-
1
-
-
84871394690
-
The Future of Peptide-Based Drugs
-
Craik, D. J.; Fairlie, D. P.; Liras, S.; Price, D. The Future of Peptide-Based Drugs Chem. Biol. Drug Des. 2013, 81, 136-147
-
(2013)
Chem. Biol. Drug Des.
, vol.81
, pp. 136-147
-
-
Craik, D.J.1
Fairlie, D.P.2
Liras, S.3
Price, D.4
-
2
-
-
0028657017
-
Enzymatic Barriers for GI Peptide and Protein Delivery
-
Woodley, J. F. Enzymatic Barriers for GI Peptide and Protein Delivery Crit. Rev. Ther. Drug Carrier Syst. 1994, 11, 61-95
-
(1994)
Crit. Rev. Ther. Drug Carrier Syst.
, vol.11
, pp. 61-95
-
-
Woodley, J.F.1
-
3
-
-
16244418685
-
Current Strategies Used to Enhance the Paracellular Transport of Therapeutic Polypeptides across the Intestinal Epithelium
-
Salamat-Miller, N.; Johnston, T. P. Current Strategies Used to Enhance the Paracellular Transport of Therapeutic Polypeptides across the Intestinal Epithelium Int. J. Pharm. 2005, 294, 201-216
-
(2005)
Int. J. Pharm.
, vol.294
, pp. 201-216
-
-
Salamat-Miller, N.1
Johnston, T.P.2
-
4
-
-
84875138812
-
Getting in Shape: Controlling Peptide Bioactivity and Bioavailability Using Conformational Constraints
-
Bock, J. E.; Gavenonis, J.; Kritzer, J. A. Getting in Shape: Controlling Peptide Bioactivity and Bioavailability Using Conformational Constraints ACS Chem. Biol. 2012, 8, 488-499
-
(2012)
ACS Chem. Biol.
, vol.8
, pp. 488-499
-
-
Bock, J.E.1
Gavenonis, J.2
Kritzer, J.A.3
-
5
-
-
57349171593
-
N-Methylation of Peptides: A New Perspective in Medicinal Chemistry
-
Chatterjee, J.; Gilon, C.; Hoffman, A.; Kessler, H. N-Methylation of Peptides: A New Perspective in Medicinal Chemistry Acc. Chem. Res. 2008, 41, 1331-1342
-
(2008)
Acc. Chem. Res.
, vol.41
, pp. 1331-1342
-
-
Chatterjee, J.1
Gilon, C.2
Hoffman, A.3
Kessler, H.4
-
6
-
-
37848999397
-
Effect of Structural and Conformation Modifications, Including Backbone Cyclization, of Hydrophilic Hexapeptides on Their Intestinal Permeability and Enzymatic Stability
-
Hess, S.; Ovadia, O.; Shalev, D. E.; Senderovich, H.; Qadri, B.; Yehezkel, T.; Salitra, Y.; Sheynis, T.; Jelinek, R.; Gilon, C.; Hoffman, A. Effect of Structural and Conformation Modifications, Including Backbone Cyclization, of Hydrophilic Hexapeptides on Their Intestinal Permeability and Enzymatic Stability J. Med. Chem. 2007, 50, 6201-6211
-
(2007)
J. Med. Chem.
, vol.50
, pp. 6201-6211
-
-
Hess, S.1
Ovadia, O.2
Shalev, D.E.3
Senderovich, H.4
Qadri, B.5
Yehezkel, T.6
Salitra, Y.7
Sheynis, T.8
Jelinek, R.9
Gilon, C.10
Hoffman, A.11
-
7
-
-
39749193898
-
Backbone Cyclic Peptidomimetic Melanocortin-4 Receptor Agonist as a Novel Orally Administrated Drug Lead for Treating Obesity
-
Hess, S.; Linde, Y.; Ovadia, O.; Safrai, E.; Shalev, D. E.; Swed, A.; Halbfinger, E.; Lapidot, T.; Winkler, I.; Gabinet, Y.; Faier, A.; Yarden, D.; Xiang, Z.; Portillo, F. P.; Haskell-Luevano, C.; Gilon, C.; Hoffman, A. Backbone Cyclic Peptidomimetic Melanocortin-4 Receptor Agonist as a Novel Orally Administrated Drug Lead for Treating Obesity J. Med. Chem. 2008, 51, 1026-1034
-
(2008)
