当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Exploration of GGTase-I substrate requirements. Part 1: Synthesis and biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs.

Exploration of GGTase-I substrate requirements. Part 1: Synthesis and biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs.

Abstract：

:Protein geranylgeranylation is a type of post-translational modification that aids in the localization of proteins to the plasma member where they elicit cellular signals. To better understand the isoprenoid requirements of GGTase-I, a series of aryl-modified geranylgeranyl diphosphate analogs were synthesized and screened against mammalian GGTase-I. Of our seven-member library of compounds, six analogs proved to be substrates of GGTase-I, with 6d having a krel=1.93 when compared to GGPP (krel=1.0).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Temple KJ,Wright EN,Fierke CA,Gibbs RA

doi

10.1016/j.bmcl.2016.06.034

subject

Has Abstract

pub_date

2016-08-01 00:00:00

pages

3499-502

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)30645-X

journal_volume

26

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Synthesis of a Streptococcus pyogenes vaccine candidate based on the M protein PL1 epitope.

    abstract：:Group A streptococcus is a Gram-positive bacteria that causes a range of infectious diseases. Targeting the bacteria, a new self-adjuvanting vaccine candidate, incorporating a carbohydrate carrier and an amino acid-based adjuvant, was synthesised utilising carbohydrate chemistry and solid-phase peptide synthesis proce...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.12.013

    authors： Simerska P,Lu H,Toth I

    更新日期：2009-02-01 00:00:00

  • Synthesis and biological evaluation of new symmetric curcumin derivatives.

    abstract：:A series of novel curcumin bisacetamides aiming of enriching their biological activities have been synthesized. The synthesized compounds were screened for their in vitro antioxidant, anti-inflammatory and cytotoxic activities. All the compounds exhibited potent to good anti-inflammatory, antioxidant and noteworthy cy...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.07.088

    authors： Sribalan R,Kirubavathi M,Banuppriya G,Padmini V

    更新日期：2015-10-01 00:00:00

  • Activation of antibacterial prodrugs by peptide deformylase.

    abstract：:5'-Dipeptidyl derivatives of 5-fluorodeoxyuridine (FdU) (1a-d) were synthesized. These compounds are biologically inactive but can be activated by peptide deformylase, which removes the N-terminal formyl group of the dipeptide, to release the active drug FdU via an intramolecular cyclization reaction. Because the defo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00167-0

    authors： Wei Y,Pei D

    更新日期：2000-05-15 00:00:00

  • Trace amine-associated receptor 1 (TAAR1) is activated by amiodarone metabolites.

    abstract：:Amiodarone (Cordarone, Wyeth-Ayerst Pharmaceuticals) is a clinically available drug used to treat a wide variety of cardiac arrhythmias. We report here the synthesis and characterization of a panel of potential amiodarone metabolites that have significant structural similarity to thyroid hormone and its metabolites th...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.08.013

    authors： Snead AN,Miyakawa M,Tan ES,Scanlan TS

    更新日期：2008-11-15 00:00:00

  • N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.

    abstract：:A new class of potent NK3R antagonists based on the N',2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ(90) 30 mg/kg po; plasma Occ(90) 0.95 microM) and has good selectivity and promising PK properti...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.08.086

    authors： Elliott JM,Carling RW,Chambers M,Chicchi GG,Hutson PH,Jones AB,MacLeod A,Marwood R,Meneses-Lorente G,Mezzogori E,Murray F,Rigby M,Royo I,Russell MG,Sohal B,Tsao KL,Williams B

    更新日期：2006-11-15 00:00:00

  • Multiple-step, one-pot synthesis of 2-substituted-3-phosphono-1-thia-4-aza-2-cyclohexene-5-carboxylates and their corresponding ethyl esters.

    abstract：:The multiple-step, one-pot procedure for a series of 2-substituted-3-phosphono-1-thia-4-aza-2-cyclohexene-5-carboxylates, analogues of the natural, sulfur amino acid metabolite lanthionine ketimine (LK), its 5-ethyl ester (LKE) and 2-substituted LKEs is described. Initiating the synthesis with the Michaelis-Arbuzov pr...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.01.052

    authors： Shen D,Hensley K,Denton TT

    更新日期：2018-02-15 00:00:00

  • Synthesis of new bergenin derivatives as potent inhibitors of inflammatory mediators NO and TNF-α.

