Past Publications

80. Cyclic peptides with a distinct arginine-fork motif recognize the HIV trans-activation response RNA in vitro and in cells

Chavali† SS, Mali† SM, Jenkins JL, Bonn RMS, Saseendran Anitha A, Bennett RP, Smith HC, Fasan* R, Wedekind* JE (ǂ equal contribution)

J. Biol. Chem. 2021, 297 (6), 101390 PDF.

79.Comprehensive Structure-Activity Profiling of Micheliolide and its Targeted Proteome in Leukemia Cells via Probe-Guided Late-Stage C—H Functionalization

Alwaseem† H, Giovani† S, Crotti M, Welle K, Jordan CT, Ghaemmaghami S, Fasan* R

ACS Cent. Sci. 2021, 7 (5), 841–857 PDF.

78.Engineered and Artificial Metalloenzymes for Selective C–H Functionalization

Ren X, Fasan* R

Curr. Opin. Green Sustain. Chem. 2021, 31100494 PDF.

77.A Diverse Library of Chiral Cyclopropane Scaffolds via Chemoenzymatic Assembly and Diversification of Cyclopropyl Ketones

Nam D, Steck V, Potenzino R, Fasan* R

J. Am. Chem. Soc. 2021, 143 (5), 2221-2231 PDF.

76.Biocatalytic strategy for the highly stereoselective synthesis of CHF2-containing trisubstituted cyclopropanes

Carminati DM, Decaens J, Couve-Bonnaire S, Jubault* P, Fasan* R

Angew. Chem. Int. Ed. 2021, 60 (13), 7072-7076 PDF.

75.MOrPH-PhD: a Phage Display System for the Functional Selection of Genetically Encoded Macrocyclic Peptides

Gu Y, Iannuzzelli JA, Fasan* R

Methods Mol. Biol. 2021, vol. 2371 PDF.

74.Co-crystal structures of HIV TAR RNA bound to lab-evolved proteins show key roles for arginine relevant to the design of cyclic peptide TAR inhibitors

Chavali SS, Mali SM, Jenkins JL, Fasan R, Wedekind* JE

J. Biol. Chem. 2020, 295 (49), 16470-16486 PDF.

73.An enzymatic platform for the highly enantioselective and stereodivergent construction of cyclopropyl-d-lactones

Ren† X, Liu† N, Chandgude AL, Fasan* R

Angew. Chem. Int. Ed. 2020, 59 (48), 21634-21639 PDF.

72.Enantioselective Synthesis of Chiral Amines via Biocatalytic Carbene N—H Insertion

Steck V, Carminati DM, Johnson NR, Fasan* R

ACS Catal. 2020, 10, 10967−10977 PDF.

71.Strategies for the Expression and Characterization of Artificial Myoglobin-based Carbene Transferases

Carminati DM, Moore EJ, Fasan* R

Methods Enzymol. 2020, 644, 35-61 PDF.

70.Organic Solvent Stability and Long-term Storage of Myoglobin-based Carbene Transfer Biocatalysts

Pineda-Knauseder† AJ, Vargas† DA, Fasan* R

Biotechnol. Appl. Biochem. 2020, 67 (4), 516-526 PDF.

69.Expanded toolbox for directing the biosynthesis of macrocyclic peptides in bacterial cells

Iannuzzelli JA, Fasan* R

Chem. Sci. 2020, 11, 6202-6208 PDF.

68.Mechanism-Guided Design and Discovery of Efficient P450-Derived C—H Amination Biocatalysts

Steck† V, Kolev† JN, Ren X, Fasan* R

J. Am. Chem. Soc. 2020, 142, 10343-10357 PDF.

67.Synergistic catalysis in an artificial enzyme

Ren X, Fasan R

Nat. Chem. 2020, 3, 184–185 PDF.

66.C—H Amination via Nitrene Transfer Catalyzed by Mononuclear Non-Heme Iron-Dependent Enzymes

Vila† MA, Steck† V, Giordano SR, Carrera* I, Fasan* R

Chembiochem 2020, 21 (14), 1981-1987 PDF.

