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Artikel ; Online: Chemoselective N-Acylation of Amines with Acylsilanes under Aqueous Acidic Conditions.

Tian, Jing / Li, Wei / Deng, Xingwang / Lakshminarayanan, Rajamani / Srinivasan, Rajavel

Organic letters

2023 Band 25, Heft 31, Seite(n) 5740–5744

Abstract: We report a facile method for forming amide bonds between acylsilanes and a wide range of amines in the presence of a mild chlorinating agent under aqueous acidic conditions. The reaction is highly chemoselective, as exemplified by the late-stage ... ...

Abstract	We report a facile method for forming amide bonds between acylsilanes and a wide range of amines in the presence of a mild chlorinating agent under aqueous acidic conditions. The reaction is highly chemoselective, as exemplified by the late-stage modification of a panel of approved drugs and natural products containing reactive functionalities.
Sprache	Englisch
Erscheinungsdatum	2023-07-29
Erscheinungsland	United States
Dokumenttyp	Journal Article
ISSN	1523-7052
ISSN (online)	1523-7052
DOI	10.1021/acs.orglett.3c01911
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: Biofilm formation and virulence potential of carbapenem-resistant Pseudomonas aeruginosa.

Ma, Yeping / Aung, Thet Tun / Lakshminarayanan, Rajamani / Chua, Song Lin

The Lancet. Microbe

2023 Band 4, Heft 7, Seite(n) e489

Mesh-Begriff(e)	Virulence ; Pseudomonas aeruginosa ; Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/therapeutic use ; Carbapenems/pharmacology ; Biofilms
Chemische Substanzen	Anti-Bacterial Agents ; Carbapenems
Sprache	Englisch
Erscheinungsdatum	2023-04-24
Erscheinungsland	England
Dokumenttyp	Letter ; Research Support, Non-U.S. Gov't ; Comment
ISSN	2666-5247
ISSN (online)	2666-5247
DOI	10.1016/S2666-5247(23)00097-6
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel: Correction: Peguda et al. The Activity of Polyhomoarginine against

Peguda, Hari Kumar / Lakshminarayanan, Rajamani / Carnt, Nicole A / Gu, Zi / Willcox, Mark D P

Biology

2023 Band 12, Heft 3

Abstract: In the original publication [ ... ]. ...

Abstract	In the original publication [...].
Sprache	Englisch
Erscheinungsdatum	2023-03-20
Erscheinungsland	Switzerland
Dokumenttyp	Published Erratum
ZDB-ID	2661517-4
ISSN	2079-7737
ISSN	2079-7737
DOI	10.3390/biology12030470
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: The Activity of Polyhomoarginine against Acanthamoeba castellanii

Peguda, Hari Kumar / Lakshminarayanan, Rajamani / Carnt, Nicole A. / Gu, Zi / Willcox, Mark D. P.

Biology (Basel). 2022 Nov. 28, v. 11, no. 12

2022

Abstract: Arginine-rich peptides can have broad-spectrum anti-bacterial and anti-fungal activities. Polyhomoarginine consists of highly cationic residues which can act on the negatively charged microbial cell membranes. Acanthamoeba is a free-living protozoan ... ...

Abstract	Arginine-rich peptides can have broad-spectrum anti-bacterial and anti-fungal activities. Polyhomoarginine consists of highly cationic residues which can act on the negatively charged microbial cell membranes. Acanthamoeba is a free-living protozoan known to cause a rare corneal infection which is difficult to diagnose and treat. This study evaluated the activity of the polyhomoarginines against Acanthamoeba castellanii. Acanthamoeba amoebicidal, amoebistatic, encystation and excystment assays were performed using protocols described in the literature. The activity of polyhomoarginines (PHAs) of different lengths (10 to 400 residues) was measured against the trophozoites and cysts of Acanthamoeba castellanii ATCC30868 in concentrations ranging from 0.93 μM to 15 μM. Data were represented as mean ± SE and analysed using one-way ANOVA. Overall, PHAs demonstrated good anti-acanthamoeba activity against both trophozoites and cysts. PHA 30 reduced the number of viable trophozoites by 99%, inhibited the formation of cysts by 96% and the emergence of trophozoites from cysts by 67% at 3.75 μM. PHA 10 was similarly active, but at a slightly higher concentration of 15 μM, reducing the numbers of viable trophozoites by 98%, inhibiting cyst formation by 84% and preventing the emergence of trophozoites from cysts by 99%. At their greatest anti-amoeba concentrations, PHA 10 gave only 8% haemolysis at 15 μM while PHA 30 gave <40 % haemolysis at 3.75 μM. Polyhomoarginine 10 showed excellent anti-amoebic activity against both forms of Acanthamoeba castellanii and was non-toxic at its most active concentrations. This implies that polyhomoarginines can be developed into a potential therapeutic agent for Acanthamoeba keratitis. However, there is a need to carry out further pre-clinical and then in vivo experiments in the AK animal model.
Schlagwörter	Acanthamoeba castellanii ; animal models ; encystment ; excystation ; hemolysis ; keratitis ; peptides ; therapeutics ; trophozoites
Sprache	Englisch
Erscheinungsverlauf	2022-1128
Erscheinungsort	Multidisciplinary Digital Publishing Institute
Dokumenttyp	Artikel ; Online
ZDB-ID	2661517-4
ISSN	2079-7737
ISSN	2079-7737
DOI	10.3390/biology11121726
Datenquelle	NAL Katalog (AGRICOLA)

