| Rank |
Title |
Journal |
Year |
PubWeight™‹?› |
|
1
|
Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.
|
Antimicrob Agents Chemother
|
2003
|
3.23
|
|
2
|
High resolution crystal structures of HIV-1 protease with a potent non-peptide inhibitor (UIC-94017) active against multi-drug-resistant clinical strains.
|
J Mol Biol
|
2004
|
2.21
|
|
3
|
A potent human immunodeficiency virus type 1 protease inhibitor, UIC-94003 (TMC-126), and selection of a novel (A28S) mutation in the protease active site.
|
J Virol
|
2002
|
2.02
|
|
4
|
Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.
|
J Biol Chem
|
2007
|
1.79
|
|
5
|
Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M.
|
J Med Chem
|
2006
|
1.69
|
|
6
|
Ultra-high resolution crystal structure of HIV-1 protease mutant reveals two binding sites for clinical inhibitor TMC114.
|
J Mol Biol
|
2006
|
1.66
|
|
7
|
Deubiquitinating and interferon antagonism activities of coronavirus papain-like proteases.
|
J Virol
|
2010
|
1.64
|
|
8
|
The microtubule stabilizing agent laulimalide does not bind in the taxoid site, kills cells resistant to paclitaxel and epothilones, and may not require its epoxide moiety for activity.
|
Biochemistry
|
2002
|
1.45
|
|
9
|
A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication.
|
Proc Natl Acad Sci U S A
|
2008
|
1.39
|
|
10
|
Altered HIV-1 Gag protein interactions with cyclophilin A (CypA) on the acquisition of H219Q and H219P substitutions in the CypA binding loop.
|
J Biol Chem
|
2005
|
1.38
|
|
11
|
Synergistic effects of peloruside A and laulimalide with taxoid site drugs, but not with each other, on tubulin assembly.
|
Mol Pharmacol
|
2006
|
1.36
|
|
12
|
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
|
Antimicrob Agents Chemother
|
2007
|
1.34
|
|
13
|
Beta-secretase inhibitor GRL-8234 rescues age-related cognitive decline in APP transgenic mice.
|
FASEB J
|
2010
|
1.29
|
|
14
|
Atomic resolution crystal structures of HIV-1 protease and mutants V82A and I84V with saquinavir.
|
Proteins
|
2007
|
1.28
|
|
15
|
Fluoro-Julia olefination as a mild, high-yielding route to alpha-fluoro acrylonitriles.
|
J Org Chem
|
2008
|
1.27
|
|
16
|
In vitro selection of highly darunavir-resistant and replication-competent HIV-1 variants by using a mixture of clinical HIV-1 isolates resistant to multiple conventional protease inhibitors.
|
J Virol
|
2010
|
1.24
|
|
17
|
In vivo inhibition of Abeta production by memapsin 2 (beta-secretase) inhibitors.
|
J Neurochem
|
2004
|
1.23
|
|
18
|
Laulimalide and paclitaxel: a comparison of their effects on tubulin assembly and their synergistic action when present simultaneously.
|
Mol Pharmacol
|
2004
|
1.22
|
|
19
|
(-)-Doliculide, a new macrocyclic depsipeptide enhancer of actin assembly.
|
J Biol Chem
|
2002
|
1.20
|
|
20
|
Development of protease inhibitors and the fight with drug-resistant HIV-1 variants.
|
Adv Pharmacol
|
2008
|
1.16
|
|
21
|
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.
|
J Med Chem
|
2007
|
1.12
|
|
22
|
Specificity of memapsin 1 and its implications on the design of memapsin 2 (beta-secretase) inhibitor selectivity.
|
Biochemistry
|
2002
|
1.11
|
|
23
|
The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors.
|
Curr Top Med Chem
|
2013
|
1.11
|
|
24
|
Effect of flap mutations on structure of HIV-1 protease and inhibition by saquinavir and darunavir.
|
J Mol Biol
|
2008
|
1.09
|
|
25
|
A non-antibacterial oxazolidinone derivative that inhibits epithelial cell sheet migration.
|
Chembiochem
|
2002
|
1.08
|
|
26
|
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
|
Antimicrob Agents Chemother
|
2008
|
1.05
|
|
27
|
Crystal structure of memapsin 2 (beta-secretase) in complex with an inhibitor OM00-3.
|
Biochemistry
|
2002
|
1.04
|
|
28
|
Julia Olefination as a General Route to Phenyl (alpha-Fluoro)vinyl Sulfones.
|
Synlett
|
2008
|
1.03
|
|
29
|
Structural locations and functional roles of new subsites S5, S6, and S7 in memapsin 2 (beta-secretase).
|
Biochemistry
|
2005
|
1.03
|
|
30
|
Joint X-ray/neutron crystallographic study of HIV-1 protease with clinical inhibitor amprenavir: insights for drug design.
|
J Med Chem
|
2013
|
0.99
|
|
31
|
Coherence between cellular responses and in vitro splicing inhibition for the anti-tumor drug pladienolide B and its analogs.
|
J Biol Chem
|
2013
|
0.97
|
|
32
|
Novel P2 tris-tetrahydrofuran group in antiviral compound 1 (GRL-0519) fills the S2 binding pocket of selected mutants of HIV-1 protease.
