当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > A combinatorial approach to chemical modification of subtilisin Bacillus lentus.

A combinatorial approach to chemical modification of subtilisin Bacillus lentus.

Abstract：

:The reaction between methanethiosulfonate reagents and cysteine mutants of subtilisin is quantitative and can be used to prepare chemically modified mutant enzymes (CMMs) with novel properties. The virtually unrestricted structural variations possible for CMMs presents a preparative and screening challenge. To address this, a rapid combinatorial method for preparing and screening the activities of CMMs has been developed.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Plettner E,Khumtaveeporn K,Shang X,Jones JB

doi

10.1016/s0960-894x(98)00415-6

subject

Has Abstract

pub_date

1998-09-08 00:00:00

pages

2291-6

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960894X98004156

journal_volume

8

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.

    abstract：:The synthesis of novel C6-aryl substituted derivatives of 3-(dimethylamino)chroman is described. The novel derivatives display 5-HT(7) receptor affinities that varies from nM to muM, indicating that this small set of derivatives constitute a novel and interesting starting point for further structure-serotonin 5-HT(7) ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.11.013

    authors： Holmberg P,Tedenborg L,Rosqvist S,Johansson AM

    更新日期：2005-02-01 00:00:00

  • Development of sub-nanomolar dipeptidic ligands of neuropeptide FF receptors.

    abstract：:Based on our earlier reported neuropeptide FF receptors antagonist (RF9), we carried out an extensive structural exploration of the N-terminus part of the amidated dipeptide Arg-Phe-NH(2) in order to establish a structure-activity relationships (SAR) study towards both NPFF receptor subtypes. This SAR led to the disco...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.10.049

    authors： Gealageas R,Schneider S,Humbert JP,Bertin I,Schmitt M,Laboureyras E,Dugave C,Mollereau C,Simonnet G,Bourguignon JJ,Simonin F,Bihel F

    更新日期：2012-12-15 00:00:00

  • Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) delta agonists.

    abstract：:A series of 1,4-benzyloxybenzylsulfanylaryl carboxylic acids were prepared and their activities for PPAR receptor subtypes (alpha, delta, and gamma) with potential indications for the treatment of dyslipidemia were investigated. Analog 13a displayed the greatest binding affinity (IC(50)=10nM) and selectivity (120-fold...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.04.046

    authors： Bratton LD,Filzen GF,Geyer A,Hoffman JK,Lu G,Pulaski J,Trivedi BK,Unangst PC,Xu X

    更新日期：2007-07-01 00:00:00

  • Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.

    abstract：:P2X purinoceptors are ligand-gated ion channels whose endogenous ligand is ATP. Both the P2X(3) and P2X(2/3) receptor subtypes have been shown to play an important role in the regulation of sensory function and dual P2X(3)/P2X(2/3) antagonists offer significant potential for the treatment of pain. A high-throughput sc...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.02.003

    authors： Carter DS,Alam M,Cai H,Dillon MP,Ford AP,Gever JR,Jahangir A,Lin C,Moore AG,Wagner PJ,Zhai Y

    更新日期：2009-03-15 00:00:00

  • Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.

    abstract：:Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibito...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.12.112

    authors： Lin S,Han F,Liu P,Tao J,Zhong X,Liu X,Yi C,Xu H

    更新日期：2014-02-01 00:00:00

  • Synthesis and biological evaluation of novel 4-(hetero) aryl-2-piperazino quinazolines as anti-leishmanial and anti-proliferative agents.

    abstract：:A series of new class of 4-(hetero)aryl-2-piperazino quinazolines were synthesized and assessed for in vitro activity against extracellular promastigotes and intracellular amastigotes of Leishmania donovani. Among the compounds evaluated, compound 4bb and 4cb showed the selectivity index (SI) value>8.03 and 4.21, resp...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.03.020

    authors： Kumar S,Shakya N,Gupta S,Sarkar J,Sahu DP

    更新日期：2009-05-01 00:00:00

  • Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives.

    abstract：:A series of 8-heteroarylthiomethyldipyridodiazepinone derivatives were prepared and evaluated for their antiviral profile against wild type virus and the important K103N/Y181C mutant as an indicator for broad activity. 2,6-Dimethylpyridine derivative 16 was found to have a good pharmacokinetic profile in spite of poor...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.11.049

    authors： Yoakim C,Bonneau PR,Déziel R,Doyon L,Duan J,Guse I,Landry S,Malenfant E,Naud J,Ogilvie WW,O'Meara JA,Plante R,Simoneau B,Thavonekham B,Bös M,Cordingley MG

    更新日期：2004-02-09 00:00:00

  • Novel pyrimidines as acid pump antagonists (APAs).

