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A letter from Professor Samuel J. Danishefsky.

Danishefsky SJ.

J Antibiot (Tokyo). 2019 Jun;72(6):319-322. doi: 10.1038/s41429-019-0179-7. Epub 2019 May 27. No abstract available.


Chemical biology of glycoproteins: From chemical synthesis to biological impact.

Li Y, Tran AH, Danishefsky SJ, Tan Z.

Methods Enzymol. 2019;621:213-229. doi: 10.1016/bs.mie.2019.02.030. Epub 2019 Mar 14.


Total Chemical Synthesis of Human Thyroid-Stimulating Hormone (hTSH) β-Subunit: Application of Arginine-tagged Acetamidomethyl (AcmR) Protecting Groups.

Brailsford JA, Stockdill JL, Axelrod AJ, Peterson MT, Vadola PA, Johnston EV, Danishefsky SJ.

Tetrahedron. 2018 Apr 12;74(15):1951-1956. doi: 10.1016/j.tet.2018.02.067. Epub 2018 Mar 6.


Antibodies Against Specific MUC16 Glycosylation Sites Inhibit Ovarian Cancer Growth.

Rao TD, Fernández-Tejada A, Axelrod A, Rosales N, Yan X, Thapi S, Wang A, Park KJ, Nemieboka B, Xiang J, Lewis JS, Olvera N, Levine DA, Danishefsky SJ, Spriggs DR.

ACS Chem Biol. 2017 Aug 18;12(8):2085-2096. doi: 10.1021/acschembio.7b00305. Epub 2017 Jun 28.


Total Chemical Synthesis and Folding of All-l and All-d Variants of Oncogenic KRas(G12V).

Levinson AM, McGee JH, Roberts AG, Creech GS, Wang T, Peterson MT, Hendrickson RC, Verdine GL, Danishefsky SJ.

J Am Chem Soc. 2017 Jun 7;139(22):7632-7639. doi: 10.1021/jacs.7b02988. Epub 2017 May 22.


Staged induction of HIV-1 glycan-dependent broadly neutralizing antibodies.

Bonsignori M, Kreider EF, Fera D, Meyerhoff RR, Bradley T, Wiehe K, Alam SM, Aussedat B, Walkowicz WE, Hwang KK, Saunders KO, Zhang R, Gladden MA, Monroe A, Kumar A, Xia SM, Cooper M, Louder MK, McKee K, Bailer RT, Pier BW, Jette CA, Kelsoe G, Williams WB, Morris L, Kappes J, Wagh K, Kamanga G, Cohen MS, Hraber PT, Montefiori DC, Trama A, Liao HX, Kepler TB, Moody MA, Gao F, Danishefsky SJ, Mascola JR, Shaw GM, Hahn BH, Harrison SC, Korber BT, Haynes BF.

Sci Transl Med. 2017 Mar 15;9(381). pii: eaai7514. doi: 10.1126/scitranslmed.aai7514.


Vaccine Elicitation of High Mannose-Dependent Neutralizing Antibodies against the V3-Glycan Broadly Neutralizing Epitope in Nonhuman Primates.

Saunders KO, Nicely NI, Wiehe K, Bonsignori M, Meyerhoff RR, Parks R, Walkowicz WE, Aussedat B, Wu NR, Cai F, Vohra Y, Park PK, Eaton A, Go EP, Sutherland LL, Scearce RM, Barouch DH, Zhang R, Von Holle T, Overman RG, Anasti K, Sanders RW, Moody MA, Kepler TB, Korber B, Desaire H, Santra S, Letvin NL, Nabel GJ, Montefiori DC, Tomaras GD, Liao HX, Alam SM, Danishefsky SJ, Haynes BF.

Cell Rep. 2017 Feb 28;18(9):2175-2188. doi: 10.1016/j.celrep.2017.02.003.


A Phase I Study of Unimolecular Pentavalent (Globo-H-GM2-sTn-TF-Tn) Immunization of Patients with Epithelial Ovarian, Fallopian Tube, or Peritoneal Cancer in First Remission.

O'Cearbhaill RE, Ragupathi G, Zhu J, Wan Q, Mironov S, Yang G, Spassova MK, Iasonos A, Kravetz S, Ouerfelli O, Spriggs DR, Danishefsky SJ, Sabbatini PJ.

Cancers (Basel). 2016 Apr 22;8(4). pii: E46. doi: 10.3390/cancers8040046.


