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Property-based optimisation of PROTACs

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00769G, Opinion
James Scott, Iacovos Michaelides, Markus Schade
PROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical...
The content of this RSS Feed (c) The Royal Society of Chemistry




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3-Thio-3,4,5-Trisubstituted-1,2,4-Triazoles: High Affinity Somatostatin Receptor-4 Agonist Synthesis and Structure-Activity Relationships

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00597J, Research Article
Albert Michael Crider, Audrey Hospital, Karin Sandoval, William Neumann, Stephen Kukielski, Lejla Garic, Kristen Ingold, Matthew Dunahoo, Khush Srabony, Rafael Frare, Olivia Slater, Nathan Peel, Maria Kontoyianni, Ken Witt
Somatostatin receptor-4 (SST4) is a therapeutic target for several conditions, including Alzheimer’s disease, seizures, neuropsychiatric disorders, and pain. Our previous work on 1,2,4-triazole derivatives led to enhanced SST4 binding affinity,...
The content of this RSS Feed (c) The Royal Society of Chemistry




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A practical guide for the assay-dependent characterisation of irreversible inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00707G, Review Article
Lavleen K. Mader, Jessica E. Borean, Jeffrey W. Keillor
Kinetic evaluations for assay dependent characterization of irreversible inhibitors.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




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SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity Prediction

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00722K, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Maria Cristina Lomuscio, Nicola Corriero, Vittoria Nanna, Antonio Piccinno, Michele Saviano, Rosa Lanzilotti, Carmen Abate, Domenico Alberga, Giuseppe Felice Mangiatordi
Developing sigma-1 receptor (S1R) modulators is considered a valuable therapeutic strategy to counteract neurodegeneration, cancer progression, and viral infections, including COVID-19. In this context, in-silico tools capable of accurately predicting...
The content of this RSS Feed (c) The Royal Society of Chemistry




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Synthesis and antifungal evaluation of new azole derivatives containing 1,2,3-triazole

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00724G, Research Article
Zhengxiao Huang, Hongjie Chen, Xiao Zhang, Ruirui Wang, Chunyan Hu, Zewei Mao
A series of novel azole derivatives containing 1,2,3-triazole have been synthesized with good antifungal effects on sensitive and drug-resistant C. albicans.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Adjuvant strategies to tackle mcr-mediated polymyxin resistance

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00654B, Review Article
Madison R. Nuske, Junlang Zhong, Renjie Huang, Vijayalekshmi Sarojini, Jack L. Y. Chen, Christopher J. Squire, Mark A. T. Blaskovich, Ivanhoe K. H. Leung
The emergence of the mobile colistin resistance (mcr) gene is a significant threat contributing to the worldwide antibiotic resistance crisis. This review discusses adjuvant strategies to restore polymyxin sensitivity in these resistant bacteria.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




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U.S. Presidential polls: Thulasendrapuram residents pray for Kamala Harris ‘victory




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Will decide on sharing stage with actor Vijay in consultation with VCK leaders: Thirumavalavan

Mr. Thirumavalavan told reporters in Tiruchi that the book release event was not something that was planned recently, and that he had consented to take part in it almost a year ago




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50 new primary health centres to be opened in State soon: Minister




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Data crucial for building climate resilience, says ISRO scientist




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Heavy weed growth at Kasi Viswanathar Temple tank prevents replenishing of underground water table, say Tiruchi residents




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Tiruchi Today (November 7, 2024)




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Ensure time-bound implementation of development schemes, says Thirumavalavan




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Agro-tourism push needs industry-specific policies, say farmers




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Paddy crop loss compensation pegged at ₹36,500




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TNSTC Kumbakonam Division mops up ₹17.13 crore in four days




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Pumping stations to be set up in eight low-lying areas in Tiruchi to prevent inundation




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Case filed against actor Kasthuri over remarks on Telugu community




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Urban Primary Health Centre stuck in cramped, temporary facility




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Property owners block the entrance to Balasubramanya temple in Karur




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Govt. urged to extend last date to pay crop insurance premium by farmers




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Deputy CM releases commemorative flag of Bharat Scouts and Guides




