Author Archive

What are your colleagues reading in MedChemComm?

The articles below are some of the most read MedChemComm articles in April, May and June 2017.

Review Articles:

Multivalent glycoconjugates as vaccines and potential drug candidates
Sumati Bhatia, Mathias Dimde and Rainer Haag
DOI: 10.1039/C4MD00143E

Surface plasmon resonance for the characterization of bacterial polysaccharide antigens: a review
Barbara Brogioni and Francesco Berti
DOI: 10.1039/C4MD00088A

Recent advances in the rational design and optimization of antibacterial agents
Jesse A. Jones, Kristopher G. Virga, Giuseppe Gumina and Kirk E. Hevener
DOI: 10.1039/C6MD00232C

Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospects
Isidro Cortés-Ciriano, Qurrat Ul Ain, Vigneshwari Subramanian, Eelke B. Lenselink, Oscar Méndez-Lucio, Adriaan P. IJzerman, Gerd Wohlfahrt, Peteris Prusis, Thérèse E. Malliavin, Gerard J. P. van Westen and Andreas Bender
DOI: 10.1039/C4MD00216D

Protein–ligand (un)binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling
M. Bernetti, A. Cavalli and L. Mollica
DOI: 10.1039/C6MD00581K

Structural biology and chemistry of protein arginine methyltransferases
Matthieu Schapira and Renato Ferreira de Freitas
DOI: 10.1039/C4MD00269E

Small molecule-mediated protein knockdown as a new approach to drug discovery
Christopher P. Tinworth, Hannah Lithgow and Ian Churcher
DOI: 10.1039/C6MD00347H

Chemical probes and inhibitors of bromodomains outside the BET family
Moses Moustakim, Peter G. K. Clark, Duncan A. Hay, Darren J. Dixon and Paul E. Brennan
DOI: 10.1039/C6MD00373G

Amphiphilic designer nano-carriers for controlled release: from drug delivery to diagnostics
Malinda Salim, Hiroyuki Minamikawa, Akihiko Sugimura and Rauzah Hashim
DOI: 10.1039/C4MD00085D

2-[18F]Fluoroethyl tosylate – a versatile tool for building 18F-based radiotracers for positron emission tomography
Torsten Kniess, Markus Laube, Peter Brust and Jörg Steinbach
DOI: 10.1039/C5MD00303B

Structural features of many circular and leaderless bacteriocins are similar to those in saposins and saposin-like peptides
K. M. Towle and J. C. Vederas
DOI: 10.1039/C6MD00607H

Bacterial lipid membranes as promising targets to fight antimicrobial resistance, molecular foundations and illustration through the renewal of aminoglycoside antibiotics and emergence of amphiphilic aminoglycosides
Marie-Paule Mingeot-Leclercq and Jean-Luc Décout
DOI: 10.1039/C5MD00503E

Research Articles:

Towards understanding cell penetration by stapled peptides
Qian Chu, Raymond E. Moellering, Gerard J. Hilinski, Young-Woo Kim, Tom N. Grossmann, Johannes T.-H. Yeh and Gregory L. Verdine
DOI: 10.1039/C4MD00131A

Design and synthesis of DNA-encoded libraries based on a benzodiazepine and a pyrazolopyrimidine scaffold
M. Klika Škopić, O. Bugain, K. Jung, S. Onstein, S. Brandherm, T. Kalliokoski and A. Brunschweiger
DOI: 10.1039/C6MD00243A

Methods of protein surface PEGylation under structure preservation for the emulsion-based formation of stable nanoparticles
Lydia Radi, Matthias Fach, Mirko Montigny, Elena Berger-Nicoletti, Wolfgang Tremel and Peter R. Wich
DOI: 10.1039/C5MD00475F

Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling
R. Moslin, D. Gardner, J. Santella, Y. Zhang, J. V. Duncia, C. Liu, J. Lin, J. S. Tokarski, J. Strnad, D. Pedicord, J. Chen, Y. Blat, A. Zupa-Fernandez, L. Cheng, H. Sun, C. Chaudhry, C. Huang, C. D’Arienzo, J. S. Sack, J. K. Muckelbauer, C. Chang, J. Tredup, D. Xie, N. Aranibar, J. R. Burke, P. H. Carter and D. S. Weinstein
DOI: 10.1039/C6MD00560H

Exploring the links between peptoid antibacterial activity and toxicity
H. L. Bolt, G. A. Eggimann, C. A. B. Jahoda, R. N. Zuckermann, G. J. Sharples and S. L. Cobb
DOI: 10.1039/C6MD00648E