    abstract：:Bergenin is an isocoumarin natural product which aides in fat loss, healthy weight maintenance, enhancing the lipolytic effects of norepinephrine, inhibiting the formation of interleukin 1α and cyclooxygenases-2. Here we describe the anti-inflammatory activity of new bergenin derivatives 1-15 in the respiratory burst ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.02.096

    authors： Shah MR,Arfan M,Amin H,Hussain Z,Qadir MI,Choudhary MI,VanDerveer D,Mesaik MA,Soomro S,Jabeen A,Khan IU

    更新日期：2012-04-15 00:00:00

  • Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14).

    abstract：:Our series of competitive antagonists against the G-protein coupled receptor P2Y(14) were found to be highly shifted in the presence of serum (>99% protein bound). A binding assay using 2% human serum albumin (HSA) was developed to guide further SAR studies and led to the identification of the zwitterion 2, which is s...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.12.113

    authors： Robichaud J,Fournier JF,Gagné S,Gauthier JY,Hamel M,Han Y,Hénault M,Kargman S,Levesque JF,Mamane Y,Mancini J,Morin N,Mulrooney E,Wu J,Black WC

    更新日期：2011-07-15 00:00:00

  • Pleuromutilin derivatives having a purine ring. Part 1: new compounds with promising antibacterial activity against resistant Gram-positive pathogens.

    abstract：:In the course of our research aimed at the discovery of metabolic stable pleuromutilin derivatives with more potent antibacterial activity against Gram-positive pathogens than previous analogues, a series of compounds bearing a purine ring were prepared and evaluated. From SAR studies, we identified two promising comp...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.05.011

    authors： Hirokawa Y,Kinoshita H,Tanaka T,Nakamura T,Fujimoto K,Kashimoto S,Kojima T,Kato S

    更新日期：2008-06-15 00:00:00

  • Enantioselective synthesis of (R)-(+)- and (S)-(-)-higenamine and their analogues with effects on platelet aggregation and experimental animal model of disseminated intravascular coagulation.

    abstract：:Optically active tetrahydroisoquinoline alkaloids, (R)-(+)-higenamine (1R) and (S)-(-)-higenamine (1 S), and their optically active 1-naphthylmethyl analogues (2 and 3), were synthesized by enantioselective hydrogenation of the corresponding dihydroisoquinoline intermediates 7 as a key step. The evaluation of the plat...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.05.094

    authors： Pyo MK,Lee DH,Kim DH,Lee JH,Moon JC,Chang KC,Yun-Choi HS

    更新日期：2008-07-15 00:00:00

  • Structure-based engineering of benzalacetone synthase.

    abstract：:Benzalacetone synthase (BAS) and chalcone synthase (CHS) are plant-specific type III polyketide synthases (PKSs), sharing 70% amino acid sequence identity and highly homologous overall protein structures. BAS catalyzes the decarboxylative coupling of 4-coumaroyl-CoA with malonyl-CoA to produce the diketide benzalaceto...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.07.022

    authors： Shimokawa Y,Morita H,Abe I

    更新日期：2010-09-01 00:00:00

  • Structure-activity relationships of novel potent MurF inhibitors.

    abstract：:A novel class of MurF inhibitors was discovered and structure-activity relationship studies have led to several potent compounds with IC(50)=22 approximately 70 nM. Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.09.073

    authors： Gu YG,Florjancic AS,Clark RF,Zhang T,Cooper CS,Anderson DD,Lerner CG,McCall JO,Cai Y,Black-Schaefer CL,Stamper GF,Hajduk PJ,Beutel BA

    更新日期：2004-01-05 00:00:00

  • In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis.

    abstract：:A group of sixteen iridoids isolated from plants used as anti-inflammatory remedies in Mexican folk medicine were evaluated for their potential to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. From these assays, loganic acid (10) was identified as the most promising compound with both COX-1 (3...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.08.075

    authors： Ramírez-Cisneros MÁ,Rios MY,Aguilar-Guadarrama AB,Rao PP,Aburto-Amar R,Rodríguez-López V

    更新日期：2015-10-15 00:00:00

  • Novel fluorescent oligoDNA probe bearing a multi-conjugated nucleoside with a fluorophore and a non-fluorescent intercalator as a quencher.