J. Med. Chem.
, vol.51
, pp. 1026-1034
-
-
Hess, S.1
Linde, Y.2
Ovadia, O.3
Safrai, E.4
Shalev, D.E.5
Swed, A.6
Halbfinger, E.7
Lapidot, T.8
Winkler, I.9
Gabinet, Y.10
Faier, A.11
Yarden, D.12
Xiang, Z.13
Portillo, F.P.14
Haskell-Luevano, C.15
Gilon, C.16
Hoffman, A.17
-
8
-
-
33750482579
-
Conformational Flexibility, Internal Hydrogen Bonding, and Passive Membrane Permeability: Successful in Silico Prediction of the Relative Permeabilities of Cyclic Peptides
-
Rezai, T.; Bock, J. E.; Zhou, M. V.; Kalyanaraman, C.; Lokey, R. S.; Jacobson, M. P. Conformational Flexibility, Internal Hydrogen Bonding, and Passive Membrane Permeability: Successful in Silico Prediction of the Relative Permeabilities of Cyclic Peptides J. Am. Chem. Soc. 2006, 128, 14073-14080
-
(2006)
J. Am. Chem. Soc.
, vol.128
, pp. 14073-14080
-
-
Rezai, T.1
Bock, J.E.2
Zhou, M.V.3
Kalyanaraman, C.4
Lokey, R.S.5
Jacobson, M.P.6
-
9
-
-
33644644973
-
Testing the Conformational Hypothesis of Passive Membrane Permeability Using Synthetic Cyclic Peptide Diastereomers
-
Rezai, T.; Yu, B.; Millhauser, G.; Jacobson, M. P.; Lokey, R. S. Testing the Conformational Hypothesis of Passive Membrane Permeability Using Synthetic Cyclic Peptide Diastereomers J. Am. Chem. Soc. 2006, 128, 2510-2511
-
(2006)
J. Am. Chem. Soc.
, vol.128
, pp. 2510-2511
-
-
Rezai, T.1
Yu, B.2
Millhauser, G.3
Jacobson, M.P.4
Lokey, R.S.5
-
10
-
-
79960153981
-
Intramolecular Hydrogen Bonding to Improve Membrane Permeability and Absorption in beyond Rule of Five Chemical Space
-
Alex, A.; Millan, D. S.; Perez, M.; Wakenhut, F.; Whitlock, G. A. Intramolecular Hydrogen Bonding to Improve Membrane Permeability and Absorption in Beyond Rule of Five Chemical Space Med. Chem. Commun. 2011, 2, 669-674
-
(2011)
Med. Chem. Commun.
, vol.2
, pp. 669-674
-
-
Alex, A.1
Millan, D.S.2
Perez, M.3
Wakenhut, F.4
Whitlock, G.A.5
-
11
-
-
79953811147
-
The Effect of Multiple N-Methylation on Intestinal Permeability of Cyclic Hexapeptides
-
Ovadia, O.; Greenberg, S.; Chatterjee, J.; Laufer, B.; Opperer, F.; Kessler, H.; Gilon, C.; Hoffman, A. The Effect of Multiple N-Methylation on Intestinal Permeability of Cyclic Hexapeptides Mol. Pharm. 2011, 8, 479-487
-
(2011)
Mol. Pharm.
, vol.8
, pp. 479-487
-
-
Ovadia, O.1
Greenberg, S.2
Chatterjee, J.3
Laufer, B.4
Opperer, F.5
Kessler, H.6
Gilon, C.7
Hoffman, A.8
-
12
-
-
84864182405
-
Intestinal Permeability of Cyclic Peptides: Common Key Backbone Motifs Identified
-
Beck, J. G.; Chatterjee, J.; Laufer, B.; Kiran, M. U.; Frank, A. O.; Neubauer, S.; Ovadia, O.; Greenberg, S.; Gilon, C.; Hoffman, A.; Kessler, H. Intestinal Permeability of Cyclic Peptides: Common Key Backbone Motifs Identified J. Am. Chem. Soc. 2012, 134, 12125-12133
-
(2012)