|
J Med Chem
|
2013
|
0.96
|
|
33
|
Peloruside B, a potent antitumor macrolide from the New Zealand marine sponge Mycale hentscheli: isolation, structure, total synthesis, and bioactivity.
|
J Org Chem
|
2010
|
0.96
|
|
34
|
GRL-0519, a novel oxatricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor (PI), potently suppresses replication of a wide spectrum of multi-PI-resistant HIV-1 variants in vitro.
|
Antimicrob Agents Chemother
|
2013
|
0.96
|
|
35
|
Structural evidence for effectiveness of darunavir and two related antiviral inhibitors against HIV-2 protease.
|
J Mol Biol
|
2008
|
0.95
|
|
36
|
A mouse model for Betacoronavirus subgroup 2c using a bat coronavirus strain HKU5 variant.
|
MBio
|
2014
|
0.95
|
|
37
|
P-glycoprotein mediates efflux transport of darunavir in human intestinal Caco-2 and ABCB1 gene-transfected renal LLC-PK1 cell lines.
|
Biol Pharm Bull
|
2009
|
0.93
|
|
38
|
Novel HIV-1 protease inhibitors (PIs) containing a bicyclic P2 functional moiety, tetrahydropyrano-tetrahydrofuran, that are potent against multi-PI-resistant HIV-1 variants.
|
Antimicrob Agents Chemother
|
2011
|
0.91
|
|
39
|
Critical differences in HIV-1 and HIV-2 protease specificity for clinical inhibitors.
|
Protein Sci
|
2012
|
0.91
|
|
40
|
Loss of protease dimerization inhibition activity of darunavir is associated with the acquisition of resistance to darunavir by HIV-1.
|
J Virol
|
2011
|
0.90
|
|
41
|
Selective inhibition of the West Nile virus methyltransferase by nucleoside analogs.
|
Antiviral Res
|
2012
|
0.90
|
|
42
|
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
|
J Med Chem
|
2008
|
0.90
|
|
43
|
S-adenosyl-homocysteine is a weakly bound inhibitor for a flaviviral methyltransferase.
|
PLoS One
|
2013
|
0.87
|
|
44
|
The assembly-inducing laulimalide/peloruside a binding site on tubulin: molecular modeling and biochemical studies with [³H]peloruside A.
|
J Chem Inf Model
|
2010
|
0.87
|
|
45
|
Lasonolide A, a potent and reversible inducer of chromosome condensation.
|
Cell Cycle
|
2012
|
0.87
|
|
46
|
GRL-04810 and GRL-05010, difluoride-containing nonpeptidic HIV-1 protease inhibitors (PIs) that inhibit the replication of multi-PI-resistant HIV-1 in vitro and possess favorable lipophilicity that may allow blood-brain barrier penetration.
|
Antimicrob Agents Chemother
|
2013
|
0.86
|
|
47
|
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
|
Antimicrob Agents Chemother
|
2010
|
0.85
|
|
48
|
Candida albicans secreted aspartic proteases 4-6 induce apoptosis of epithelial cells by a novel Trojan horse mechanism.
|
FASEB J
|
2013
|
0.85
|
|
49
|
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
|
J Med Chem
|
2013
|
0.85
|
|
50
|
Synergistic inhibitor binding to the papain-like protease of human SARS coronavirus: mechanistic and inhibitor design implications.
|
ChemMedChem
|
2013
|
0.82
|
|
51
|
Expedient synthesis of α-substituted fluoroethenes.
|
Org Biomol Chem
|
2012
|
0.82
|
|
52
|
P2' benzene carboxylic acid moiety is associated with decrease in cellular uptake: evaluation of novel nonpeptidic HIV-1 protease inhibitors containing P2 bis-tetrahydrofuran moiety.
|
Antimicrob Agents Chemother
|
2013
|
0.82
|
|
53
|
Effects of CC chemokine receptor 5 (CCR5) inhibitors on the dynamics of CCR5 and CC-chemokine-CCR5 interactions.
|
Antivir Ther
|
2010
|
0.81
|
|
54
|
Prediction of potency of protease inhibitors using free energy simulations with polarizable quantum mechanics-based ligand charges and a hybrid water model.
|
J Chem Inf Model
|
2009
|
0.81
|
|
55
|
Conformations of laulimalide in DMSO-d6.
|
J Am Chem Soc
|
2005
|
0.81
|
|
56
|
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring.
|
J Med Chem
|
2012
|
0.80
|
|
57
|
Inhibition of anthrax lethal factor: lability of hydroxamate as a chelating group.
|
Appl Microbiol Biotechnol
|
2012
|
0.80
|
|
58
|
Metabolism-directed structure optimization of benzimidazole-based Francisella tularensis enoyl-reductase (FabI) inhibitors.
|
Xenobiotica
|
2013
|
0.76
|
|
59
|
Study of memapsin 2 (beta-secretase) and strategy of inhibitor design.
|
J Mol Neurosci
|
2003
|
0.76
|
|
60
|
Memapsin 2, a drug target for Alzheimer's disease.
|
Biochem Soc Symp
|
2003
|
0.75
|
|
61
|
Correction to Enantioselective Total Synthesis of (+)-Amphirionin-4.
|
Org Lett
|
2016
|
0.75
|