Author
M. Mergler
Bio: M. Mergler is an academic researcher. The author has contributed to research in topics: Peptide synthesis & Benzyl alcohol. The author has an hindex of 6, co-authored 6 publications receiving 304 citations.
Papers
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TL;DR: In this article, the synthesis of a new polymeric support for the preparation of fully protected peptide fragments by the Fmoc/t-butyl method is described, and data for coupling yields and racemization data are given.
168 citations
TL;DR: In this paper, the synthesis of fully protected peptide fragments by the Fmoc/ t-butyl method on a new polymeric support is described, which is obtained in good yields and high purity upon cleavage from the resin with 0.5 - 1 % trifluoroacetic acid in methylene chloride.
81 citations
TL;DR: In this article, the conversion of 4-alkoxy benzyl alcohol resin and 2-methoxy-4-alkoxal alcohol resin (SASRIN) into the corresponding halides is described.
21 citations
TL;DR: In this paper, a mild and efficient method to obtain fully t-butyl type protected alcohols based on the alkylation of Fmoc amino alcohols with the polymeric diphenyldiazomethane was presented.
15 citations
TL;DR: The cesium salts of N α -9-fluorenylmethyloxycarbonyl (Fmoc) amino acids couple smoothly to new chloro derivatives of alkoxy benzyl alcohol resins.
14 citations
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3,281 citations
TL;DR: The great variety of conditions under which Fmoc solid phase peptide synthesis may be carried out represents a truly "orthogonal" scheme, and thus offers many unique opportunities for bioorganic chemistry.
Abstract: 9-Fluorenylmethoxycarbonyl (Fmoc) amino acids were first used for solid phase peptide synthesis a little more than a decade ago. Since that time, Fmoc solid phase peptide synthesis methodology has been greatly enhanced by the introduction of a variety of solid supports, linkages, and side chain protecting groups, as well as by increased understanding of solvation conditions. These advances have led to many impressive syntheses, such as those of biologically active and isotopically labeled peptides and small proteins. The great variety of conditions under which Fmoc solid phase peptide synthesis may be carried out represents a truly "orthogonal" scheme, and thus offers many unique opportunities for bioorganic chemistry.
2,336 citations
TL;DR: This review reports on the unexpected and considerable number of peptides that are currently available as drugs and the chemical strategies that were used to bring them into the market.
1,237 citations
TL;DR: 1. Small Molecule Libraries 420 1. Acyclic Libraries 422 2. Libraries on Preformed Scaffolds 422 3. Heterocyclic Libraries 423 4. Structurally Heterogeneous Libraries 427 E. Cleavable Linkers 428 1. Single Cleavables 428 2. Multiply Cleavably Linkers 429 IV. Screening Methods 432
Abstract: 1. Peptoids 419 2. Oligocarbamates 420 3. Oligoureas 420 4. Vinylogous Sulfonyl Peptides 420 5. Peptidosulfonamides 420 6. Azatides 420 7. Ketides 420 D. Small Molecule Libraries 420 1. Acyclic Libraries 422 2. Libraries on Preformed Scaffolds 422 3. Heterocyclic Libraries 423 4. Structurally Heterogeneous Libraries 427 E. Cleavable Linkers 428 1. Single Cleavable Linkers 428 2. Multiply Cleavable Linkers 429 IV. Screening Methods 432 A. On-Bead Screening 432 1. Binding Assay 432 2. Functional Assay 434 B. Solution-Phase Screening 434 1. The 96-Well Two-Stage Releasable Assays 435
672 citations
TL;DR: It is a privilege to be able to contribute to this volume in which Professor Zervas’ friends, students, and colleagues have joined together to honor him and his remarkable contributions to peptide chemistry.
Abstract: It is a privilege to be able to contribute to this volume in which Professor Zervas’ friends, students, and colleagues have joined together to honor him and his remarkable contributions to peptide chemistry. Although I did not know him until after his days in the Bergmann Laboratory at the Rockefeller Institute, I can claim the distinction of now working in those very same rooms that they occupied back in the mid-1930s. Like all peptide chemists, I am greatly indebted to Professor Zervas, having depended so heavily on the carbobenzoxy group and on the various modified urethan protecting groups which have been direct extensions of the revolutionary advance that Bergmann and Zervas made.
507 citations