J. Am. Chem. Soc.
, vol.134
, pp. 12125-12133
-
-
Beck, J.G.1
Chatterjee, J.2
Laufer, B.3
Kiran, M.U.4
Frank, A.O.5
Neubauer, S.6
Ovadia, O.7
Greenberg, S.8
Gilon, C.9
Hoffman, A.10
Kessler, H.11
-
13
-
-
41949086504
-
Improving Oral Bioavailability of Peptides by Multiple N-Methylation: Somatostatin Analogues
-
Biron, E.; Chatterjee, J.; Ovadia, O.; Langenegger, D.; Brueggen, J.; Hoyer, D.; Schmid, H. A.; Jelinek, R.; Gilon, C.; Hoffman, A.; Kessler, H. Improving Oral Bioavailability of Peptides by Multiple N-Methylation: Somatostatin Analogues Angew. Chem. 2008, 47, 2595-2599
-
(2008)
Angew. Chem.
, vol.47
, pp. 2595-2599
-
-
Biron, E.1
Chatterjee, J.2
Ovadia, O.3
Langenegger, D.4
Brueggen, J.5
Hoyer, D.6
Schmid, H.A.7
Jelinek, R.8
Gilon, C.9
Hoffman, A.10
Kessler, H.11
-
14
-
-
80054853098
-
On-Resin N-Methylation of Cyclic Peptides for Discovery of Orally Bioavailable Scaffolds
-
White, T. R.; Renzelman, C. M.; Rand, A. C.; Rezai, T.; McEwen, C. M.; Gelev, V. M.; Turner, R. A.; Linington, R. G.; Leung, S. S.; Kalgutkar, A. S.; Bauman, J. N.; Zhang, Y.; Liras, S.; Price, D. A.; Mathiowetz, A. M.; Jacobson, M. P.; Lokey, R. S. On-Resin N-Methylation of Cyclic Peptides for Discovery of Orally Bioavailable Scaffolds Nat. Chem. Biol. 2011, 7, 810-817
-
(2011)
Nat. Chem. Biol.
, vol.7
, pp. 810-817
-
-
White, T.R.1
Renzelman, C.M.2
Rand, A.C.3
Rezai, T.4
McEwen, C.M.5
Gelev, V.M.6
Turner, R.A.7
Linington, R.G.8
Leung, S.S.9
Kalgutkar, A.S.10
Bauman, J.N.11
Zhang, Y.12
Liras, S.13
Price, D.A.14
Mathiowetz, A.M.15
Jacobson, M.P.16
Lokey, R.S.17
-
15
-
-
0025311288
-
Epithelial Transport of Drugs in Cell Culture. I: A Model for Studying the Passive Diffusion of Drugs over Intestinal Absorbtive (Caco-2) Cells
-
Artursson, P. Epithelial Transport of Drugs in Cell Culture. I: A Model for Studying the Passive Diffusion of Drugs over Intestinal Absorbtive (Caco-2) Cells. J. Pharm. Sci. 1990, 79.
-
(1990)
J. Pharm. Sci.
, vol.79
-
-
Artursson, P.1
-
16
-
-
0025329248
-
Epithelial Transport of Drugs in Cell Culture. II: Effect of Extracellular Calcium Concentration on the Paracellular Transport of Drugs of Different Lipophilicities across Monolayers of Intestinal Epithelial (Caco-2) Cells
-
Artursson, P.; Magnusson, C. Epithelial Transport of Drugs in Cell Culture. II: Effect of Extracellular Calcium Concentration on the Paracellular Transport of Drugs of Different Lipophilicities across Monolayers of Intestinal Epithelial (Caco-2) Cells J. Pharm. Sci. 1990, 79, 595-600
-
(1990)
