-
1
-
-
78649254350
-
Grand challenge commentary: Accessing new chemical space for 'undruggable' targets
-
Dandapani, S. & Marcaurelle, L. A. Grand challenge commentary: accessing new chemical space for 'undruggable' targets. Nat. Chem. Biol. 6, 861-863 (2010).
-
(2010)
Nat. Chem. Biol.
, vol.6
, pp. 861-863
-
-
Dandapani, S.1
Marcaurelle, L.A.2
-
3
-
-
79960503652
-
Chemical genetics
-
O'Connor, C. J., Laraia, L. & Spring, D. R. Chemical genetics. Chem. Soc. Rev. 40, 4332-4345 (2011).
-
(2011)
Chem. Soc. Rev.
, vol.40
, pp. 4332-4345
-
-
O'Connor, C.J.1
Laraia, L.2
Spring, D.R.3
-
4
-
-
0034678033
-
Target-oriented and diversity-oriented organic synthesis in drug discovery
-
Schreiber, S. L. Target-oriented and diversity-oriented organic synthesis in drug discovery. Science 287, 1964-1969 (2000).
-
(2000)
Science
, vol.287
, pp. 1964-1969
-
-
Schreiber, S.L.1
-
5
-
-
58149358949
-
Organic chemistry: Molecular diversity by design
-
Schreiber, S. L. Organic chemistry: molecular diversity by design. Nature 457, 153-154 (2009).
-
(2009)
Nature
, vol.457
, pp. 153-154
-
-
Schreiber, S.L.1
-
6
-
-
84880296641
-
Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules
-
Galloway, W. R. J. D., Isidro-Llobet, A. & Spring, D. R. Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules. Nat. Commun. 1, 80-86 (2010).
-
(2010)
Nat. Commun.
, vol.1
, pp. 80-86
-
-
Galloway, W.R.J.D.1
Isidro-Llobet, A.2
Spring, D.R.3
-
7
-
-
84858704374
-
A diversity-oriented synthesis approach to macrocycles via oxidative ring expansion
-
Kopp, F., Stratton, C. F., Akella, L. B. & Tan, D. S. A diversity-oriented synthesis approach to macrocycles via oxidative ring expansion. Nat. Chem. Biol. 8, 358-365 (2012).
-
(2012)
Nat. Chem. Biol.
, vol.8
, pp. 358-365
-
-
Kopp, F.1
Stratton, C.F.2
Akella, L.B.3
Tan, D.S.4
-
8
-
-
84884837727
-
A strategy for the diversity-oriented synthesis of macrocyclic scaffolds using multidimensional coupling
-
Beckmann, H. S. et al. A strategy for the diversity-oriented synthesis of macrocyclic scaffolds using multidimensional coupling. Nat. Chem. 5, 861-867 (2013).
-
(2013)
Nat. Chem.
, vol.5
, pp. 861-867
-
-
Beckmann, H.S.1
-
9
-
-
84875466221
-
A ring-distortion strategy to construct stereochemically complex and structurally diverse compounds from natural products
-
Huigens, R. W. III et al. A ring-distortion strategy to construct stereochemically complex and structurally diverse compounds from natural products. Nat. Chem. 5, 195-202 (2013).
-
(2013)
Nat. Chem.
, vol.5
, pp. 195-202
-
-
Huigens, R.W.1
-
10
-
-
84890895066
-
Biogenetically inspired synthesis and skeletal diversification of indole alkaloids
-
Mizoguchi, H., Oikawa, H. & Oguri, H. Biogenetically inspired synthesis and skeletal diversification of indole alkaloids. Nat. Chem. 6, 57-64 (2014).
-
(2014)
Nat. Chem.
, vol.6
, pp. 57-64
-
-
Mizoguchi, H.1
Oikawa, H.2
Oguri, H.3
-
11
-
-
84905489992
-
Diversity-oriented synthesis of Lycopodium alkaloids inspired by the hidden functional group pairing pattern
-
Zhang, J. et al. Diversity-oriented synthesis of Lycopodium alkaloids inspired by the hidden functional group pairing pattern. Nat. Commun. 5, 4614-4622 (2014).
-
(2014)
Nat. Commun.