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Artikel: The Activity of Polyhomoarginine against

Peguda, Hari Kumar / Lakshminarayanan, Rajamani / Carnt, Nicole A / Gu, Zi / Willcox, Mark D P

Biology

2022 Band 11, Heft 12

Abstract	Arginine-rich peptides can have broad-spectrum anti-bacterial and anti-fungal activities. Polyhomoarginine consists of highly cationic residues which can act on the negatively charged microbial cell membranes. Acanthamoeba is a free-living protozoan known to cause a rare corneal infection which is difficult to diagnose and treat. This study evaluated the activity of the polyhomoarginines against Acanthamoeba castellanii. Acanthamoeba amoebicidal, amoebistatic, encystation and excystment assays were performed using protocols described in the literature. The activity of polyhomoarginines (PHAs) of different lengths (10 to 400 residues) was measured against the trophozoites and cysts of Acanthamoeba castellanii ATCC30868 in concentrations ranging from 0.93 μM to 15 μM. Data were represented as mean ± SE and analysed using one-way ANOVA. Overall, PHAs demonstrated good anti-acanthamoeba activity against both trophozoites and cysts. PHA 30 reduced the number of viable trophozoites by 99%, inhibited the formation of cysts by 96% and the emergence of trophozoites from cysts by 67% at 3.75 μM. PHA 10 was similarly active, but at a slightly higher concentration of 15 μM, reducing the numbers of viable trophozoites by 98%, inhibiting cyst formation by 84% and preventing the emergence of trophozoites from cysts by 99%. At their greatest anti-amoeba concentrations, PHA 10 gave only 8% haemolysis at 15 μM while PHA 30 gave <40 % haemolysis at 3.75 μM. Polyhomoarginine 10 showed excellent anti-amoebic activity against both forms of Acanthamoeba castellanii and was non-toxic at its most active concentrations. This implies that polyhomoarginines can be developed into a potential therapeutic agent for Acanthamoeba keratitis. However, there is a need to carry out further pre-clinical and then in vivo experiments in the AK animal model.
Sprache	Englisch
Erscheinungsdatum	2022-11-28
Erscheinungsland	Switzerland
Dokumenttyp	Journal Article
ZDB-ID	2661517-4
ISSN	2079-7737
ISSN	2079-7737
DOI	10.3390/biology11121726
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel: Host Defense Peptides at the Ocular Surface: Roles in Health and Major Diseases, and Therapeutic Potentials.

Ting, Darren Shu Jeng / Mohammed, Imran / Lakshminarayanan, Rajamani / Beuerman, Roger W / Dua, Harminder S

Frontiers in medicine

2022 Band 9, Seite(n) 835843

Abstract: Sight is arguably the most important sense in human. Being constantly exposed to the environmental stress, irritants and pathogens, the ocular surface - a specialized functional and anatomical unit composed of tear film, conjunctival and corneal ... ...

