BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY

GROEGER C, Wenzel H, Tschesche H (1994)
INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH 44(2): 166-172.

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Abstract
Structural variants of BPTI were synthesized en route an enzymatic-chemical semisynthesis. The P-1-P-2 amide bond of the inhibitor molecule, which, as donor, contributes a hydrogen bond towards trypsin in the enzyme-inhibitor complex, was replaced by either a ketomethylene function or an ester bond yielding molecules with inhibitory activity. The two backbone-mutated BPTI derivatives showed increased dissociation constants of their respective trypsin complexes, obviously due to the lack of a single hydrogen-bond interaction in the enzyme-inhibitor complex. (C) Munksgaard 1994.
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GROEGER C, Wenzel H, Tschesche H. BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY. INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH. 1994;44(2):166-172.
GROEGER, C., Wenzel, H., & Tschesche, H. (1994). BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY. INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, 44(2), 166-172.
GROEGER, C., Wenzel, H., and Tschesche, H. (1994). BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY. INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH 44, 166-172.
GROEGER, C., Wenzel, H., & Tschesche, H., 1994. BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY. INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, 44(2), p 166-172.
C. GROEGER, H. Wenzel, and H. Tschesche, “BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY”, INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, vol. 44, 1994, pp. 166-172.
GROEGER, C., Wenzel, H., Tschesche, H.: BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY. INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH. 44, 166-172 (1994).
GROEGER, C, Wenzel, Herbert, and Tschesche, Harald. “BPTI BACKBONE VARIANTS AND IMPLICATIONS FOR INHIBITORY ACTIVITY”. INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH 44.2 (1994): 166-172.
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