65.Blocking SHH/Patched interaction triggers tumor growth inhibition through Patched-induced apoptosis

Bissey AP, Mathot P, Guix C, Jasmin M, Goddard I, Costechareyre C, Gadot N, Delcros JG, Mali SM, Fasan R, Arrigo AP, Dante R, Ichim G, Mehlen P, Fombonne J

Cancer Res. 2020, 80 (10), 1970-1980 PDF.

64.MOrPH-PhD: an integrated phage display platform for the discovery of functional genetically-encoded peptide macrocycles

Owens AE, Iannuzzelli JA, Gu Y, Fasan* R

ACS Cent. Sci. 2020, 6 (3), 368-381 PDF.

63.Highly Stereoselective Synthesis of Fused Cyclopropane-γ-Lactams via Biocatalytic Iron-Catalyzed Intramolecular Cyclopropanation

Ren X, Chandgude AL, Fasan* R

ACS Catal. 2020, 10 (3), 2308-2313 PDF.

62.Structure of sonic hedgehog protein in complex with Zn(II) and Mg(II) reveals ion coordination plasticity relevant to peptide drug design

Bonn-Breach R, Gu Y, Jenkins J, Fasan R, Wedekind W

Acta Crystallogr. D 2019, D75, 969-979 PDF.

61.A continuing career in biocatalysis: Frances H. Arnold

Fasan* R, Kan* SBJ, Zhao* H

ACS Catal. 2019, 9 (11), 9775-9788 PDF.

60.Stereoselective cyclopropanation of electron-deficient olefins with a cofactor redesigned carbene transferase featuring radical reactivity

Carminati MD, Fasan* R

ACS Catal. 2019, 9 (10), 9683-9697 PDF.

59.Selective functionalization of aliphatic amines via myoglobin-catalyzed carbene N-H insertion

Steck V, Sreenilayam G, Fasan* R

Synlett 2020, 31 (3), 224-229 PDF.

58.Mechanistic investigation of biocatalytic heme carbenoid Si—H insertions

Khade RL, Chandgude AL, Fasan* R, Zhang* Y

ChemCatChem 2019, 11 (13), 3101-3108 PDF.

57.Biocatalytic strategy for highly diastereo- and enantioselective synthesis of 2,3-dihydrobenzofuran based tricyclic scaffolds

Vargas DA, Khade RL, Zhang* Y, Fasan* R

Angew. Chem. Int. Ed. 2019, 58 (30), 10148-10152 PDF.

56.Stereodivergent Intramolecular Cyclopropanation Enabled by Engineered Carbene Transferases

Chandgude AL, Ren X, Fasan* R

J. Am. Chem. Soc. 2019, 141 (23), 9145-9150 PDF.

55.Effect of proximal ligand substitutions on the carbene and nitrene transferase activity of myoglobin

Moore EJ, Fasan* R

Tetrahedron 2019, 75 (16), 2357-2363 PDF.

54.Origin of high stereocontrol in olefin cyclopropanation catalyzed by an engineered carbene transferase

Tinoco A, Wei Y, Bacik JP, Carminati DM, Moore EJ, Ando N, Zhang* Y, Fasan* R

ACS Catal. 2019, 9 (10), 1514−1524 PDF.

53.Highly diastereo- and enantioselective synthesis of nitrile-substituted cyclopropanes via myoglobin-mediated carbene transfer catalysis

Chandgude AL, Fasan* R

Angew. Chem. Int. Ed. 2018, 57 (48), 15852-15856 PDF.

52.Myoglobin-catalyzed C—H functionalization of unprotected indoles

Vargas D, Tinoco A, Tyagi V, Fasan* R

Angew. Chem. Int. Ed. 2018, 57 (31), 9911-9915 PDF.

51.Chemoselective Cyclopropanation over Carbene Y—H insertion Catalyzed by an Engineered Carbene Transferase

Moore E, Steck V, Bajaj P, Fasan* R

J. Org. Chem. 2018, 83 (14), 7480–7490 PDF.

50.Transcriptional coactivator PGC-1α contains a novel CBP80-binding motif that orchestrates efficient target gene expression

Cho H, Rambout X, Gleghorn ML, Nguyen PQT, Phipps CR, Miyoshi K, Myers JR, Kataoka N, Fasan R, Maquat* LE

Genes Dev. 2018, 32(7-8), 555-567 PDF.