Human Cancer Antigen Globo H Is a Cell-Surface Ligand for Human Ribonuclease 1.

Eller CH, Chao TY, Singarapu KK, Ouerfelli O, Yang G, Markley JL, Danishefsky SJ, Raines RT.

ACS Cent Sci. 2015 Jul 22;1(4):181-190. Epub 2015 Jul 13.


Fully Synthetic Granulocyte Colony-Stimulating Factor Enabled by Isonitrile-Mediated Coupling of Large, Side-Chain-Unprotected Peptides.

Roberts AG, Johnston EV, Shieh JH, Sondey JP, Hendrickson RC, Moore MA, Danishefsky SJ.

J Am Chem Soc. 2015 Oct 14;137(40):13167-75. doi: 10.1021/jacs.5b08754. Epub 2015 Oct 1.


Designing synthetic vaccines for HIV.

Fernández-Tejada A, Haynes BF, Danishefsky SJ.

Expert Rev Vaccines. 2015 Jun;14(6):815-31. doi: 10.1586/14760584.2015.1027690. Epub 2015 Mar 31. Review.


Total synthesis of glycosylated proteins.

Fernández-Tejada A, Brailsford J, Zhang Q, Shieh JH, Moore MA, Danishefsky SJ.

Top Curr Chem. 2015;362:1-26. doi: 10.1007/128_2014_622. Review.


Development of Globo-H cancer vaccine.

Danishefsky SJ, Shue YK, Chang MN, Wong CH.

Acc Chem Res. 2015 Mar 17;48(3):643-52. doi: 10.1021/ar5004187. Epub 2015 Feb 10.


Studies toward the total synthesis of pluraflavin A.

Hartung J, J D Wright B, Danishefsky SJ.

Chemistry. 2014 Jul 7;20(28):8731-6. doi: 10.1002/chem.201402254. Epub 2014 Jun 12.


Stereospecific cis- and trans-ring fusions arising from common intermediates.

Townsend SD, Ross AG, Liu K, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2014 Jun 3;111(22):7931-5. doi: 10.1073/pnas.1407613111. Epub 2014 May 19.


Chemical synthesis of the β-subunit of human luteinizing (hLH) and chorionic gonadotropin (hCG) glycoprotein hormones.

Fernández-Tejada A, Vadola PA, Danishefsky SJ.

J Am Chem Soc. 2014 Jun 11;136(23):8450-8. doi: 10.1021/ja503545r. Epub 2014 May 27.


Chemical synthesis of the ATAD2 bromodomain.

Creech GS, Paresi C, Li YM, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2014 Feb 25;111(8):2891-6. doi: 10.1073/pnas.1400556111. Epub 2014 Feb 10.


Synthesis of granulocyte-macrophage colony-stimulating factor as homogeneous glycoforms and early comparisons with yeast cell-derived material.

Zhang Q, Johnston EV, Shieh JH, Moore MA, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2014 Feb 25;111(8):2885-90. doi: 10.1073/pnas.1400140111. Epub 2014 Feb 10.


Intramolecular Diels-Alder reactions of cycloalkenones: stereoselectivity, Lewis acid acceleration, and halogen substituent effects.

Pham HV, Paton RS, Ross AG, Danishefsky SJ, Houk KN.

J Am Chem Soc. 2014 Feb 12;136(6):2397-403. doi: 10.1021/ja410220w. Epub 2014 Feb 4.


Erythropoietin derived by chemical synthesis.

Wang P, Dong S, Shieh JH, Peguero E, Hendrickson R, Moore MAS, Danishefsky SJ.

Science. 2013 Dec 13;342(6164):1357-1360. doi: 10.1126/science.1245095.


Recognition of synthetic glycopeptides by HIV-1 broadly neutralizing antibodies and their unmutated ancestors.

Alam SM, Dennison SM, Aussedat B, Vohra Y, Park PK, Fernández-Tejada A, Stewart S, Jaeger FH, Anasti K, Blinn JH, Kepler TB, Bonsignori M, Liao HX, Sodroski JG, Danishefsky SJ, Haynes BF.

Proc Natl Acad Sci U S A. 2013 Nov 5;110(45):18214-9. doi: 10.1073/pnas.1317855110. Epub 2013 Oct 21.


A vision for vaccines built from fully synthetic tumor-associated antigens: from the laboratory to the clinic.

