223702
-
Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling
-
N.T. Ihle, and et al. Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling Mol. Cancer Ther. 3 2004 763 772
-
(2004)
Mol. Cancer Ther.
, vol.3
, pp. 763-772
-
-
Ihle, N.T.1
-
60
-
-
84856373151
-
Proteasome inhibitors: An expanding army attacking a unique target
-
A.F. Kisselev, and et al. Proteasome inhibitors: an expanding army attacking a unique target Chem. Biol. 19 2012 99 115
-
(2012)
Chem. Biol.
, vol.19
, pp. 99-115
-
-
Kisselev, A.F.1
-
61
-
-
0036181371
-
Development of the proteasome inhibitor PS-341
-
J. Adams Development of the proteasome inhibitor PS-341 Oncologist 7 2002 9 16
-
(2002)
Oncologist
, vol.7
, pp. 9-16
-
-
Adams, J.1
-
62
-
-
79952136166
-
Fumaric acid esters exert neuroprotective effects in neuroinflammation via activation of the Nrf2 antioxidant pathway
-
R.A. Linker, and et al. Fumaric acid esters exert neuroprotective effects in neuroinflammation via activation of the Nrf2 antioxidant pathway Brain 134 2011 678 692
-
(2011)
Brain
, vol.134
, pp. 678-692
-
-
Linker, R.A.1
-
63
-
-
84902491159
-
Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO
-
T.G. Davies, and et al. Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO PLoS ONE 9 2014 98896
-
(2014)
PLoS ONE
, vol.9
, pp. 98896
-
-
Davies, T.G.1
-
64
-
-
0015856236
-
Effect of ethacrynic acid on the thick ascending limp of Henle's loop
-
M. Burg, and N. Green Effect of ethacrynic acid on the thick ascending limp of Henle's loop Kidney Intl. 4 1973 301 308
-
(1973)
Kidney Intl.
, vol.4
, pp. 301-308
-
-
Burg, M.1
Green, N.2
-
65
-
-
0028209437
-
Reversible conjugation of ethacrynic acid with glutathione and human glutathione S-transferase P 1-1
-
J.H.T.M. Ploemen, and et al. Reversible conjugation of ethacrynic acid with glutathione and human glutathione S-transferase P 1-1 Cancer Res. 54 1994 915 919
-
(1994)
Cancer Res.
, vol.54
, pp. 915-919
-
-
Ploemen, J.H.T.M.1
-
66
-
-
60249099489
-
The pleiotropic effects of ethacrynic acid
-
J.C. Somberg, and J. Molnar The pleiotropic effects of ethacrynic acid Am. J. Ther. 16 2009 102 104
-
(2009)
Am. J. Ther.
, vol.16
, pp. 102-104
-
-
Somberg, J.C.1
Molnar, J.2
-
67
-
-
84863905057
-
Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor
-
D.E. Ehmann, and et al. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor Proc. Natl. Acad. Sci. U. S. A. 109 2012 11663 11668
-
(2012)
Proc. Natl. Acad. Sci. U. S. A.
, vol.109
, pp. 11663-11668
-
-
Ehmann, D.E.1
-
68
-
-
84896045360
-
Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
-
A.A. Joharapurkar, and et al. Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity Diabetes Metab. Syndr. Obes. Target Ther. 7 2014 73 84
-
(2014)
Diabetes Metab. Syndr. Obes. Target Ther.
, vol.7
, pp. 73-84
-
-
Joharapurkar, A.A.1
-
69
-
-
84884905713
-
Ascending dose-controlled trial of beloranib, a novel obesity treatment for safety, tolerability, and weight loss in obese women
-
T.E. Hughes, and et al. Ascending dose-controlled trial of beloranib, a novel obesity treatment for safety, tolerability, and weight loss in obese women Obesity 21 2013 1782 1788
-
(2013)
Obesity
, vol.21
, pp. 1782-1788
-
-
Hughes, T.E.1
-
71
-
-
79951518976
-
Discovery of PF-04457845: A highly potent, orally bioavailable, and selective urea FAAH inhibitor
-
D.S. Johnson, and et al. Discovery of PF-04457845: a highly potent, orally bioavailable, and selective urea FAAH inhibitor ACS Med. Chem. Lett. 2 2011 91 96
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 91-96
-
-
Johnson, D.S.1
-
72
-
-
79959506821
-
Mechanistic and pharmacological characterization of PF-04457845: A highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain
-
K. Ahn, and et al. Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain J. Pharmacol. Exp. Ther. 338 2011 114 124
-
(2011)
J. Pharmacol. Exp. Ther.
, vol.338
, pp. 114-124
-
-
Ahn, K.1
-
73
-
-
0033985927
-
Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease
-
M.W. Jann Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease Pharmacotherapy 20 2000 1 12
-
(2000)
Pharmacotherapy
, vol.20
, pp. 1-12
-
-
Jann, M.W.1
-
74
-
-
0029937631
-
Mechanism-based inhibition of human steroid 5α-reductase by finasteride: Enzyme-catalyzed formation of NADP-dihydrofinasteride, a potent bisubstrate analog inhibitor
-
H.G. Bull, and et al. Mechanism-based inhibition of human steroid 5α-reductase by finasteride: enzyme-catalyzed formation of NADP-dihydrofinasteride, a potent bisubstrate analog inhibitor J. Am. Chem. Soc. 118 1996 2359 2365
-
(1996)
J. Am. Chem. Soc.
, vol.118
, pp. 2359-2365
-
-
Bull, H.G.1
-
75
-
-
38949191974
-
Challenges in modern drug discovery: A case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection
-
F.G. Njoroge, and et al. Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection Acc. Chem. Res. 41 2007 50 59
-
(2007)
Acc. Chem. Res.