Abstract	Sight is arguably the most important sense in human. Being constantly exposed to the environmental stress, irritants and pathogens, the ocular surface - a specialized functional and anatomical unit composed of tear film, conjunctival and corneal epithelium, lacrimal glands, meibomian glands, and nasolacrimal drainage apparatus - serves as a crucial front-line defense of the eye. Host defense peptides (HDPs), also known as antimicrobial peptides, are evolutionarily conserved molecular components of innate immunity that are found in all classes of life. Since the first discovery of lysozyme in 1922, a wide range of HDPs have been identified at the ocular surface. In addition to their antimicrobial activity, HDPs are increasingly recognized for their wide array of biological functions, including anti-biofilm, immunomodulation, wound healing, and anti-cancer properties. In this review, we provide an updated review on: (1) spectrum and expression of HDPs at the ocular surface; (2) participation of HDPs in ocular surface diseases/conditions such as infectious keratitis, conjunctivitis, dry eye disease, keratoconus, allergic eye disease, rosacea keratitis, and post-ocular surgery; (3) HDPs that are currently in the development pipeline for treatment of ocular diseases and infections; and (4) future potential of HDP-based clinical pharmacotherapy for ocular diseases.
Sprache	Englisch
Erscheinungsdatum	2022-06-16
Erscheinungsland	Switzerland
Dokumenttyp	Journal Article ; Review
ZDB-ID	2775999-4
ISSN	2296-858X
ISSN	2296-858X
DOI	10.3389/fmed.2022.835843
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: Enzyme-Linked Immunosorbent Assay for T-Cell Dependent Immunogenicity Assessment of Therapeutic Peptides.

Chalasani, Madhavi Latha Somaraju / Lakshminarayanan, Rajamani / Verma, Navin Kumar

Methods in molecular biology (Clifton, N.J.)

2019 Band 1930, Seite(n) 129–138

Abstract: Immunogenicity assessment of therapeutic peptides, proteins, oligonucleotides, and hybrid molecules, such as nucleopeptides, is a major aspect in understanding their safety and efficacy. Both T-cell independent and dependent immune reactions contribute ... ...

Abstract	Immunogenicity assessment of therapeutic peptides, proteins, oligonucleotides, and hybrid molecules, such as nucleopeptides, is a major aspect in understanding their safety and efficacy. Both T-cell independent and dependent immune reactions contribute to an immunogenic response against antigen, including secretion of cytokines and production of an antigen-specific antibody. Various assays exist for detecting and quantifying such immunogenic responses by human T-cells ex vivo or in mouse serum, which primarily include enzyme-linked immunosorbent assay (ELISA, direct and indirect), flow-cytometry and surface plasmon resonance (SPR). ELISA is a popular choice due to its robustness, reliability, sensitivity, ease of automation, and the requirement of simple equipment commonly available in most molecular biology and biochemistry laboratories. The chapter describes the detailed protocol of cytokine analysis by an ELISA method and highlights few crucial steps to be considered while performing the assay for successful immunogenicity studies.
Mesh-Begriff(e)	Animals ; Antibodies, Monoclonal/immunology ; Cytokines/immunology ; Cytokines/metabolism ; Enzyme-Linked Immunosorbent Assay/methods ; Humans ; Immunity, Cellular/immunology ; Peptide Fragments/immunology ; Peptide Fragments/therapeutic use ; Serum/metabolism ; T-Lymphocytes/immunology ; T-Lymphocytes/metabolism
Chemische Substanzen	Antibodies, Monoclonal ; Cytokines ; Peptide Fragments
Sprache	Englisch
Erscheinungsdatum	2019-01-04
Erscheinungsland	United States
Dokumenttyp	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1940-6029
ISSN (online)	1940-6029
DOI	10.1007/978-1-4939-9036-8_16
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel: SLAP reagents for the photocatalytic synthesis of C3/C5-substituted, N-unprotected selenomorpholines and 1,4-selenazepanes

Zhou, Guan / Deng, Xingwang / Pan, Chenyu / Goh, Eunice Tze Leng / Lakshminarayanan, Rajamani / Srinivasan, Rajavel

Chemical communications. 2020 Oct. 20, v. 56, no. 83

2020

Abstract: Herein, we disclose the first set of unique selenium-containing SLAP (SiLicon Amine Protocol) reagents for the direct synthesis of C3/C5-substituted selenomorpholines and 1,4-selenazepanes from diverse (hetero)aldehydes under mild photocatalytic ... ...