    abstract：:A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H(+)/K(+) ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a pote...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.08.007

    authors： Yoon YA,Park CS,Cha MH,Choi H,Sim JY,Kim JG

    更新日期：2010-10-01 00:00:00

  • Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.

    abstract：:The discovery, synthesis, and SAR of chromanes as ER alpha subtype selective ligands are described. X-ray studies revealed that the origin of the ER alpha-selectivity resulted from a C-4 trans methyl substitution to the cis-2,3-diphenyl-chromane platform. Selected compounds from this class demonstrated very potent in ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.01.046

    authors： Tan Q,Blizzard TA,Morgan JD 2nd,Birzin ET,Chan W,Yang YT,Pai LY,Hayes EC,DaSilva CA,Warrier S,Yudkovitz J,Wilkinson HA,Sharma N,Fitzgerald PM,Li S,Colwell L,Fisher JE,Adamski S,Reszka AA,Kimmel D,DiNinno F,Rohre

    更新日期：2005-03-15 00:00:00

  • Chemoenzymatic deacylation of ramoplanin.

    abstract：:The chemoenzymatic deacylation of ramoplanin A2 is described for the first time: ramoplanin A2 was Boc-protected and hydrogenated to Boc-protected tetrahydroramoplanin, which was subsequently deacylated using an acylase from Actinoplanes utahensis NRRL 12052. The chemoenzymatic process proceeded with 80% overall yield...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.06.046

    authors： Gandolfi R,Marinelli F,Ragg E,Romano D,Molinari F

    更新日期：2012-08-15 00:00:00

  • Enzymatic synthesis of labeled DNA by PCR using new fluorescent thymidine nucleotide analogue and superthermophilic KOD dash DNA polymerase.

    abstract：:Triphosphate of a new fluorescent labeled thymidine analogue was incorporated as a substrate for PCR using KOD Dash DNA polymerase forming the corresponding fluorescent labeled DNA which is useful for a DNA probe. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00111-7

    authors： Obayashi T,Masud MM,Ozaki AN,Ozaki H,Kuwahara M,Sawai H

    更新日期：2002-04-22 00:00:00

  • Selective inhibition of monoamine oxidase A by chelerythrine, an isoquinoline alkaloid.

    abstract：:Chelerythrine, an isoquinoline alkaloid isolated from the herbaceous perennial Chelidonium majus, was found to potently and selectively inhibit an isoform of recombinant human monoamine oxidase-A (MAO-A) with an IC50 value of 0.55 µM. Chelerythrine was a reversible competitive MAO-A inhibitor (Ki = 0.22 µM) with a pot...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.06.023

    authors： Baek SC,Ryu HW,Kang MG,Lee H,Park D,Cho ML,Oh SR,Kim H

    更新日期：2018-08-01 00:00:00

  • [(13)C3,(15)N1]-labeled isodesmosine: A potential internal standard for LC-MS/MS analysis of desmosines in elastin degradation.

    abstract：:Isodesmosine and desmosine are crosslinking amino acids that are present only in elastin. They are useful biomarkers for the degradation of elastin, which occurs during the progression of chronic obstructive pulmonary disease (COPD) and related diseases. This Letter describes the synthesis of [(13)C3,(15)N1]-labeled i...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.03.084

    authors： Tanigawa T,Komatsu A,Usuki T

    更新日期：2015-01-01 00:00:00

  • Elucidation of antimicrobial activity and mechanism of action by N-substituted carbazole derivatives.

    abstract：:Compounds belonging to a carbazole series have been identified as potent fungal plasma membrane proton adenosine triphophatase (H+-ATPase) inhibitors with a broad spectrum of antifungal activity. The carbazole compounds inhibit the adenosine triphosphate (ATP) hydrolysis activity of the essential fungal H+-ATPase, the...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.08.067

    authors： Clausen JD,Kjellerup L,Cohrt KO,Hansen JB,Dalby-Brown W,Winther AL

    更新日期：2017-10-01 00:00:00

  • Synthesis and antimalarial activity of 2-methoxyprop-2-yl peroxides derivatives.

    abstract：:2-Methoxyprop-2-yl peroxides were synthesized and evaluated in vitro against Plasmodium falciparum. These acyclic artemisinin-related peroxides revealed moderate to good activity but were devoid of alkylating property towards the synthetic model of heme Mn(II)-TPP. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00837-5

    authors： Cointeaux L,Berrien JF,Peyrou V,Provot O,Ciceron L,Danis M,Robert A,Meunier B,Mayrargue J

    更新日期：2003-01-06 00:00:00

  • Evaluation of PNU-159682 antibody drug conjugates (ADCs).

