TY - JOUR
T1 - Direct dimerization simplifies the synthesis of himastatin and elucidates its mode of action
AU - Smith, Myles
N1 - Funding Information:
TheWelch Foundation (I-2045)andUniversityof Texas Southwestern MedicalCenter(W.W.Caruth Jr.Scholarship) are acknowledged for funding.
Publisher Copyright:
© 2022 American Association for the Advancement of Science. All rights reserved.
PY - 2022/2/25
Y1 - 2022/2/25
N2 - W ith tant rent need modes urgentthe bacteria frontline for (of 1emergence). One antibiotics actionthatemerging therapeutics, iscan ofincreasinglydrug-resis- evadewith strategy newcur- the to address this need is to revisit previously identified antibiotics of promise and apply modern medicinal chemistry and biochemical tools to improve their activity and unveil their often ill-defined modes of action (2, 3). Among such natural products is himastatin (1), a dimeric peptide antibiotic isolated in 1990 that shows good activity against Gram-positive bacteria, albeit through a largely unknown mode of action (4). On page 894 of this issue, D’Angelo et al. (5) develop an efficient chemical synthesis of himastatin through a bioinspired dimerization of its native monomeric units. This approach provides a blueprint to access not only this complex target and its derivatives, but also molecular probes that allow for its mode of action to be elucidated (5).
AB - W ith tant rent need modes urgentthe bacteria frontline for (of 1emergence). One antibiotics actionthatemerging therapeutics, iscan ofincreasinglydrug-resis- evadewith strategy newcur- the to address this need is to revisit previously identified antibiotics of promise and apply modern medicinal chemistry and biochemical tools to improve their activity and unveil their often ill-defined modes of action (2, 3). Among such natural products is himastatin (1), a dimeric peptide antibiotic isolated in 1990 that shows good activity against Gram-positive bacteria, albeit through a largely unknown mode of action (4). On page 894 of this issue, D’Angelo et al. (5) develop an efficient chemical synthesis of himastatin through a bioinspired dimerization of its native monomeric units. This approach provides a blueprint to access not only this complex target and its derivatives, but also molecular probes that allow for its mode of action to be elucidated (5).
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U2 - 10.1126/science.abn8327
DO - 10.1126/science.abn8327
M3 - Article
C2 - 35201871
AN - SCOPUS:85125344353
SN - 0036-8075
VL - 375
SP - 820
EP - 821
JO - Science
JF - Science
IS - 6583
ER -