J. Pharm. Sci.
, vol.79
, pp. 595-600
-
-
Artursson, P.1
Magnusson, C.2
-
17
-
-
80053250836
-
Development of a New Permeability Assay Using Low-Efflux MDCKII Cells
-
Di, L.; Whitney-Pickett, C.; Umland, J. P.; Zhang, H.; Zhang, X.; Gebhard, D. F.; Lai, Y.; F, J. J., III; Davidson, R. E.; Smith, R.; Reyner, E. L.; Lee, C.; Feng, B.; Rotter, C.; Varma, M. V.; Kempshall, S.; Fenner, K.; El-kattan, A. F.; Liston, T. E.; Troutman, M. D. Development of a New Permeability Assay Using Low-Efflux MDCKII Cells J. Pharm. Sci. 2011, 100, 4974-4985
-
(2011)
J. Pharm. Sci.
, vol.100
, pp. 4974-4985
-
-
Di, L.1
Whitney-Pickett, C.2
Umland, J.P.3
Zhang, H.4
Zhang, X.5
Gebhard, D.F.6
Lai, Y.7
Lai, Y.F.J.J.8
Davidson, R.E.9
Smith, R.10
Reyner, E.L.11
Lee, C.12
Feng, B.13
Rotter, C.14
Varma, M.V.15
Kempshall, S.16
Fenner, K.17
El-Kattan, A.F.18
Liston, T.E.19
Troutman, M.D.20
more..
-
19
-
-
14144250264
-
Caco-2 Permeability of Weakly Basic Drugs Predicted with the Double-Sink PAMPA Pka(Flux) Method
-
Avdeef, A.; Artursson, P.; Neuhoff, S.; Lazorova, L.; Gråsjö, J.; Tavelin, S. Caco-2 Permeability of Weakly Basic Drugs Predicted with the Double-Sink PAMPA Pka(Flux) Method Eur. J. Pharm. Sci. 2005, 24, 333-349
-
(2005)
Eur. J. Pharm. Sci.
, vol.24
, pp. 333-349
-
-
Avdeef, A.1
Artursson, P.2
Neuhoff, S.3
Lazorova, L.4
Gråsjö, J.5
Tavelin, S.6
-
20
-
-
84862025745
-
Use of 3d Properties to Characterize beyond Rule-of-5 Property Space for Passive Permeation
-
Guimarães, C. R. W.; Mathiowetz, A. M.; Shalaeva, M.; Goetz, G.; Liras, S. Use of 3d Properties to Characterize Beyond Rule-of-5 Property Space for Passive Permeation J. Chem. Inf. Model. 2012, 52, 882-890
-
(2012)
J. Chem. Inf. Model.
, vol.52
, pp. 882-890
-
-
Guimarães, C.R.W.1
Mathiowetz, A.M.2
Shalaeva, M.3
Goetz, G.4
Liras, S.5
-
21
-
-
84898441883
-
High Throughput Method for the Indirect Detection of Intramolecular Hydrogen Bonding
-
Goetz, G. H.; Farrell, W.; Shalaeva, M.; Sciabola, S.; Anderson, D.; Yan, J.; Philippe, L.; Shapiro, M. J. High Throughput Method for the Indirect Detection of Intramolecular Hydrogen Bonding J. Med. Chem. 2014, 57, 2920-2929
-
(2014)
J. Med. Chem.
, vol.57
, pp. 2920-2929
-
-
Goetz, G.H.1
Farrell, W.2
Shalaeva, M.3
Sciabola, S.4
Anderson, D.5
Yan, J.6
Philippe, L.7
Shapiro, M.J.8
-
22
-
-
0034720879
-
Elogpoct: A Tool for Lipophilicity Determination in Drug Discovery
-
Lombardo, F.; Shalaeva, M. Y.; Tupper, K. A.; Gao, F.; Abraham, M. H. Elogpoct: A Tool for Lipophilicity Determination in Drug Discovery J. Med. Chem. 2000, 43, 2922-2928
-
(2000)