Nonomuraea sp. ATCC 55076 harbours the largest actinomycete chromosome to date and the kistamicin biosynthetic gene cluster
Behnam Nazari, Clarissa C. Forneris, Marcus I. Gibson, Kyuho Moon, Kelsey R. Schramma and Mohammad R. Seyedsayamdost
DOI: 10.1039/C6MD00637J

Structure-based virtual screening for fragment-like ligands of the G protein-coupled histamine H4 receptor
Enade P. Istyastono, Albert J. Kooistra, Henry F. Vischer, Martien Kuijer, Luc Roumen, Saskia Nijmeijer, Rogier A. Smits, Iwan J. P. de Esch, Rob Leurs and Chris de Graaf
DOI: 10.1039/C5MD00022J

Human lysosomal acid lipase inhibitor lalistat impairs Mycobacterium tuberculosis growth by targeting bacterial hydrolases
J. Lehmann, J. Vomacka, K. Esser, M. Nodwell, K. Kolbe, P. Rämer, U. Protzer, N. Reiling and S. A. Sieber
DOI: 10.1039/C6MD00231E

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains
Duncan A. Hay, Catherine M. Rogers, Oleg Fedorov, Cynthia Tallant, Sarah Martin, Octovia P. Monteiro, Susanne Müller, Stefan Knapp, Christopher J. Schofield and Paul E. Brennan
DOI: 10.1039/C5MD00152H

A fundamental view of enthalpy–entropy compensation
Ulf Ryde
DOI: 10.1039/C4MD00057A

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor
Katherine S. England, Anthony Tumber, Tobias Krojer, Giuseppe Scozzafava, Stanley S. Ng, Michelle Daniel, Aleksandra Szykowska, KaHing Che, Frank von Delft, Nicola A. Burgess-Brown, Akane Kawamura, Christopher J. Schofield and Paul E. Brennan
DOI: 10.1039/C4MD00291A

From linked open data to molecular interaction: studying selectivity trends for ligands of the human serotonin and dopamine transporter
Barbara Zdrazil, Eva Hellsberg, Michael Viereck and Gerhard F. Ecker
DOI: 10.1039/C6MD00207B

Keep up-to-date with the latest issues of MedChemComm with our E-alerts

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What are your colleagues reading in MedChemComm?

The articles below are some of the most read MedChemComm articles in January, February and March 2016.

Multivalent glycoconjugates as vaccines and potential drug candidates
Sumati Bhatia, Mathias Dimde and Rainer Haag
DOI: 10.1039/C4MD00143E, Review Article

Thermoresponsive fluorinated small-molecule drugs: a new concept for efficient localized chemotherapy
Catherine M. Clavel, Patrycja Nowak-Sliwinska, Emilia Păunescu and Paul J. Dyson
DOI: 10.1039/C5MD00409H, Review Article

Mechanisms of resistance to membrane-disrupting antibiotics in Gram-positive and Gram-negative bacteria
Kfir B. Steinbuch and Micha Fridman
DOI: 10.1039/C5MD00389J, Review Article

Endless resistance. Endless antibiotics?
Jed F. Fisher and Shahriar Mobashery
DOI: 10.1039/C5MD00394F, Review Article

Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospects
Isidro Cortés-Ciriano, Qurrat Ul Ain, Vigneshwari Subramanian, Eelke B. Lenselink, Oscar Méndez-Lucio, Adriaan P. IJzerman, Gerd Wohlfahrt, Peteris Prusis, Thérèse E. Malliavin, Gerard J. P. van Westen and Andreas Bender
DOI: 10.1039/C4MD00216D, Review Article

Surface plasmon resonance for the characterization of bacterial polysaccharide antigens: a review
Barbara Brogioni and Francesco Berti
DOI: 10.1039/C4MD00088A, Review Article

Towards understanding cell penetration by stapled peptides
Qian Chu, Raymond E. Moellering, Gerard J. Hilinski, Young-Woo Kim, Tom N. Grossmann, Johannes T.-H. Yeh and Gregory L. Verdine
DOI: 10.1039/C4MD00131A, Concise Article

Rational design of protein–protein interaction inhibitors
Didier Rognan
DOI: 10.1039/C4MD00328D, Review Article

Identification of an inhibitor of the ubiquitin–proteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
Caroline Haglund, Chitralekha Mohanty, Mårten Fryknäs, Padraig D’Arcy, Rolf Larsson, Stig Linder and Linda Rickardson
DOI: 10.1039/C3MD00386H, Concise Article

Mechanisms of resistance to aminoglycoside antibiotics: overview and perspectives
Sylvie Garneau-Tsodikova and Kristin J. Labby
DOI: 10.1039/C5MD00344J, Review Article

(more…)

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What are your colleagues reading in MedChemComm?