Wilson RM, Danishefsky SJ.

J Am Chem Soc. 2013 Oct 2;135(39):14462-72. doi: 10.1021/ja405932r. Epub 2013 Sep 18.


Chemical synthesis of highly congested gp120 V1V2 N-glycopeptide antigens for potential HIV-1-directed vaccines.

Aussedat B, Vohra Y, Park PK, Fernández-Tejada A, Alam SM, Dennison SM, Jaeger FH, Anasti K, Stewart S, Blinn JH, Liao HX, Sodroski JG, Haynes BF, Danishefsky SJ.

J Am Chem Soc. 2013 Sep 4;135(35):13113-20. doi: 10.1021/ja405990z. Epub 2013 Aug 22.


Solid-phase peptide synthesis and solid-phase fragment coupling mediated by isonitriles.

Wang T, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):11708-13. doi: 10.1073/pnas.1310431110. Epub 2013 Jul 2.


Pattern recognition analysis in complex molecule synthesis and the preparation of iso-Diels-Alder motifs.

Peng F, Grote RE, Wilson RM, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):10904-9. doi: 10.1073/pnas.1309795110. Epub 2013 Jun 19.


The winding pathway to erythropoietin along the chemistry-biology frontier: a success at last.

Wilson RM, Dong S, Wang P, Danishefsky SJ.

Angew Chem Int Ed Engl. 2013 Jul 22;52(30):7646-65. doi: 10.1002/anie.201301666. Epub 2013 Jun 17. Review.


Building biologics by chemical synthesis: practical preparation of di- and triantennary N-linked glycoconjugates.

Walczak MA, Hayashida J, Danishefsky SJ.

J Am Chem Soc. 2013 Mar 27;135(12):4700-3. doi: 10.1021/ja401385v. Epub 2013 Mar 19.


Halocycloalkenones as Diels-Alder dienophiles. Applications to generating useful structural patterns.

Ross AG, Townsend SD, Danishefsky SJ.

J Org Chem. 2013 Jan 4;78(1):204-10. doi: 10.1021/jo302230m. Epub 2012 Nov 27.


Permuting Diels-Alder and Robinson Annulation Stereopatterns.

Peng F, Dai M, Angeles AR, Danishefsky SJ.

Chem Sci. 2012 Jan 1;3(10):3076-3080. Epub 2012 Aug 1.


Total synthesis of (±)-maoecrystal V.

Peng F, Danishefsky SJ.

J Am Chem Soc. 2012 Nov 14;134(45):18860-7. doi: 10.1021/ja309905j. Epub 2012 Nov 5.


Chemistry as an expanding resource in protein science: fully synthetic and fully active human parathyroid hormone-related protein (1-141).

Li J, Dong S, Townsend SD, Dean T, Gardella TJ, Danishefsky SJ.

Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12263-7. doi: 10.1002/anie.201207603. Epub 2012 Nov 4. No abstract available.


At last: erythropoietin as a single glycoform.

Wang P, Dong S, Brailsford JA, Iyer K, Townsend SD, Zhang Q, Hendrickson RC, Shieh J, Moore MA, Danishefsky SJ.

Angew Chem Int Ed Engl. 2012 Nov 12;51(46):11576-84. doi: 10.1002/anie.201206090. Epub 2012 Sep 25. No abstract available.


An advance in the chemical synthesis of homogeneous N-linked glycopolypeptides by convergent aspartylation.

Wang P, Aussedat B, Vohra Y, Danishefsky SJ.

Angew Chem Int Ed Engl. 2012 Nov 12;51(46):11571-5. doi: 10.1002/anie.201205038. Epub 2012 Sep 25. No abstract available.


Solving the convergence problem in the synthesis of triantennary N-glycan relevant to prostate-specific membrane antigen (PSMA).

Walczak MA, Danishefsky SJ.

J Am Chem Soc. 2012 Oct 3;134(39):16430-3. doi: 10.1021/ja307628w. Epub 2012 Sep 21.


Intramolecular Diels-Alder reactions of cycloalkenones: translation of high endo selectivity to trans junctions.

Ross AG, Li X, Danishefsky SJ.

J Am Chem Soc. 2012 Sep 26;134(38):16080-4. Epub 2012 Sep 18.


Engineering of therapeutic polypeptides through chemical synthesis: early lessons from human parathyroid hormone and analogues.

