References
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98. Mahon AB, Arora PS (2012) End-capped α-helices as modulators of protein function. Drug
Discov Today: Technol 9:e57–e62
99. Cabezas E, Satterthwait AC (1999) The hydrogen bond mimic approach: solid-phase synthesis
of a peptide stabilized as an α-helix with a hydrazone link. J Am Chem Soc 121:3862–3875
100. Mahon AB, Arora PS (2012) Design, synthesis and protein-targeting properties of thioetherlinked hydrogen bond surrogate helices. Chem Commun 48:1416–1418
101. Chapman RN, Dimartino G, Arora PS (2004) A highly stable short α-helix constrained by a
main-chain hydrogen-bond surrogate. J Am Chem Soc 126:12252–12253
102. Kushal S, Lao BB, Henchey LK, Dubey R, Mesallati H, Traaseth NJ, Olenyuk BZ, Arora PS
(2013) Protein domain mimetics as in vivo modulators of hypoxia-inducible factor signaling.
Proc Natl Acad Sci 110:15602–15607
103. Henchey LK, Kushal S, Dubey R, Chapman RN, Olenyuk BZ, Arora PS (2010) Inhibition of
hypoxia inducible factor 1—transcription coactivator interaction by a hydrogen bond surrogate
α-helix. J Am Chem Soc 132:941–943
104. Henchey LK, Porter JR, Ghosh I, Arora PS (2010) High specificity in protein recognition by hydrogen-bond-surrogate α-helices: selective inhibition of the p53/mdm2 complex.
ChemBioChem 11:2104–2107
105. Patgiri A, Yadav KK, Arora PS, Bar-Sagi D (2011) An orthosteric inhibitor of the Ras-Sos
interaction. Nat Chem Biol 7:585–587
106. Hill TA, Shepherd NE, Diness F, Fairlie DP (2014) Constraining cyclic peptides to mimic
protein structure motifs. Angew Chem Int Edit 53:13020–13041
107. Walensky LD, Kung AL, Escher I, Malia TJ, Barbuto S, Wright RD, Wagner G, Verdine GL,
Korsmeyer SJ (2004) Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix.
Sci 305:1466–1470
108. Bernal F, Tyler AF, Korsmeyer SJ, Walensky LD, Verdine GL (2007) Reactivation of the p53
tumor suppressor pathway by a stapled p53 peptide. J Am Chem Soc 129:5298–5298
109. Moellering RE, Cornejo M, Davis TN, Del Bianco C, Aster JC, Blacklow SC, Kung AL,
Gilliland DG, Verdine GL, Bradner JE (2009) Direct inhibition of the NOTCH transcription
factor complex. Nat 462:152–187
110. Bird GH, Madani N, Perry AF, Princiotto AM, Supko JG, He X, Gavathiotis E, Sodroski JG,
Walensky LD (2010) Hydrocarbon double-stapling remedies the proteolytic instability of a
lengthy peptide therapeutic. Proc Natl Acad Sci 107:14093–14098
111. Phillips C, Roberts LR, Schade M, Bazin R, Bent A, Davies NL, Moore R, Pannifer AD,
Pickford AR, Prior SH, Read CM, Scott A, Brown DG, Xu B, Irving SL (2011) Design and
structure of stapled peptides binding to estrogen receptors. J Am Chem Soc 133:9696–9699
112. LaBelle JL, Katz SG, Bird GH, Gavathiotis E, Stewart ML, Lawrence C, Fisher JK, Godes
M, Pitter K, Kung AL, Walensky LD (2012) A stapled BIM peptide overcomes apoptotic
resistance in hematologic cancers. J Clin Invest 122:2018–2031
113. Brown CJ, Quah ST, Jong J, Goh AM, Chiam PC, Khoo KH, Choong ML, Lee MA, Yurlova L,
Zolghadr K, Joseph TL, Verma CS, Lane DP (2013) Stapled peptides with improved potency
and specificity that activate p53. ACS Chem Biol 8:506–512
114. Cui H-K, Zhao B, Li Y, Guo Y, Hu H, Liu L, Chen Y-G (2013) Design of stapled α-helical
peptides to specifically activate Wnt/β-catenin signaling. Cell Res 23:581–584
115. Giordanetto F, Revell JD, Knerr L, Hostettler M, Paunovic A, Priest C, Janefeldt A, Gill A
(2013) Stapled vasoactive intestinal peptide (VIP) derivatives improve VPAC(2) agonism and
glucose-dependent insulin secretion. ACS Med Chem Lett 4:1163–1168
116. Leshchiner ES, Braun CR, Bird GH, Walensky LD (2013) Direct activation of full-length
proapoptotic BAK. Proc Natl Acad Sci U S A 110:E986–E995
117. Long YQ, Huang SX, Zawahir Z, Xu ZL, Li HY, Sanchez TW, Zhi Y, De Houwer S, Christ F,
Debyser Z, Neamati N (2013) Design of cell-permeable stapled peptides as HIV-1 integrase
inhibitors. J Med Chem 56:5601–5612
118. Nomura W, Aikawa H, Ohashi N, Urano E, Metifiot M, Fujino M, Maddali K, Ozaki T, Nozue
A, Narumi T, Hashimoto C, Tanaka T, Pommier Y, Yamamoto N, Komano JA, Murakami T,
Tamamura H (2013) Cell-permeable stapled peptides based on HIV-1 integrase inhibitors
derived from HIV-1 gene products. ACS Chem Biol 8:2235–2244
23
98. Mahon AB, Arora PS (2012) End-capped α-helices as modulators of protein function. Drug
Discov Today: Technol 9:e57–e62
99. Cabezas E, Satterthwait AC (1999) The hydrogen bond mimic approach: solid-phase synthesis
of a peptide stabilized as an α-helix with a hydrazone link. J Am Chem Soc 121:3862–3875
100. Mahon AB, Arora PS (2012) Design, synthesis and protein-targeting properties of thioetherlinked hydrogen bond surrogate helices. Chem Commun 48:1416–1418
101. Chapman RN, Dimartino G, Arora PS (2004) A highly stable short α-helix constrained by a
main-chain hydrogen-bond surrogate. J Am Chem Soc 126:12252–12253
102. Kushal S, Lao BB, Henchey LK, Dubey R, Mesallati H, Traaseth NJ, Olenyuk BZ, Arora PS
(2013) Protein domain mimetics as in vivo modulators of hypoxia-inducible factor signaling.