, vol.5
, pp. 4614-4622
-
-
Zhang, J.1
-
12
-
-
84900401394
-
Development of a natural-product-derived chemical toolbox for modulation of protein function
-
Rizzo, S. & Waldmann, H. Development of a natural-product-derived chemical toolbox for modulation of protein function. Chem. Rev. 114, 4621-4639 (2014).
-
(2014)
Chem. Rev.
, vol.114
, pp. 4621-4639
-
-
Rizzo, S.1
Waldmann, H.2
-
13
-
-
84900412775
-
Diversity-oriented synthesis as a tool for identifying new modulators of mitosis
-
Ibbeson, B. M. et al. Diversity-oriented synthesis as a tool for identifying new modulators of mitosis. Nat. Commun. 5, 3155-3162 (2014).
-
(2014)
Nat. Commun.
, vol.5
, pp. 3155-3162
-
-
Ibbeson, B.M.1
-
14
-
-
84925061498
-
De novo branching cascades for structural and functional diversity in small molecules
-
Garcia-Carstro, M. et al. De novo branching cascades for structural and functional diversity in small molecules. Nat. Commun. 6, 6516-6528 (2015).
-
(2015)
Nat. Commun.
, vol.6
, pp. 6516-6528
-
-
Garcia-Carstro, M.1
-
15
-
-
82255170673
-
A design strategy for drug-like polyheterocycles with privileged substructures for discovery of specific small-molecule modulators
-
Oh, S. & Park, S. B. A design strategy for drug-like polyheterocycles with privileged substructures for discovery of specific small-molecule modulators. Chem. Commun. 47, 12754-12761 (2011).
-
(2011)
Chem. Commun.
, vol.47
, pp. 12754-12761
-
-
Oh, S.1
Park, S.B.2
-
16
-
-
84887947768
-
Privileged substructure-based diversityoriented synthesis pathway for diverse pyrimidine-embedded polyheterocycles
-
Kim, H., Tung, T. T. & Park, S. B. Privileged substructure-based diversityoriented synthesis pathway for diverse pyrimidine-embedded polyheterocycles. Org. Lett. 15, 5814-5817 (2013).
-
(2013)
Org. Lett.
, vol.15
, pp. 5814-5817
-
-
Kim, H.1
Tung, T.T.2
Park, S.B.3
-
17
-
-
84908431043
-
Privileged structures: Efficient chemical 'navigators' toward unexplored biologically relevant chemical spaces
-
Kim, J., Kim, H. & Park, S. B. Privileged structures: efficient chemical 'navigators' toward unexplored biologically relevant chemical spaces. J. Am. Chem. Soc. 136, 14629-14638 (2014).
-
(2014)
J. Am. Chem. Soc.
, vol.136
, pp. 14629-14638
-
-
Kim, J.1
Kim, H.2
Park, S.B.3
-
18
-
-
84861486811
-
Discovery and target identification of an antiproliferative agent in live cells using fluorescence difference in two-dimensional gel electrophoresis
-
Park, J., Oh, S. & Park, S. B. Discovery and target identification of an antiproliferative agent in live cells using fluorescence difference in two-dimensional gel electrophoresis. Angew Chem. Int. Ed. Engl. 51, 5447-5451 (2012).
-
(2012)
Angew Chem. Int. Ed. Engl.
, vol.51
, pp. 5447-5451
-
-
Park, J.1
Oh, S.2
Park, S.B.3
-
19
-
-
84922479862
-
A small molecule binding HMGB1 and HMGB2 inhibits microgliamediated neuroinflammation
-
Lee, S. et al. A small molecule binding HMGB1 and HMGB2 inhibits microgliamediated neuroinflammation. Nat. Chem. Biol. 10, 1055-1060 (2014).
-
(2014)
Nat. Chem. Biol.
, vol.10
, pp. 1055-1060
-
-
Lee, S.1
-
20
-
-
0037109014
-
ZD1839 (Iressa): An orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy
-
Wakeling, A. E. et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 62, 5749-5754 (2002).
-
(2002)
Cancer Res.
, vol.62
, pp. 5749-5754
-
-
Wakeling, A.E.1
-
21
-
-
27844464469
-
Characterization of the first potent and selective PDE9 inhibitor using a cGMP reporter cell line
-
Wunder, F. et al. Characterization of the first potent and selective PDE9 inhibitor using a cGMP reporter cell line. Mol. Pharmacol. 68, 1775-1781 (2005).