Abstract	Herein, we disclose the first set of unique selenium-containing SLAP (SiLicon Amine Protocol) reagents for the direct synthesis of C3/C5-substituted selenomorpholines and 1,4-selenazepanes from diverse (hetero)aldehydes under mild photocatalytic conditions. Enantiomerically pure 1,2-amino alcohol/α-amino acid versions of these heterocycles were also synthesized. Further, we have shown the late-stage modification of certain biologically active agents using the developed seleno-SLAP reagents.
Schlagwörter	heterocyclic compounds ; photocatalysis ; silicon
Sprache	Englisch
Erscheinungsverlauf	2020-1020
Umfang	p. 12546-12549.
Erscheinungsort	The Royal Society of Chemistry
Dokumenttyp	Artikel
Anmerkung	NAL-AP-2-clean
ZDB-ID	1472881-3
ISSN	1364-548X ; 1359-7345 ; 0009-241X
ISSN (online)	1364-548X
ISSN	1359-7345 ; 0009-241X
DOI	10.1039/d0cc04471g
Datenquelle	NAL Katalog (AGRICOLA)

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Artikel ; Online: Strategies in Translating the Therapeutic Potentials of Host Defense Peptides.

Ting, Darren Shu Jeng / Beuerman, Roger W / Dua, Harminder S / Lakshminarayanan, Rajamani / Mohammed, Imran

Frontiers in immunology

2020 Band 11, Seite(n) 983

Abstract: The golden era of antibiotics, heralded by the discovery of penicillin, has long been challenged by the emergence of antimicrobial resistance (AMR). Host defense peptides (HDPs), previously known as antimicrobial peptides, are emerging as a group of ... ...

Abstract	The golden era of antibiotics, heralded by the discovery of penicillin, has long been challenged by the emergence of antimicrobial resistance (AMR). Host defense peptides (HDPs), previously known as antimicrobial peptides, are emerging as a group of promising antimicrobial candidates for combatting AMR due to their rapid and unique antimicrobial action. Decades of research have advanced our understanding of the relationship between the physicochemical properties of HDPs and their underlying antimicrobial and non-antimicrobial functions, including immunomodulatory, anti-biofilm, and wound healing properties. However, the mission of translating novel HDP-derived molecules from bench to bedside has yet to be fully accomplished, primarily attributed to their intricate structure-activity relationship, toxicity, instability in host and microbial environment, lack of correlation between
Mesh-Begriff(e)	Animals ; Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/pharmacology ; Antifungal Agents/chemistry ; Antifungal Agents/pharmacology ; Antimicrobial Cationic Peptides/chemistry ; Antimicrobial Cationic Peptides/pharmacology ; Artificial Intelligence ; Computer-Aided Design ; Drug Design ; Drug Discovery ; Drug Resistance, Bacterial ; Drug Resistance, Fungal ; Humans ; Protein Conformation ; Structure-Activity Relationship ; Translational Research, Biomedical
Chemische Substanzen	Anti-Bacterial Agents ; Antifungal Agents ; Antimicrobial Cationic Peptides
Schlagwörter	covid19
Sprache	Englisch
Erscheinungsdatum	2020-05-22
Erscheinungsland	Switzerland
Dokumenttyp	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2606827-8
ISSN	1664-3224 ; 1664-3224
ISSN (online)	1664-3224
ISSN	1664-3224
DOI	10.3389/fimmu.2020.00983
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: SLAP reagents for the photocatalytic synthesis of C3/C5-substituted, N-unprotected selenomorpholines and 1,4-selenazepanes.

Zhou, Guan / Deng, Xingwang / Pan, Chenyu / Goh, Eunice Tze Leng / Lakshminarayanan, Rajamani / Srinivasan, Rajavel

Chemical communications (Cambridge, England)

2020 Band 56, Heft 83, Seite(n) 12546–12549

Abstract	Herein, we disclose the first set of unique selenium-containing SLAP (SiLicon Amine Protocol) reagents for the direct synthesis of C3/C5-substituted selenomorpholines and 1,4-selenazepanes from diverse (hetero)aldehydes under mild photocatalytic conditions. Enantiomerically pure 1,2-amino alcohol/α-amino acid versions of these heterocycles were also synthesized. Further, we have shown the late-stage modification of certain biologically active agents using the developed seleno-SLAP reagents.
Sprache	Englisch
Erscheinungsdatum	2020-09-16
Erscheinungsland	England
Dokumenttyp	Journal Article
ZDB-ID	1472881-3
ISSN	1364-548X ; 1359-7345 ; 0009-241X
ISSN (online)	1364-548X
ISSN	1359-7345 ; 0009-241X
DOI	10.1039/d0cc04471g
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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