    abstract：:A set of 15mer linear oligoDNA probes bearing a modified nucleoside conjugated with a polyamine/fluorescein/anthraquinone reporting moiety were synthesized. In a single-stranded form, the fluorescence generated by the excitation of fluorescein was efficiently quenched, while marked recovery of the fluorescence was obs...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.02.016

    authors： Kodama S,Asano S,Moriguchi T,Sawai H,Shinozuka K

    更新日期：2006-05-15 00:00:00

  • Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

    abstract：:Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in a mouse MCF7 xenograft model. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.04.124

    authors： Staben ST,Siu M,Goldsmith R,Olivero AG,Do S,Burdick DJ,Heffron TP,Dotson J,Sutherlin DP,Zhu BY,Tsui V,Le H,Lee L,Lesnick J,Lewis C,Murray JM,Nonomiya J,Pang J,Prior WW,Salphati L,Rouge L,Sampath D,Sideris S,

    更新日期：2011-07-01 00:00:00

  • Synthetic studies on selective adenosine A2A receptor antagonists. Part II: synthesis and structure-activity relationships of novel benzofuran derivatives.

    abstract：:Based on the previously reported lead compound, a series of benzofuran derivatives were prepared to study their antagonistic activities to A(2A) receptor. The replacement of the phenyl group at the 4-position with a heterocyclic ring improved the PK profile and aqueous solubility. From these studies, we discovered a p...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.04.058

    authors： Saku O,Saki M,Kurokawa M,Ikeda K,Uchida S,Takizawa T,Uesaka N

    更新日期：2010-06-15 00:00:00

  • Optimization of the enzymatic synthesis of O-glycan core 2 structure by use of a genetic algorithm.

    abstract：:The enzymatic synthesis of Gal-beta 1,3[GlcNAc-beta 1,6]-GalNAc-alpha 1-OBn (core 2-Bn) using a multi-enzyme system consisting of a beta-galactosidase (EC 3.2.1.23) from bovine testes and a recombinant core 2 beta 1,6-GlcNAc transferase (C2GnT, EC 2.4.1.102) was empirically optimized by the use of a genetic algorithm....

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00087-2

    authors： Hoh C,Dudziak G,Liese A

    更新日期：2002-04-08 00:00:00

  • Discovery of ITX 4520: a highly potent orally bioavailable hepatitis C virus entry inhibitor.

    abstract：:The manuscript reports an identification of a highly potent, orally bioavailable hepatitis C virus entry inhibitor through optimization of a previously reported class of molecules (1) that were not stable in the rat plasma. Compound 39 (ITX 4520) exhibited an excellent PK profile in both rats and dogs with good oral e...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.06.038

    authors： Mittapalli GK,Zhao F,Jackson A,Gao H,Lee H,Chow S,Kaur MP,Nguyen N,Zamboni R,McKelvy J,Wong-Staal F,Macdonald JE

    更新日期：2012-08-01 00:00:00

  • Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.

    abstract：:Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the e...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.06.091

    authors： Bollini M,Cisneros JA,Spasov KA,Anderson KS,Jorgensen WL

    更新日期：2013-09-15 00:00:00

  • Anti-inflammatory isoflavones and isoflavanones from the roots of Pongamia pinnata (L.) Pierre.

    abstract：:A phytochemical study on the roots of Pongamia pinnata afforded five new isoflavone and isoflavanone derivatives (1-5), including two previously undescribed phenylisoflavones possessing an 1,2-oxetane ring, along with 21 known compounds (6-26) among which compound 18 is the first time to be isolated from nature. The s...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.02.026

    authors： Wen R,Lv H,Jiang Y,Tu P

    更新日期：2018-04-01 00:00:00

  • Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.

    abstract：:A novel series of 5-HT(7) receptor ligands has been identified and evaluated, providing compounds showing a broad spectrum of functional activities and good selectivity over selected receptors and ion channels. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.11.067

    authors： Raubo P,Beer MS,Hunt PA,Huscroft IT,London C,Stanton JA,Kulagowski JJ

    更新日期：2006-03-01 00:00:00

  • Cu2+-labeled dansyl compounds as fluorescent and PET probes for imaging apoptosis.

    abstract：:Compound DNSTT-Cu2+, a novel chelate of Cu2+ with DOTA conjugated to a fluorescent dansyl fragment, is developed for imaging cell apoptosis. Apoptotic U-87MG cells could be selectively visualized by the fluorescence of DNSTT-Cu2+ from cytoplasm of cells, confirmed by the fluorescence of apoptosis cells co-labeled with...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.09.057

    authors： Han J,Wang X,Yu M

    更新日期：2016-11-15 00:00:00

  • Adamantyl-tethered-biphenylic compounds induce apoptosis in cancer cells by targeting Bcl homologs.