-
(2005)
Mol. Pharmacol.
, vol.68
, pp. 1775-1781
-
-
Wunder, F.1
-
22
-
-
78751657692
-
Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists
-
Yaziji, V. et al. Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists. J. Med. Chem. 54, 457-471 (2011).
-
(2011)
J. Med. Chem.
, vol.54
, pp. 457-471
-
-
Yaziji, V.1
-
23
-
-
44949154279
-
Small molecular weight protein-protein interaction antagonists: An insurmountable challenge?
-
Domling, A. Small molecular weight protein-protein interaction antagonists: an insurmountable challenge? Curr. Opin. Chem. Biol. 12, 281-291 (2008).
-
(2008)
Curr. Opin. Chem. Biol.
, vol.12
, pp. 281-291
-
-
Domling, A.1
-
24
-
-
77953699074
-
Targeting the undruggable proteome: The small molecules of my dreams
-
Crews, C. M. Targeting the undruggable proteome: the small molecules of my dreams. Chem. Biol. 17, 551-555 (2010).
-
(2010)
Chem. Biol.
, vol.17
, pp. 551-555
-
-
Crews, C.M.1
-
25
-
-
80053567577
-
Tackling transcription factors: Challenges in antitumor therapy
-
Grivas, P. D., Kiaris, H. & Papavassiliou, A. G. Tackling transcription factors: challenges in antitumor therapy. Trends Mol. Med. 17, 537-538 (2011).
-
(2011)
Trends Mol. Med.
, vol.17
, pp. 537-538
-
-
Grivas, P.D.1
Kiaris, H.2
Papavassiliou, A.G.3
-
26
-
-
84920194283
-
Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals
-
Vitaku, E., Smith, D. T. & Njardarson, J. T. Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals. J. Med. Chem. 57, 10257-10274 (2014).
-
(2014)
J. Med. Chem.
, vol.57
, pp. 10257-10274
-
-
Vitaku, E.1
Smith, D.T.2
Njardarson, J.T.3
-
27
-
-
84901429774
-
Privileged diazepine compounds and their emergence as bromodomain inhibitors
-
Smith, S. G., Sanchez, R. & Zhou, M. M. Privileged diazepine compounds and their emergence as bromodomain inhibitors. Chem. Biol. 21, 573-583 (2014).
-
(2014)
Chem. Biol.
, vol.21
, pp. 573-583
-
-
Smith, S.G.1
Sanchez, R.2
Zhou, M.M.3
-
28
-
-
84862777407
-
Leucyl-tRNA synthetase is an intracellular leucine sensor for the mTORC1-signaling pathway
-
Han, J. M. et al. Leucyl-tRNA synthetase is an intracellular leucine sensor for the mTORC1-signaling pathway. Cell 149, 410-424 (2012).
-
(2012)
Cell
, vol.149
, pp. 410-424
-
-
Han, J.M.1
-
29
-
-
84899883725
-
Rhodium-catalyzed oxygenative [2+2] cycloaddition of terminal alkynes and imines for the synthesis of b-lactams
-
Kim, I., Roh, S. W., Lee, D. G. & Lee, C. Rhodium-catalyzed oxygenative [2+2] cycloaddition of terminal alkynes and imines for the synthesis of b-lactams. Org. Lett. 16, 2482-2485 (2014).
-
(2014)
Org. Lett.
, vol.16
, pp. 2482-2485
-
-
Kim, I.1
Roh, S.W.2
Lee, D.G.3
Lee, C.4
-
30
-
-
0027189691
-
[2,3] Sigmatropic rearrangement of 1-vinylic tetrahydroisoguinoline N-Yileds and N-Oxides
-
Bailey, T. S., Bremner, J. B. & Carver, J. A. [2,3] Sigmatropic rearrangement of 1-vinylic tetrahydroisoguinoline N-Yileds and N-Oxides. Tetrahedron Lett. 34, 3331-3334 (1993).
-
(1993)
Tetrahedron Lett.
, vol.34
, pp. 3331-3334
-
-
Bailey, T.S.1
Bremner, J.B.2
Carver, J.A.3
-
31
-
-
79953854409
-
3-catalyzed diastereoselective ring opening of bridged oxazolidines: Asymmetric synthesis of 2-azapodophyllotoxin
-
3-catalyzed diastereoselective ring opening of bridged oxazolidines: asymmetric synthesis of 2-azapodophyllotoxin. Chem. Eur. J. 17, 4905-4913 (2011).