49.Cyclopropanations via Heme Carbenes: Basic Mechanism and Effects of Carbene Substituent, Protein Axial Ligand, and Porphyrin Substitution

Wei Y, Tinoco A, Steck V, Fasan* R, Zhang* Y

J. Am. Chem. Soc. 2018, 140(5), 1649–1662 PDF.

48.Stabilization of the Reductase Domain in the Catalytically Self-Sufficient Cytochrome P450BM3 via Consensus-Guided Mutagenesis

Saab-Rincón* G, Alwaseem H, Guzmán-Luna V, Olvera L, Fasan R

ChemBioChem 2018, 19 (6), 622-632 PDF.

47.Anticancer activity profiling of parthenolide analogs generated via P450-mediated chemoenzymatic synthesis

Alwaseem H, Frisch BJ, Fasan* R

Bioorg. Med. Chem. 2018, 26, 1365–1373 PDF.

46.Enzyme stabilization via computationally guided protein stapling

Moore EJ, Zorine D, Hansen WA, Khare* SD, Fasan* R

Proc. Natl. Acad. Sci. U.S. 2017, 114 (47), 12472-12477 PDF.

45.Stereoselective olefin cyclopropanation under aerobic conditions with an artificial enzyme incorporating an iron-chlorin e6 cofactor

Sreenilayam G, Moore EJ, Steck V, Fasan* R

ACS Catal. 2017, 7, 7629-7633 PDF.

44.Design and Evolution of a Macrocyclic Peptide Inhibitor of the Sonic Hedgehog/Patched Protein-Protein Interaction

Owens AE, de Paola I, Hansen WA, Liu YW, Khare SD, Fasan* R

J. Am. Chem. Soc. 2017, 139 (36), 12559-12568 PDF.

43.Exploiting and engineering hemoproteins for abiological carbene and nitrene transfer reactions

Brandenberg OF, Fasan* R, Arnold* FH

Curr. Opin. Biotechnol. 2017, 47, 102-111 PDF.

42.Enzymatic Catalysis: New Functional twists for P450 enzymes

Fasan R

Nat. Chem. 2017, 9, 609–611 (invited commentary) PDF.

41.Metal substitution modulates the reactivity and extends the reaction scope of myoglobin carbene transfer catalysts

Sreenilayam G, Moore EJ, Steck V, Fasan* R

Adv. Synth. Catal. 2017, 359, 2076-2089 PDF.

40.Two-tier Screening Platform for Directed Evolution of Aminoacyl-tRNA Synthetases with Enhanced Stop Codon Suppression Efficiency

Owens AE, Grasso KT, Ziegler CA, Fasan* R

ChemBioChem 2017, 18 (12), 1109-1116 PDF.

39.Highly diastereo- and enantioselective synthesis of trifluoromethyl-substituted cyclopropanes via myoglobin-catalyzed transfer of tri-fluoromethylcarbene

Tinoco A, Steck V, Tyagi V, Fasan* R

J. Am. Chem. Soc. 2017, 139 (15), 5293–5296 PDF.

38.Gram-scale synthesis of chiral cyclopropane-containing drugs and drug precursors using engineered myoglobin catalysts with complementary stereoselectivity

Bajaj P, Sreenilayam G, Tyagi V, Fasan* R

Angew. Chem. Int. Ed. 2016, 55 (52), 16110–16114 PDF.

37.Biocatalytic synthesis of allylic and allenyl sulfides via a myoglobin-catalyzed Doyle-Kirmse reaction

Tyagi V, Sreenilayam G, Bajaj P, Tinoco A, Fasan* R

Angew. Chem. Int. Ed. 2016, 55 (43), 13562-13566 PDF.

36.Chemoenzymatic synthesis and antileukemic activity of novel C9- and C14-functionalized parthenolide analogs

Tyagi V, Alwaseem H, O’Dwyer KM, Ponder J, Li QY, Jordan CT, Fasan* R

Bioorg. Med. Chem. 2016, 24 (17), 3876-86 PDF.

35.Aldehyde and ketone synthesis via P450-catalyzed oxidative deamination of alkyl azides

Giovani S, Alwaseem H, Fasan* R

ChemCatChem 2016, 8 (16), 2609–2613 PDF.

34.Ribosomal Synthesis of Thioether-Bridged Bicyclic Peptides

Bionda N, Fasan* R

Methods Mol. Biol. 2017, 1495, 57-76 PDF.