    abstract：:PNU-159682 is a highly potent secondary metabolite of nemorubicin belonging to the anthracycline class of natural products. Due to its extremely high potency and only partially understood mechanism of action, it was deemed an interesting starting point for the development of a new suite of linker drugs for antibody dr...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2020.127640

    authors： Holte D,Lyssikatos JP,Valdiosera AM,Swinney Z,Sisodiya V,Sandoval J,Lee C,Aujay MA,Tchelepi RB,Hamdy OM,Gu C,Lin B,Sarvaiya H,Pysz MA,Laysang A,Williams S,Jun Lee D,Holda MK,Purcell JW,Gavrilyuk J

    更新日期：2020-12-15 00:00:00

  • Absolute configurations of tubulin inhibitors taltobulin (HTI-286) and HTI-042 characterized by X-ray diffraction analysis and NMR studies.

    abstract：:The stereochemistry of the tubulin inhibitors taltobulin HTI-286 (2) and HTI-042 (3) was determined by utilizing the DPFGSE 1D NOE experiment. Single crystal X-ray diffraction analysis further confirmed the absolute configuration of these two compounds, which carry the (S,S,S)-configuration necessary for biological ac...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.01.047

    authors： Niu C,Ho DM,Williamson RT,Zask A,Ayral-Kaloustian S

    更新日期：2010-03-01 00:00:00

  • Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.

    abstract：:Analogues related to dirlotapide (1), a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) were prepared with the goal of further reducing the potential for unwanted liver MTP inhibition and associated side-effects. Compounds were designed to decrease active metabolite load: reducing MTP activit...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.05.099

    authors： Robinson RP,Bartlett JA,Bertinato P,Bessire AJ,Cosgrove J,Foley PM,Manion TB,Minich ML,Ramos B,Reese MR,Schmahai TJ,Swick AG,Tess DA,Vaz A,Wolford A

    更新日期：2011-07-15 00:00:00

  • Synthesis of novel 2-pyrazoline analogues with potent anti-inflammatory effect mediated by inhibition of phospholipase A2: Crystallographic, in silico docking and QSAR analysis.

    abstract：:Oxidative-stress induces inflammatory diseases. Further, infections caused by drug-resistant microbial strains are on the rise. This necessitates the discovery of novel small-molecules for intervention therapy. A series of 3-(2,3-dichlorophenyl)-1-(aryl)prop-2-en-1-ones are synthesized as intermediates via Claisen-Sch...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.06.063

    authors： Lokeshwari DM,Achutha DK,Srinivasan B,Shivalingegowda N,Krishnappagowda LN,Kariyappa AK

    更新日期：2017-08-15 00:00:00

  • Carboxy derivatized glucosamine is a potent inhibitor of matrix metalloproteinase-9 in HT1080 cells.

    abstract：:Experimental evidences have confirmed that matrix metalloproteinases (MMPs) play a fundamental role in a wide variety of pathologic conditions and recent advances in medicinal chemistry approach to the design of MMP inhibitors with desired structural and functional properties. Among MMPs, MMP-9 has demonstrated to pla...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.03.077

    authors： Mendis E,Kim MM,Rajapakse N,Kim SK

    更新日期：2006-06-15 00:00:00

  • The food-grade antimicrobial xanthorrhizol targets the enoyl-ACP reductase (FabI) in Escherichia coli.

    abstract：:Xanthorrhizol, isolated from the Indonesian Java turmeric Curcuma xanthorrhiza, displays broad-spectrum antibacterial activity. We report herein the evidence that mechanism of action of xanthorrhizol may involve FabI, an enoyl-(ACP) reductase, inhibition. The predicted Y156V substitution in the FabI enzyme promoted xa...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2020.127651

    authors： Yogiara,Mordukhova EA,Kim D,Kim WG,Hwang JK,Pan JG

    更新日期：2020-12-15 00:00:00

  • Submonomer synthesis of azapeptide ligands of the Insulin Receptor Tyrosine Kinase domain.

    abstract：:Azapeptide ligands of the Insulin Receptor Tyrosine Kinase (IRTK) were developed by solid-phase submonomer azapeptide synthesis in sufficient isolated yields (36-55%) and purities >95% for structure-activity relationship studies. The azapeptides adopted folded geometries with some proportion of random coil according t...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.07.046

    authors： Kurian LA,Silva TA,Sabatino D

    更新日期：2014-09-01 00:00:00

  • Synthesis of C-5a-chain extended derivatives of 4-epi-isofagomine: Powerful β-galactosidase inhibitors and low concentration activators of GM1-gangliosidosis-related human lysosomal β-galactosidase.