    abstract：:Bcl homologs prominently contribute to apoptotic resistance in cancer cells and serve as molecular targets in treatment of various cancers. Herein, we report the synthesis of biphenyl-adamantane derivatives by a ligand free palladium on carbon based Suzuki reaction using diisopropylamine as a base for the coupling of ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.12.026

    authors： Anusha S,Mohan CD,Ananda H,Baburajeev CP,Rangappa S,Mathai J,Fuchs JE,Li F,Shanmugam MK,Bender A,Sethi G,Basappa,Rangappa KS

    更新日期：2016-02-01 00:00:00

  • Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives.

    abstract：:The Naturally occurring novel cyclohexanonyl bromophenol 2(R)-2-(2,3,6-tribromo-4,5-dihydroxybenzyl)cyclohexanone (4) was synthesized as a racemic compound. Cyclohexylphenyl methane derivatives (10-17) with Br, OMe, CO, and OH were also obtained. Inhibition of four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.12.069

    authors： Balaydın HT,Sentürk M,Menzek A

    更新日期：2012-02-01 00:00:00

  • Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.

    abstract：:A series of 1-aminotetralin scaffolds was synthesized via metal-catalyzed ring-opening reactions of heterobicyclic alkenes. Small libraries of amides and amines were made using the amino group of each scaffold as a handle. Screening of these libraries against human opioid receptors led to the identification of (S)-(S)...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.12.095

    authors： Dockendorff C,Jin S,Olsen M,Lautens M,Coupal M,Hodzic L,Spear N,Payza K,Walpole C,Tomaszewski MJ

    更新日期：2009-02-15 00:00:00

  • Structure based medicinal chemistry approach to develop 4-methyl-7-deazaadenine carbocyclic nucleosides as anti-HCV agent.

    abstract：:The structure-based approaches were implemented to design and rationally select the molecules for synthesis and anti-HCV activity evaluation. The systematic structure-activity relationships of previously discovered molecules (types I, II, III) were analyzed to design new molecules (type IV) by bioisosteric replacement...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.09.072

    authors： Thiyagarajan A,Salim MT,Balaraju T,Bal C,Baba M,Sharon A

    更新日期：2012-12-15 00:00:00

  • Effects of a novel carbocyclic analog of pyrrolo[2,3-d]pyrimidine nucleoside on pleiotropic induction of cell death in prostate cancer cells with different androgen responsiveness.

    abstract：:Prostate cancer is the most frequently diagnosed cancer and is one of the leading causes of male cancer death in the world. Recently, in the course of our screening for a novel anticancer compound, we synthesized carbocyclic analogs of pyrrolo[2,3-d]pyrimidine nucleoside; compounds 5, and 6. In the current study, we r...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.01.057

    authors： Suh H,Choi KW,Lee J,Ryou C,Rhee H,Lee CH

    更新日期：2016-02-15 00:00:00

  • Structural measurements and cell line studies of the copper-PEG-Rifampicin complex against Mycobacterium tuberculosis.

    abstract：:The bacterium responsible for tuberculosis is increasing its resistance to antibiotics resulting in new multidrug-resistant Mycobacterium tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB). In this study, several analytical techniques including NMR, FT-ICR, MALDI-MS, LC-MS and UV/Vis are used t...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.12.053

    authors： Manning T,Mikula R,Wylie G,Phillips D,Jarvis J,Zhang F

    更新日期：2015-02-01 00:00:00

  • Novel, potent and orally bioavailable indolizidinone-derived inhibitors of the hepatitis C virus NS3 protease.

    abstract：:A novel, potent, and orally bioavailable class of product-like inhibitors of the HCV NS3 protease was discovered by constraining the P2-P3 amide bond and the P3 hydrocarbon substituent to the protease-bound conformation. This preorganization was accomplished by incorporation of the P2-P3 amide into a six-membered ring...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.11.107

    authors： Clarke MO,Byun D,Chen X,Doerffler E,Leavitt SA,Sheng XC,Yang CY,Kim CU

    更新日期：2012-01-15 00:00:00

  • Synthesis of gibberellin derivatives with anti-tumor bioactivities.

    abstract：:A series of gibberellin based molecules were designed and synthesized. Gibberellin derivatives bearing two alpha,beta-unsaturated ketone units showed strong anticancer activities in MTT assay towards a number of human cancer cell lines including HT29, A549, HepG2 and MKN28. The most potent gibberellin derivative (comp...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.07.090

    authors： Chen J,Sun Z,Zhang Y,Zeng X,Qing C,Liu J,Li L,Zhang H

    更新日期：2009-09-15 00:00:00