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Udhayanidhi lays foundation stone for infrastructure development projects in Thanjavur district

Buildings at the Government Arts and Science College, Thirukkattupalli, construction of compound wall and an indoor stadium at the Government Rajah Serfoji College, Thanjavur, are among the projects




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Railways using treated water from its STP for maintaining green spaces

The treated water is stored in an overhead tank and used in gardens at the two railway rest houses meant for officers at Kallukuzhi near Tiruchi Railway Junction




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Tiruchi district SHGs compete to prepare healthy millet-based recipes at food festival

Women entrepreneurs urged to take advantage of social media platforms to advertise and market their products to a wider customer base




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Consultant to be appointed soon to design Kalaignar grand library in Tiruchi

The centre will offer translation, services for persons with disabilities and children, training and mentorship programmes, besides hosting monthly literary events




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High-level committee formed to facilitate clearances for companies that signed MoU, says Minister

Constant monitoring was being done now from the time of signing of MoUs to providing employment in new industrial units, says Industries Minister T.R.B. Rajaa




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NTK chief Seeman booked for alleged ‘derogatory remarks’ against Karunanidhi




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Uppiliyapuram, gateway to scenic Pachamalai, lacks bus stand with passengers left to fight the elements

Buses stop at a busy junction making it difficult for commuters as well as local businessmen; a site is yet to be identified for the bus stand




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Guidelines issued for fertilizer distribution in Karaikal for samba, thaladi paddy cultivation




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EPS’s dream of AIADMK staging a comeback in 2026 election will not materialise: Law Minister Regupathy




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Two doctors posted at Uppiliyapuram UPHC




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Library to hold Group II-A Mains, Group IV TNPSC model test




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Advanced baggage handling system introduced in Tiruchi airport




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Art and literary contests lined up for District Central Library’s National Library Week




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Tiruchi Corporation office expansion plan witnesses more delay




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‘State should retain primary agricultural cooperative societies under its purview’




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IECD holds graduation ceremony of SUITS

As many as 93,435 students from Grade V to Grade IX in 358 schools across the State appeared for 2023-2024 BDU examinations




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Students and agriculture officials grapple with logistical, technical issues during digital crop survey




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Nagapattinam MP presses for new express trains, railway line extensions




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Association holds protest against delay in Anna University’s staff absorption, promotions




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AIADMK ready to join hands with like-minded parties to defeat DMK: Palaniswami




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Live Cricket Scores, Cricket News, Analysis, Results & More | The Hindu




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543: Zach Leatherman on Eleventy, Mastodon, Twitter, and is-land

Zach Leatherman talks with us about what's new with Eleventy, setting up on Mastodon, what's happened with Twitter, and is-land.




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546: Ryan Dahl and Deno

Ryan Dahl stops by to talk about Node, Deno, JavaScript, testing, V8, and thoughts around getting started with Deno.




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550: Sanity with Simen Svale Skogsrud and Espen Hovlandsdal

Simen and Espen from Sanity stop by to talk about the origins of Sanity, how Sanity Studio works, good use cases for Sanity, how Sanity does real time updates, what Groq is, and where to start with Sanity.




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551: PlanetScale with Iheanyi Ekechukwu and Mike Coutermarsh

Iheanyi Ekechukwu and Mike Coutermarsh talk about PlanetScale, what Vitess is, if PlanetScale is for both side and big projects, what read only regions are, what schema changes are, and how PlanetScale compares to other projects.




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552: Do You Want to Build a JS Framework? ☃️ CSS Wishlist for 2023

Austin power updates, what do you need if you want to build a new JavaScript framework, and what do we hope CSS brings in 2023?




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553: TypeScript, DX, GripeScript, and Astro v2 with Fred Schott

Fred Schott stops by to talk about TypeScript, what DX means in 2023, a bit of GripeScript, and being transparent about what Astro is good at, and what it's not.




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555: React Documentary, Front of the Front End, Fast Fallacy, and Best Practices

Reacting to the React.js documentary, is there still jobs for front of the front end anymore? The fast fallacy in frameworks, best practices, dealing with too much or too little isolation, and AI test generation.