Dong S, Shang S, Li J, Tan Z, Dean T, Maeda A, Gardella TJ, Danishefsky SJ.

J Am Chem Soc. 2012 Sep 12;134(36):15122-9. doi: 10.1021/ja306637u. Epub 2012 Aug 29.


Synthetic studies toward (+)-cortistatin A.

Wang Z, Dai M, Park PK, Danishefsky SJ.

Tetrahedron. 2011 Dec 30;67(52):10249-10260. Epub 2011 Oct 29.


Revisiting oxytocin through the medium of isonitriles.

Wang T, Danishefsky SJ.

J Am Chem Soc. 2012 Aug 15;134(32):13244-7. doi: 10.1021/ja3063452. Epub 2012 Aug 2.


Enhancing the scope of the Diels-Alder reaction through isonitrile chemistry: emergence of a new class of acyl-activated dienophiles.

Townsend SD, Wu X, Danishefsky SJ.

J Am Chem Soc. 2012 Jun 27;134(25):10659-63. doi: 10.1021/ja303876e. Epub 2012 Jun 18.


Probing the stability of nonglycosylated wild-type erythropoietin protein via reiterative alanine ligations.

Brailsford JA, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2012 May 8;109(19):7196-201. doi: 10.1073/pnas.1202762109. Epub 2012 Apr 12.


A fascinating journey into history: exploration of the world of isonitriles en route to complex amides.

Wilson RM, Stockdill JL, Wu X, Li X, Vadola PA, Park PK, Wang P, Danishefsky SJ.

Angew Chem Int Ed Engl. 2012 Mar 19;51(12):2834-48. doi: 10.1002/anie.201106628. Epub 2012 Feb 24. Review.


Advances in proline ligation.

Townsend SD, Tan Z, Dong S, Shang S, Brailsford JA, Danishefsky SJ.

J Am Chem Soc. 2012 Feb 29;134(8):3912-6. doi: 10.1021/ja212182q. Epub 2012 Feb 15.


Total synthesis of the α-subunit of human glycoprotein hormones: toward fully synthetic homogeneous human follicle-stimulating hormone.

Aussedat B, Fasching B, Johnston E, Sane N, Nagorny P, Danishefsky SJ.

J Am Chem Soc. 2012 Feb 22;134(7):3532-41. doi: 10.1021/ja2111459. Epub 2012 Feb 6.


Expanding the limits of isonitrile-mediated amidations: on the remarkable stereosubtleties of macrolactam formation from synthetic seco-cyclosporins.

Wu X, Stockdill JL, Park PK, Danishefsky SJ.

J Am Chem Soc. 2012 Feb 1;134(4):2378-84. doi: 10.1021/ja2103372. Epub 2012 Jan 17.


Probing the frontiers of glycoprotein synthesis: the fully elaborated β-subunit of the human follicle-stimulating hormone.

Nagorny P, Sane N, Fasching B, Aussedat B, Danishefsky SJ.

Angew Chem Int Ed Engl. 2012 Jan 23;51(4):975-9. doi: 10.1002/anie.201107482. Epub 2011 Dec 9. No abstract available.


Experimental Diels-Alder reactivities of cycloalkenones and cyclic dienes explained through transition-state distortion energies.

Paton RS, Kim S, Ross AG, Danishefsky SJ, Houk KN.

Angew Chem Int Ed Engl. 2011 Oct 24;50(44):10366-8. doi: 10.1002/anie.201103998. Epub 2011 Sep 9. No abstract available.


Multifaceted cytoprotection by synthetic polyacetylenes inspired by the ginseng-derived natural product, panaxytriol.

Chou TC, Dong H, Zhang X, Lei X, Hartung J, Zhang Y, Lee JH, Wilson RM, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2011 Aug 23;108(34):14336-41. doi: 10.1073/pnas.1111332108. Epub 2011 Aug 15.


Further Expansion of the trans-Diels-Alder Paradigm: Reductive Alkylation of α-Cyanoketones.

Peng F, Grote RE, Danishefsky SJ.

Tetrahedron Lett. 2011 Aug 3;52(31):3957-3959.


Emergence of potent inhibitors of metastasis in lung cancer via syntheses based on migrastatin.

Lecomte N, Njardarson JT, Nagorny P, Yang G, Downey R, Ouerfelli O, Moore MA, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15074-8. doi: 10.1073/pnas.1015247108. Epub 2011 Aug 1.

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