-
(2011)
Chem. Eur. J.
, vol.17
, pp. 4905-4913
-
-
Srivastava, A.K.1
Koh, M.2
Park, S.B.3
-
32
-
-
11144272640
-
A free radical cyclization approach to indolo-benzodiazocine derivatives
-
Bremner, J. B. & Sengpracha, W. A free radical cyclization approach to indolo-benzodiazocine derivatives. Tetrahedron 61, 941-953 (2005).
-
(2005)
Tetrahedron
, vol.61
, pp. 941-953
-
-
Bremner, J.B.1
Sengpracha, W.2
-
33
-
-
84885488649
-
-
(eds Cossy, J., Arseniyadis, S. & Meyer, C.) (Wiley-VCH, Weinheim)
-
Blanchard, N. & Eustache, J. in Metathesis in Natural Product Synthesis (eds Cossy, J., Arseniyadis, S. & Meyer, C.) 1-43 (Wiley-VCH, Weinheim, 2010).
-
(2010)
Metathesis in Natural Product Synthesis
, pp. 1-43
-
-
Blanchard, N.1
Eustache, J.2
-
34
-
-
84919336040
-
Natural products with anti-Bredt and bridgehead double bonds
-
Mak, J. Y. W., Pouwer, R. H. & Williams, C. M. Natural products with anti-Bredt and bridgehead double bonds. Angew Chem. Int. Ed. Engl. 53, 13664-13688 (2014).
-
(2014)
Angew Chem. Int. Ed. Engl.
, vol.53
, pp. 13664-13688
-
-
Mak, J.Y.W.1
Pouwer, R.H.2
Williams, C.M.3
-
35
-
-
0032510318
-
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A designed, potent, orally active inhibitor of cholesterol absorption
-
Rosenblum, S. B. et al. Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption. J. Med. Chem. 41, 973-980 (1998).
-
(1998)
J. Med. Chem.
, vol.41
, pp. 973-980
-
-
Rosenblum, S.B.1
-
36
-
-
31444432605
-
The biosynthetic gene cluster for the beta-lactam antibiotic tabtoxin in Pseudomonas syringae
-
Kinscherf, T. G. & Willis, D. K. The biosynthetic gene cluster for the beta-lactam antibiotic tabtoxin in Pseudomonas syringae. J. Antibiot. 58, 817-821 (2005).
-
(2005)
J. Antibiot.
, vol.58
, pp. 817-821
-
-
Kinscherf, T.G.1
Willis, D.K.2
-
37
-
-
79955053789
-
An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles
-
Baumann, M. & Baxendale, I. R. An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles. Beilstein J. Org. Chem. 7, 442-495 (2011).
-
(2011)
Beilstein J. Org. Chem.
, vol.7
, pp. 442-495
-
-
Baumann, M.1
Baxendale, I.R.2
-
38
-
-
84871342809
-
Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion
-
Bauer, R. A., Wenderski, T. A. & Tan, D. S. Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion. Nat. Chem. Biol. 9, 21-29 (2013).
-
(2013)
Nat. Chem. Biol.
, vol.9
, pp. 21-29
-
-
Bauer, R.A.1
Wenderski, T.A.2
Tan, D.S.3
-
39
-
-
84859778293
-
MTOR signaling in growth control and disease
-
Laplante, M. & Sabatini, D. M. mTOR signaling in growth control and disease. Cell 149, 274-293 (2012).
-
(2012)
Cell
, vol.149
, pp. 274-293
-
-
Laplante, M.1
Sabatini, D.M.2
-
40
-
-
84922789990
-
Nutrient-sensing mechanisms and pathways
-
Efeyan, A., Comb, W. C. & Sabatini, D. M. Nutrient-sensing mechanisms and pathways. Nature 5179, 302-310 (2015).
-
(2015)
Nature
, vol.5179
, pp. 302-310
-
-
Efeyan, A.1
Comb, W.C.2
Sabatini, D.M.3
-
41
-
-
84859707963
-
Hijacking leucyl-tRNA synthetase for amino acid-dependent regulation of TORC1
-
Segev, N. & Hay, N. Hijacking leucyl-tRNA synthetase for amino acid-dependent regulation of TORC1. Mol. Cell 46, 4-6 (2012).