, vol.41
, pp. 50-59
-
-
Njoroge, F.G.1
-
76
-
-
33749834648
-
DPP-4 inhibitors and their potential role in the management of type 2 diabetes
-
A. Barnett DPP-4 inhibitors and their potential role in the management of type 2 diabetes Int. J. Clin. Pract. 60 2006 1454 1470
-
(2006)
Int. J. Clin. Pract.
, vol.60
, pp. 1454-1470
-
-
Barnett, A.1
-
77
-
-
80051471238
-
Cathepsin K: Its skeletal actions and role as a therapeutic target in osteoporosis
-
A.G. Costa, and et al. Cathepsin K: its skeletal actions and role as a therapeutic target in osteoporosis Nat. Rev. Rheumatol. 7 2011 447 456
-
(2011)
Nat. Rev. Rheumatol.
, vol.7
, pp. 447-456
-
-
Costa, A.G.1
-
78
-
-
38749144762
-
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K
-
J.Y. Gauthier, and et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K Bioorg. Med. Chem. Lett. 18 2008 923 928
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 923-928
-
-
Gauthier, J.Y.1
-
79
-
-
17144423926
-
Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: Implications for a molecular mechanism of action
-
R.D. Couch, and et al. Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action Biorg. Med. Chem. Lett. 15 2005 2215 2219
-
(2005)
Biorg. Med. Chem. Lett.
, vol.15
, pp. 2215-2219
-
-
Couch, R.D.1
-
80
-
-
79953332009
-
Reversible covalent binding of neratinib to human serum albumin in vitro
-
A. Chandrasekaran, and et al. Reversible covalent binding of neratinib to human serum albumin in vitro Drug Metab. Lett. 4 2010 220 227
-
(2010)
Drug Metab. Lett.
, vol.4
, pp. 220-227
-
-
Chandrasekaran, A.1
-
81
-
-
84859845948
-
Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles
-
I.M. Serafimova, and et al. Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles Nat. Chem. Biol. 8 2012 471 476
-
(2012)
Nat. Chem. Biol.
, vol.8
, pp. 471-476
-
-
Serafimova, I.M.1
-
82
-
-
84871342809
-
Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion
-
R.A. Bauer, and et al. Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion Nat. Chem. Biol. 9 2013 21 29
-
(2013)
Nat. Chem. Biol.
, vol.9
, pp. 21-29
-
-
Bauer, R.A.1
-
83
-
-
66149104042
-
In vitro screening of 50 highly prescribed drugs for thiol adduct formation. Comparison of potential for drug-induced toxicity and extent of adduct formation
-
J. Gan, and et al. In vitro screening of 50 highly prescribed drugs for thiol adduct formation. Comparison of potential for drug-induced toxicity and extent of adduct formation Chem. Res. Toxicol. 22 2009 690 698
-
(2009)
Chem. Res. Toxicol.
, vol.22
, pp. 690-698
-
-
Gan, J.1
-
84
-
-
80053004364
-
Structural alert/reactive metabolite concept as applied in Medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: A perspective based on the critical examination of trends in the top 200 drugs marketed in the United States
-
A.F. Stepan, and et al. Structural alert/reactive metabolite concept as applied in Medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical examination of trends in the top 200 drugs marketed in the United States Chem. Res. Toxicol. 24 2011 1345 1410
-
(2011)
Chem. Res. Toxicol.
, vol.24
, pp. 1345-1410
-
-
Stepan, A.F.1
-
85
-
-
45549108466
-
Disparate proteome reactivity profiles of carbon electrophiles
-
E. Weerapana, and et al. Disparate proteome reactivity profiles of carbon electrophiles Nat. Chem. Biol. 4 2008 405 407
-
(2008)
Nat. Chem. Biol.
, vol.4
, pp. 405-407
-
-
Weerapana, E.1
-
86
-
-
84902438455
-
A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases
-
S.G. Kathman, and et al. A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases J. Med. Chem. 57 2014 4969 4974
-
(2014)
J. Med. Chem.
, vol.57
, pp. 4969-4974
-
-
Kathman, S.G.1
-
87
-
-
84907478550
-
Promiscuity and selectivity in covalent enzyme inhibition: A systematic study of electrophilic fragments
-
C. Jöst, and et al. Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments J. Med. Chem. 57 2014 7590 7599
-
(2014)
J. Med. Chem.
, vol.57
, pp. 7590-7599
-
-
Jöst, C.1
-
88
-
-
84870260588
-
Kinetic template-guided tethering of fragments
-
R.H. Mann, and et al. Kinetic template-guided tethering of fragments ChemMedChem 2012 2012 2082 2086
-
(2012)
ChemMedChem
, vol.2012
, pp. 2082-2086
-
-
Mann, R.H.1
-
89
-
-
84876016325
-
Electrophilic fragment-based design of reversible covalent kinase inhibitors
-
R.M. Miller, and et al. Electrophilic fragment-based design of reversible covalent kinase inhibitors J. Am. Chem. Soc. 135 2013 5298 5301
-
(2013)
J. Am. Chem. Soc.
, vol.135
, pp. 5298-5301
-
-
Miller, R.M.1
-
90
-
-
77249138804
-
Active site remodeling accompanies thioester bond formation in the SUMO E1
-
S.K. Olsen, and et al. Active site remodeling accompanies thioester bond formation in the SUMO E1 Nature 463 2010 906 914
-
(2010)
Nature
, vol.463
, pp. 906-914
-
-
Olsen, S.K.1
|