    abstract：:From an easily available partially protected formal derivative of 1-deoxymannojirimycin, by hydroxymethyl chain-branching and further elaboration, lipophilic analogs of the powerful β-d-galactosidase inhibitor 4-epi-isofagomine have become available. New compounds exhibit improved inhibitory activities comparable to b...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.01.059

    authors： Thonhofer M,Weber P,Santana AG,Fischer R,Pabst BM,Paschke E,Schalli M,Stütz AE,Tschernutter M,Windischhofer W,Withers SG

    更新日期：2016-03-01 00:00:00

  • 8-Methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines: highly potent in vivo AMPA antagonists.

    abstract：:A novel series of readily water soluble 8-methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]++ +pyrazines were synthesized. The -10-yl acetic acid ((+)-3) and -10-carboxylidene (4) derivatives exhibit potent affinities (IC50=4 and 19 nM, respectively) and antagonist properties (IC50 = 2 and 3 nM, respectiv...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00054-8

    authors： Mignani S,Bohme GA,Boireau A,Cheve M,Damour D,Debono MW,Genevois-Borella A,Imperato A,Jimonet P,Pratt J,Randle JC,Ribeill Y,Vuilhorgne M,Stutzmann JM

    更新日期：2000-03-20 00:00:00

  • Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

    abstract：:A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.01.021

    authors： Skerlj R,Bridger G,McEachern E,Harwig C,Smith C,Kaller A,Veale D,Yee H,Skupinska K,Wauthy R,Wang L,Baird I,Zhu Y,Burrage K,Yang W,Sartori M,Huskens D,De Clercq E,Schols D

    更新日期：2011-03-01 00:00:00

  • Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).

    abstract：:A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K(i)'s against SYK and potent inhibition in mast cell degranulation assays. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.09.106

    authors： Farmer LJ,Bemis G,Britt SD,Cochran J,Connors M,Harrington EM,Hoock T,Markland W,Nanthakumar S,Taslimi P,Ter Haar E,Wang J,Zhaveri D,Salituro FG

    更新日期：2008-12-01 00:00:00

  • Synthesis and fluorescent study of 5-phenyl furocoumarin derivatives as vasodilatory agents.

    abstract：:Two series of 5-phenyl furocoumarin derivatives were designed and prepared based on our previous research. All new compounds were characterized by (1)H NMR, (13)C NMR and mass spectra. Furthermore, they were screened for their vasodilatory activity on the mesenteric artery of Sprague-Dawley rats, and they all presente...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.11.056

    authors： Wang C,Wang T,Huang L,Lu W,Zhang J,He H

    更新日期：2016-01-15 00:00:00

  • Synthesis and anti-BVDV activity of novel δ-sultones in vitro: implications for HCV therapies.

    abstract：:In this study we report the synthesis and activity against bovine viral diarrhea virus (BVDV) of a novel series of bicycle δ-sultones containing γ-lactones. BVDV is responsible for major losses in cattle. Some of the synthesized δ-sultones showed pronounced anti-BVDV activity with EC50 values of 0.12-1.0μM and no sign...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.03.012

    authors： Xu HW,Zhao LJ,Liu HF,Zhao D,Luo J,Xie XP,Liu WS,Zheng JX,Dai GF,Liu HM,Liu LH,Liang YB

    更新日期：2014-05-15 00:00:00

  • Synthesis and biological activity of 4-substituted benzoxazolone derivatives as a new class of sEH inhibitors with high anti-inflammatory activity in vivo.

    abstract：:A series of novel 4-substituted benzoxazolone derivatives was synthesized, characterized and evaluated as human soluble epoxide hydrolase (sEH) inhibitors and anti-inflammatory agents. Some compounds showed moderate sEH inhibitory activities in vitro, and two novel compounds, 3g and 4j, exhibited the highest activitie...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.02.048

    authors： Tang L,Ma WH,Ma YL,Ban SR,Feng XE,Li QS

    更新日期：2013-04-15 00:00:00

  • A novel mitochondria-localizing nitrobenzene derivative as a donor for photo-uncaging of nitric oxide.

    abstract：:We report a novel green-fluorescent NO donor, NBDNO, bearing a 2,6-dimethylnitrobenzene moiety for photocontrollable NO release and a triphenylphosphonium moiety for targeting to mitochondria. Photorelease of NO from NBDNO was confirmed by means of ESR analysis in aqueous solution. Intracellular release of NO from NBD...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.02.027

    authors： Horinouchi T,Nakagawa H,Suzuki T,Fukuhara K,Miyata N

    更新日期：2011-04-01 00:00:00