-
(2012)
Mol. Cell
, vol.46
, pp. 4-6
-
-
Segev, N.1
Hay, N.2
-
42
-
-
0034657687
-
The 2A crystal structure of leucyl-tRNA synthetase and its complex with a leucyl-adenylate analogue
-
Cusack, S., Yaremchuk, A. & Tukalo, M. The 2A crystal structure of leucyl-tRNA synthetase and its complex with a leucyl-adenylate analogue. EMBO J. 19, 2351-2361 (2000).
-
(2000)
EMBO J.
, vol.19
, pp. 2351-2361
-
-
Cusack, S.1
Yaremchuk, A.2
Tukalo, M.3
-
43
-
-
0345732640
-
MTOR controls cell cycle progression through its cell growth effectors S6K1 and 4E-BP1/eukaryotic translation initiation factor 4E
-
Fingar, D. C. et al. mTOR controls cell cycle progression through its cell growth effectors S6K1 and 4E-BP1/eukaryotic translation initiation factor 4E. Mol. Cell Biol. 24, 200-216 (2004).
-
(2004)
Mol. Cell Biol.
, vol.24
, pp. 200-216
-
-
Fingar, D.C.1
-
44
-
-
79551598347
-
AMPK and mTOR regulate autophagy through direct phosphorylation of Ulk1
-
Kim, J., Kundu, M., Viollet, B. & Guan, K. L. AMPK and mTOR regulate autophagy through direct phosphorylation of Ulk1. Nat. Cell Biol. 13, 132-141 (2011).
-
(2011)
Nat. Cell Biol.
, vol.13
, pp. 132-141
-
-
Kim, J.1
Kundu, M.2
Viollet, B.3
Guan, K.L.4
-
45
-
-
34548259958
-
P62/SQSTM1 binds directly to Atg8/LC3 to facilitate degradation of ubiquitinated protein aggregates by autophagy
-
Pankiv, S. et al. p62/SQSTM1 binds directly to Atg8/LC3 to facilitate degradation of ubiquitinated protein aggregates by autophagy. J. Biol. Chem. 282, 24131-24145 (2007).
-
(2007)
J. Biol. Chem.
, vol.282
, pp. 24131-24145
-
-
Pankiv, S.1
-
46
-
-
25444440875
-
The role of autophagy in cancer development and response to therapy
-
Kondo, Y., Kanzawa, T., Sawaya, R. & Kondo, S. The role of autophagy in cancer development and response to therapy. Nat. Rev. Cancer 5, 726-734 (2005).
-
(2005)
Nat. Rev. Cancer
, vol.5
, pp. 726-734
-
-
Kondo, Y.1
Kanzawa, T.2
Sawaya, R.3
Kondo, S.4
-
47
-
-
33947719279
-
Potential therapeutic applications of autophagy
-
Rubinsztein, D. C., Gestwicki, J. E., Murphy, L. O. & Klionsky, D. J. Potential therapeutic applications of autophagy. Nat. Rev. Drug Discov. 6, 304-312 (2007).
-
(2007)
Nat. Rev. Drug Discov.
, vol.6
, pp. 304-312
-
-
Rubinsztein, D.C.1
Gestwicki, J.E.2
Murphy, L.O.3
Klionsky, D.J.4
-
48
-
-
84928788868
-
Discovery of a small-molecule probe for V-ATPase function
-
Aldrich, L. N. et al. Discovery of a small-molecule probe for V-ATPase function. J. Am. Chem. Soc. 137, 5563-5568 (2015).
-
(2015)
J. Am. Chem. Soc.
, vol.137
, pp. 5563-5568
-
-
Aldrich, L.N.1
-
49
-
-
0000712790
-
The performance of the Becke-Lee-Yang-Parr (B-LYP) density functional theory with various basis sets
-
Gill, P. M. W., Johnson, B. G. & Pople, J. A. The performance of the Becke-Lee-Yang-Parr (B-LYP) density functional theory with various basis sets. Chem. Phys. Lett. 197, 499-505 (1992).
-
(1992)
Chem. Phys. Lett.
, vol.197
, pp. 499-505
-
-
Gill, P.M.W.1
Johnson, B.G.2
Pople, J.A.3
|