The articles below are the most read MedChemComm articles in July, August and September 2015.

Transition metal diamine complexes with antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA)
G. W. Karpin, D. M. Morris, M. T. Ngo, J. S. Merola and J. O. Falkinham III
DOI: 10.1039/C5MD00228A, Concise Article

Multivalent glycoconjugates as vaccines and potential drug candidates
Sumati Bhatia, Mathias Dimde and Rainer Haag
DOI: 10.1039/C4MD00143E, Review Article

Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospects
Isidro Cortés-Ciriano, Qurrat Ul Ain, Vigneshwari Subramanian, Eelke B. Lenselink, Oscar Méndez-Lucio, Adriaan P. IJzerman, Gerd Wohlfahrt, Peteris Prusis, Thérèse E. Malliavin, Gerard J. P. van Westen and Andreas Bender
DOI: 10.1039/C4MD00216D, Review Article

Towards understanding cell penetration by stapled peptides
Qian Chu, Raymond E. Moellering, Gerard J. Hilinski, Young-Woo Kim, Tom N. Grossmann, Johannes T.-H. Yeh and Gregory L. Verdine
DOI: 10.1039/C4MD00131A, Concise Article

Rational design of protein–protein interaction inhibitors
Didier Rognan
DOI: 10.1039/C4MD00328D, Review Article

Magic molecule modifiers
Derek Lowe
DOI: 10.1039/C5MD90028J, In the Pipeline

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor
Katherine S. England, Anthony Tumber, Tobias Krojer, Giuseppe Scozzafava, Stanley S. Ng, Michelle Daniel, Aleksandra Szykowska, KaHing Che, Frank von Delft, Nicola A. Burgess-Brown, Akane Kawamura, Christopher J. Schofield and Paul E. Brennan
DOI: 10.1039/C4MD00291A, Concise Article

Identification of an inhibitor of the ubiquitin–proteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
Caroline Haglund, Chitralekha Mohanty, Mårten Fryknäs, Padraig D’Arcy, Rolf Larsson, Stig Linder and Linda Rickardson
DOI: 10.1039/C3MD00386H, Concise Article

Amphiphilic designer nano-carriers for controlled release: from drug delivery to diagnostics
Malinda Salim, Hiroyuki Minamikawa, Akihiko Sugimura and Rauzah Hashim
DOI: 10.1039/C4MD00085D, Review Article

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains
Duncan A. Hay, Catherine M. Rogers, Oleg Fedorov, Cynthia Tallant, Sarah Martin, Octovia P. Monteiro, Susanne Müller, Stefan Knapp, Christopher J. Schofield and Paul E. Brennan
DOI: 10.1039/C5MD00152H, Concise Article

(more…)

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Poster Prize Winners at EuCheMS Conference

Congratulations to the Poster Prize winners at the 6th EuCheMS Conference on Nitrogen Ligands!

The winners are:

Sophie Laine (MedChemComm) – “Potential MRI Contrast Agent for Enzymatic Detection”

Neeladri Das (Chemical Science) – “Pyrazinc Based Tectons in the Self-Assembly of Finite Two­ Dimensional Supramolecular  Ensembles”

Nicole Kindermann (Dalton Transactions) – “A dicopper pyrazole/tacn system and its diOX) gcn chemistry”

Florian Schendzielorz (Dalton Transactions) – “A Well Characterized Osmium(IV)-Nitrido  Complex in a Square­ Planar  Coordination Geometry”

Charles Lochenie (Dalton Transactions) – “Synergetic effects between spin state change and fluorescent properties of Schiff base-like 3d metal complexes”

Amandine Conte-Daban (Inorganic Chemistry Frontiers) – “A new probe to determine the affini ty constant of Cu 2+ for A”

Yasin Kuzu (Inorganic Chemistry Frontiers) – “Planar ChiraJ 2-(N ,N-Dimethylaminomethyl)-1-(trimethyl­silyl)ferrocenyl Substitu ted Silanols,Silanolates and Siloxanes”

Maxim A Faraonov (Materials Horizons) – “Crystalline Salts with Radical Anions of Metal-containing and Metal­ free Pbthalocya nincs:Synthesis, Crystal Structures, Optical and Magnetic Properties”

The conference was held from 13th – 17th September in Beaune, France.  The conference aims to attract scientists with an interest in the field of metal-nitrogen ligand chemistry.  This year it also included these topics: the recent advances in the fields of coordination chemistry, metal-organic chemistry, bioinorganic chemistry, and materials & catalysis.

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