33.Side-chain-to-tail cyclization of ribosomally derived peptides promoted by aryl and alkyl amino-functionalized unnatural amino acids

Frost JR, Wu Z, Lam YC, Owens AD, Fasan* R

Org. Biomol. Chem. 2016, 14, 5803-5812 PDF.

32.Myoglobin-catalyzed olefination of aldehydes

Tyagi V, Fasan* R

Angew. Chem. Int. Ed. 2016, 55 (7), 2512-2516 PDF.

31.Efficient conversion of primary azides to aldehydes catalyzed by active site variants of myoglobin

Giovani S, Singh R, Fasan* R

Chem. Sci. 2016, 7, 234-239 PDF.

30.Ribosomal synthesis of natural product-like bicyclic peptides in E. coli

Bionda N, Fasan* R

ChemBioChem 2015, 16 (14), 2011-2016 PDF.

29.Ribosomal Synthesis of Macrocyclic Peptides in Vitro and in Vivo Mediated by Genetically Encoded Amino-thiol Unnatural Amino Acids

Frost JR, Jacob NT, Papa LJ, Owens AE, Fasan* R

ACS Chem. Biol. 2015, 10 (8), 1805-1816 PDF.

28.Intermolecular carbene S-H insertion catalysed by engineered myoglobin-based catalysts

Tyagi V, Bonn RB, Fasan* R

Chem. Sci. 2015, 6, 2488-2494 PDF.

27.Synthesis of Macrocyclic Organo-Peptide Hybrids from Ribosomal Polypeptide Precursors via CuAAC-/hydrazide-mediated cyclization

Smith JM, Fasan* R

Methods Mol. Biol. 2015, 1248, 23-38 PDF.

26.Myoglobin-catalyzed intermolecular carbene N-H insertion with arylamine substrates

Sreenilayam G, Fasan* R

Chem. Commun. 2015, 51, 1532-1534 PDF.

25.Highly diastereo- and enantioselective olefin cyclopropanation via engineered myoglobin-based catalysts

Bordeaux M, Tyagi V, Fasan* R

Angew. Chem. Int. Ed. 2015, 54 (6), 1744-1748 PDF.

24.Enzymatic C(sp3)—H amination: P450-catalyzed conversion of carbonazidates into oxazolidinones

Singh R, Kolev JN, Sutera PA, Fasan* R

ACS Catal. 2015, 5, 1685–1691 PDF.

23.Bioinspired strategy for the ribosomal synthesis of thioether-bridged macrocyclic peptides in bacteria

Bionda N, Cryan A, Fasan* R

ACS Chem. Biol. 2014, 9 (9), 2008-2013 PDF.

22.Intramolecular C(sp3)—H amination of arylsulfonyl azides with engineered and artificial myoglobin-based catalysts

Bordeaux M, Singh R, Fasan* R

Bioorg. Med. Chem. 2014, 22 (20), 5697–5704 PDF.

21.Designer macrocyclic organo-peptide hybrids inhibit the interaction between p53 and HDM2/X by accommodating a functional α-helical motif

Smith JM, Frost JR, Fasan* R

Chem. Commun. 2014, 50, 5027-5030 PDF.

20.Enhancing the Efficiency and Regioselectivity of P450 Oxidation Catalysts via Unnatural Amino Acid Mutagenesis

Kolev JN, Zaengle JM, Ravikumar R, Fasan* R

ChemBioChem 2014, 15 (7), 1001–1010 PDF.

19.P450-catalyzed intramolecular sp3 C—H amination with arylsulfonyl azide substrates

Singh R, Bordeaux M, Fasan* R

ACS Catal. 2014, 4 (2), 546–552 PDF.

18.Synthesis of bicyclic organo-peptide hybrids via oxime/intein-mediated macrocyclization followed by disulfide bond formation

Smith JM, Hill NC, Krasniak PJ, Fasan* R

Org. Biomol. Chem. 2014, 12 (7), 1135-1142 PDF.

17.Discovery of potent parthenolide-based antileukemic agents enabled by late-stage P450-mediated C―H functionalization

Kolev JN, O’Dwyer KM, Jordan CT, Fasan* R

ACS Chem. Biol. 2014, 9 (1), 164-173 PDF.