Proc Natl Acad Sci 110:15602–15607
103. Henchey LK, Kushal S, Dubey R, Chapman RN, Olenyuk BZ, Arora PS (2010) Inhibition of
hypoxia inducible factor 1—transcription coactivator interaction by a hydrogen bond surrogate
α-helix. J Am Chem Soc 132:941–943
104. Henchey LK, Porter JR, Ghosh I, Arora PS (2010) High specificity in protein recognition by hydrogen-bond-surrogate α-helices: selective inhibition of the p53/mdm2 complex.
ChemBioChem 11:2104–2107
105. Patgiri A, Yadav KK, Arora PS, Bar-Sagi D (2011) An orthosteric inhibitor of the Ras-Sos
interaction. Nat Chem Biol 7:585–587
106. Hill TA, Shepherd NE, Diness F, Fairlie DP (2014) Constraining cyclic peptides to mimic
protein structure motifs. Angew Chem Int Edit 53:13020–13041
107. Walensky LD, Kung AL, Escher I, Malia TJ, Barbuto S, Wright RD, Wagner G, Verdine GL,
Korsmeyer SJ (2004) Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix.
Sci 305:1466–1470
108. Bernal F, Tyler AF, Korsmeyer SJ, Walensky LD, Verdine GL (2007) Reactivation of the p53
tumor suppressor pathway by a stapled p53 peptide. J Am Chem Soc 129:5298–5298
109. Moellering RE, Cornejo M, Davis TN, Del Bianco C, Aster JC, Blacklow SC, Kung AL,
Gilliland DG, Verdine GL, Bradner JE (2009) Direct inhibition of the NOTCH transcription
factor complex. Nat 462:152–187
110. Bird GH, Madani N, Perry AF, Princiotto AM, Supko JG, He X, Gavathiotis E, Sodroski JG,
Walensky LD (2010) Hydrocarbon double-stapling remedies the proteolytic instability of a
lengthy peptide therapeutic. Proc Natl Acad Sci 107:14093–14098
111. Phillips C, Roberts LR, Schade M, Bazin R, Bent A, Davies NL, Moore R, Pannifer AD,
Pickford AR, Prior SH, Read CM, Scott A, Brown DG, Xu B, Irving SL (2011) Design and
structure of stapled peptides binding to estrogen receptors. J Am Chem Soc 133:9696–9699
112. LaBelle JL, Katz SG, Bird GH, Gavathiotis E, Stewart ML, Lawrence C, Fisher JK, Godes
M, Pitter K, Kung AL, Walensky LD (2012) A stapled BIM peptide overcomes apoptotic
resistance in hematologic cancers. J Clin Invest 122:2018–2031
113. Brown CJ, Quah ST, Jong J, Goh AM, Chiam PC, Khoo KH, Choong ML, Lee MA, Yurlova L,
Zolghadr K, Joseph TL, Verma CS, Lane DP (2013) Stapled peptides with improved potency
and specificity that activate p53. ACS Chem Biol 8:506–512
114. Cui H-K, Zhao B, Li Y, Guo Y, Hu H, Liu L, Chen Y-G (2013) Design of stapled α-helical
peptides to specifically activate Wnt/β-catenin signaling. Cell Res 23:581–584
115. Giordanetto F, Revell JD, Knerr L, Hostettler M, Paunovic A, Priest C, Janefeldt A, Gill A
(2013) Stapled vasoactive intestinal peptide (VIP) derivatives improve VPAC(2) agonism and
glucose-dependent insulin secretion. ACS Med Chem Lett 4:1163–1168
116. Leshchiner ES, Braun CR, Bird GH, Walensky LD (2013) Direct activation of full-length
proapoptotic BAK. Proc Natl Acad Sci U S A 110:E986–E995
117. Long YQ, Huang SX, Zawahir Z, Xu ZL, Li HY, Sanchez TW, Zhi Y, De Houwer S, Christ F,
Debyser Z, Neamati N (2013) Design of cell-permeable stapled peptides as HIV-1 integrase
inhibitors. J Med Chem 56:5601–5612
118. Nomura W, Aikawa H, Ohashi N, Urano E, Metifiot M, Fujino M, Maddali K, Ozaki T, Nozue
A, Narumi T, Hashimoto C, Tanaka T, Pommier Y, Yamamoto N, Komano JA, Murakami T,
Tamamura H (2013) Cell-permeable stapled peptides based on HIV-1 integrase inhibitors
derived from HIV-1 gene products. ACS Chem Biol 8:2235–2244