J. Med. Chem.
, vol.43
, pp. 2922-2928
-
-
Lombardo, F.1
Shalaeva, M.Y.2
Tupper, K.A.3
Gao, F.4
Abraham, M.H.5
-
23
-
-
0035913059
-
Elogdoct: A Tool for Lipophilicity Determination in Drug Discovery. 2. Basic and Neutral Compounds
-
Lombardo, F.; Shalaeva, M. Y.; Tupper, K. A.; Gao, F. Elogdoct: A Tool for Lipophilicity Determination in Drug Discovery. 2. Basic and Neutral Compounds J. Med. Chem. 2001, 44, 2490-2497
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2490-2497
-
-
Lombardo, F.1
Shalaeva, M.Y.2
Tupper, K.A.3
Gao, F.4
-
24
-
-
84876100008
-
Structure-Based Design, SAR Analysis and Antitumor Activity of PI3K/mTOR Dual Inhibitors from 4-Methyl-pyridopyrimidinone Series
-
Cheng, H.; Hoffman, J. E.; Le, P. T.; Pairish, M.; Kania, R.; Farrell, W.; Bagrodia, S.; Yuan, J.; Sun, S.; Zhang, E.; Xiang, C.; Dalvie, D.; Rahavendran, S. V. Structure-Based Design, SAR Analysis and Antitumor Activity of PI3K/mTOR Dual Inhibitors from 4-Methyl-pyridopyrimidinone Series Biorg. Med. Chem. Lett. 2013, 23, 2787-2792
-
(2013)
Biorg. Med. Chem. Lett.
, vol.23
, pp. 2787-2792
-
-
Cheng, H.1
Hoffman, J.E.2
Le, P.T.3
Pairish, M.4
Kania, R.5
Farrell, W.6
Bagrodia, S.7
Yuan, J.8
Sun, S.9
Zhang, E.10
Xiang, C.11
Dalvie, D.12
Rahavendran, S.V.13
-
25
-
-
84903818637
-
The Discovery of Potent NS5A Inhibitors with a Unique Resistance Profile-Part 2
-
Wakenhut, F.; Tran, T. D.; Pickford, C.; Shaw, S.; Westby, M.; Smith-Burchnell, C.; Watson, L.; Paradowski, M.; Milbank, Jared; Stonehouse, D.; Cheung, K.; Wybrow, R.; Daverio, F.; Crook, S.; Statham, K.; Leese, D.; Stead, D.; Adam, F.; Hay, D.; Roberts, L. R.; Chiva, J.-Y.; Nichols, C.; Blakemore, D. C.; Goetz, G. H.; Che, Y.; Gardner, I.; Dayal, S.; Pike, A.; Webster, R.; Pryde, D. C. The Discovery of Potent NS5A Inhibitors with a Unique Resistance Profile-Part 2 ChemMedChem 2014, 9, 1387-1396
-
(2014)
ChemMedChem
, vol.9
, pp. 1387-1396
-
-
Wakenhut, F.1
Tran, T.D.2
Pickford, C.3
Shaw, S.4
Westby, M.5
Smith-Burchnell, C.6
Watson, L.7
Paradowski, M.8
Milbank, J.9
Stonehouse, D.10
Cheung, K.11
Wybrow, R.12
Daverio, F.13
Crook, S.14
Statham, K.15
Leese, D.16
Stead, D.17
Adam, F.18
Hay, D.19
Roberts, L.R.20
Chiva, J.-Y.21
Nichols, C.22
Blakemore, D.C.23
Goetz, G.H.24
Che, Y.25
Gardner, I.26
Dayal, S.27
Pike, A.28
Webster, R.29
Pryde, D.C.30
more..
-
26
-
-
84867025688
-
Optimizing PK Properties of Cyclic Peptides: The Effect of Side Chain Substitutions on Permeability and Clearance
-
Rand A.C.. Leung S.S.F.; Eng H., Rotter C.J., Sharma R., Kalgutkar A.S., Zhang Y., Varma M.V., Farley K.A., Khunte B., Limberakis C., Price D.A., Liras S., Mathiowetz A.M., Jacobson M.P., Lokey R.S., Optimizing PK Properties of Cyclic Peptides: The Effect of Side Chain Substitutions on Permeability and Clearance, Med. Chem. Commun.,1282-1289, 2012, 3.
-
(2012)
Med. Chem. Commun.
, vol.3
, pp. 1282-1289
-
-
Rand, A.C.1
Leung, S.S.F.2
Eng, H.3
Rotter, C.J.4
Sharma, R.5
Kalgutkar, A.S.6
Zhang, Y.7
Varma, M.V.8
Farley, K.A.9
Khunte, B.10
Limberakis, C.11
Price, D.A.12
Liras, S.13
Mathiowetz, A.M.14
Jacobson, M.P.15
Lokey, R.S.16
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