16.Design, synthesis, and diversification of ribosomally derived peptide macrocycles

Frost JR, Smith JM, Fasan* R

Curr. Opin. Struct. Biol. 2013, 23 (4), 571-580 (invited review) PDF.

15.Emerging strategies to access peptide macrocycles from genetically encoded polypeptides

Smith JM, Frost JR, Fasan* R

J. Org. Chem. 2013, 78 (8), 3525–3531 (invited review) PDF.

14.Macrocyclization of organo-peptide hybrids via a dual bioorthogonal ligation; insights from structure-reactivity studies

Frost JR, Vitali F, Jacob NT, Brown MD, Fasan* R

ChemBioChem 2013, 14 (1), 147-160 PDF.

13.Controlled oxidation of remote sp3 C―H bonds in artemisinin via P450 catalysts with fine-tuned regio- and stereoselectivity

Zhang K, Shafer BM, Demars II MD, Stern HA, Fasan* R

J. Am. Chem. Soc. 2012, 134 (45), 18695–18704 PDF.

12.Tuning P450 Enzymes as Oxidation Catalysts

Fasan* R

ACS Catal. 2012, 2, 647-666 PDF.

11.Diverse organo-peptide macrocycles via a fast and catalyst-free oxime/intein-mediated dual ligation

Satyanarayana M, Vitali F, Frost JR, Fasan* R

Chem. Commun. 2012, 48, 1461-1463 PDF.

10.Modular assembly of macrocyclic organo-peptide hybrids (MOrPHs) from synthetic and genetically encoded precursors

Smith JM, Vitali F, Archer SA, Fasan* R

Angew. Chem. Int. Ed. 2011, 50 (22), 5075-5080 PDF.

9.P450 Fingerprinting Method for Rapid Discovery of Terpene Hydroxylating P450 Catalysts with Diversified Regioselectivity

Zhang K, El Damaty S, Fasan* R

J. Am. Chem. Soc. 2011, 13, (31), 03242-3245 PDF.

8.Chemo-enzymatic fluorination of unactivated organic compounds

Rentmeister A, Arnold FH, Fasan* R

Nat. Chem. Biol. 2009, 5 (1), 26-28 PDF.

7.Improved product-per-glucose yields in P450-dependent biotransformations using engineered E. coli

Fasan R, Crook NC, Peters MW, Meinhold P, Buelter T, Landwehr M, Cirino PC, Arnold FH

Biotechnol. Bioeng. 2011, 108 (3), 500-510 PDF.

6.Evolutionary history of a specialized propane monooxygenase

Fasan R, Meharenna YT, Snow CD, Poulos TL, Arnold* FH

J. Mol. Biol. 2008, 383 (5), 1069-1080 PDF.

5.Engineered alkane-hydroxylating cytochrome P450BM3 exhibiting native-like catalytic properties

Fasan R, Chen MM, Crook NC, Arnold* FH

Angew. Chem. Int. Ed. 2007, 46 (44), 8414-8418 PDF.

4.Structure-activity studies in a family of b-hairpin protein epitope mimetic inhibitors of the p53-HDM2 protein-protein interaction

Fasan R, Dias RL, Moehle K, Zerbe O, Obrecht D, Mittl PR, Grütter MG, Robinson* JA

Chembiochem 2006, 7 (3), 515-526 PDF.

3.Protein ligand design: from phage display to synthetic protein epitope mimetics in human antibody Fc-binding peptidomimetics

Dias RL, Fasan R, Moehle K, Renard A, Obrecht D, Robinson* JA

J. Am. Chem. Soc. 2006, 128 (8), 2726-2732 PDF.

2.Molecular basis of RNA recognition by the human alternative splicing factor Fox-1

Auweter SD, Fasan R, Reymond L, Underwood JG, Black DL, Pitsch S, Allain* FH

EMBO J 2006, 25 (1), 163-173 PDF.

1.Using a beta-hairpin to mimic an alpha-helix: cyclic peptidomimetic inhibitors of the p53-HDM2 protein-protein interaction

Fasan R, Dias RL, Moehle K, Zerbe O, Vrijbloed JW, Robinson* JA

Angew. Chem. Int. Ed. 2004, 43 (16), 2109-2112 PDF.