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At least 1,135 records · Page 63

Predicting receptor-ligand pairing preferences in plant-microbe interfaces via molecular dynamics and machine learning

Microbiome assembly, structure, and dynamics significantly influence plant health. Secreted microbial signaling molecules initiate and mediate symbiosis by binding to structurally compatible plant receptors. For example, lipo-chitooligosaccharides (LCOs), produced by nitrogen-fixing rhizobial bacteria and various fungi, are recognized by plant lysin motif receptor-like kinases (LysM-RLKs), which activate the common symbiotic pathway. Accurately predicting these molecular interactions could reveal complementary signatures underlying the initial stages of endosymbiosis. Despite the breakthrough in protein-ligand structure prediction with deep learning-based tools, such as AlphaFold3, the large size and highly flexible nature of signaling compounds like LCOs present major challenges for detailed structural characterization and binding-affinity prediction. Typical structure-/physics-based methods of ligand virtual screening are designed for small, drug-like molecules, often rely on high-resolution, experimentally determined structures of the protein receptors, and rarely achieve sufficient sampling to obtain converged thermodynamic quantities with large ligands. In this study, we developed a hybrid molecular dynamics/machine learning (MD/ML) approach capable of predicting binding affinity rankings with high accuracy in systems involving large, flexible ligands, despite limited experimental structural information. Using coarse initial structural models, the predictions using the MD/ML workflow achieved strong alignment with experimental trends, particularly in the top-affinity tier for four legume LysM-RLKs (LYR3) binding to LCOs and a chitooligosaccharide. Furthermore, the MD-based conformation selection protocol provided critical structural insights into substrate specificity and binding mechanisms. This study demonstrates a powerful method to screen for challenging cognate ligand-receptors and advance our understanding of the molecular basis of microbial colonization in plants.

Lipo-chitooligosaccharides↗

Synergistic effects of H3 and H4 nucleosome tails on structure and dynamics of a lesion-containing DNA: Binding of a displaced lesion partner base to the H3 tail for GG-NER recognition

How DNA lesions in nucleosomes are recognized for global genome nucleotide excision repair (GG-NER) remains poorly understood, and the roles that histone tails may play remains to be established. Histone H3 and H4 N-terminal tails are of particular interest as their acetylation states are important in regulating nucleosomal functions in transcription, replication and repair. In particular the H3 tail has been the focus of recent attention as a site for the interaction with XPC, the GG-NER lesion recognition factor. Here we have investigated how the structure and dynamics of the DNA lesion cis-B[a]P-dG, derived from the environmental carcinogen benzo[a]pyrene (B[a]P), is impacted by the presence of flanking H3 and H4 tails. This lesion is well-repaired by GG-NER, and adopts a base-displaced/intercalated conformation in which the lesion partner C is displaced into the major groove. We used molecular dynamics simulations to obtain structural and dynamic characterizations for this lesion positioned in nucleosomal DNA so that it is bracketed by the H3 and H4 tails. The H4 tail was studied in unacetylated and acetylated states, while the H3 tail was unacetylated, its state when it binds XPC (Kakumu, Nakanishi et al., 2017). Our results reveal that upon acetylation, the H4 tail is released from the DNA surface; the H3 tail then forms a pocket that induces flipping and capture of the displaced lesion partner base C. This reveals synergistic effects of the behavior of the two tails. We hypothesize that the dual capability of the H3 tail to sense the displaced lesion partner base and to bind XPC could foster recognition of this lesion by XPC for initiation of GG-NER in nucleosomes.

59 BASIC BIOLOGICAL SCIENCES↗

Towards a liana plant functional type for vegetation models

Lianas (woody climbers) are crucial components of tropical forests and they have been increasingly recognized to have profound effects on tropical forest carbon dynamics. Despite their importance, lianas' representation in vegetation models remains limited, partly due to the complexity of liana-tree dynamics and the diversity in liana life history strategies. This paper provides a comprehensive review of advances and challenges for mechanistically representing lianas in forest ecosystem models and a proposed path towards effectively representing lianas in these models. Defining a liana plant functional type is a significant challenge because of the high morphological and physiological diversity amongst liana species, and because of their structural association with trees. Here, we identify critical liana traits that likely should contribute to establishing a liana plant functional type, along with key processes to properly represent lianas in ecosystem models. Subsequently, we discuss a variety of possible liana implementation strategies with their associated strengths, limitations, computational costs and data requirements. A fundamental redesign of the tree-centric demographic vegetation models seems appropriate to accommodate the unique growth and competition strategies of lianas. We illustrate the potential of such models with a single-site case study where we disentangle putative mechanisms of liana increasing abundance. Furthermore, we underscore the critical need for comprehensive liana demographic and functional data (including long-term, physiological, and pantropical observations) for the qualitative implementation and evaluation in the proposed modeling efforts. Currently, there is a scarcity of liana data and the data that do exist have a neotropical bias. We finally introduce a new liana functional trait database that can centralize existing liana trait data, incentivize improved data gathering and thus facilitate model development and scientific analyses.

54 ENVIRONMENTAL SCIENCES↗

An Accelerated Testing and Analysis Framework for Qualification of Battery Materials

The continuously growing demand for batteries used within automotive, aviation, and grid applications has exacerbated the need to supplement critical battery material feedstocks, such as those for anode and cathode active materials. New or supplementary material sources, however, universally comprise unique material properties that can significantly affect the lifetime and performance of resultant batteries. As such, the influence of composition, microstructure, and morphology on electrochemical performance should be characterized quickly and accurately to accelerate commercialization of new material sources. This work introduces a tiered framework to quickly assess new material viability and understand the influence of physicochemical properties on battery performance. The Tier 1 testing described here is rapid and lower-effort to quickly recognize materials with fundamental flaws and potentially disqualify them. Later testing would require more time and effort but provide higher fidelity information with a goal of validating materials for specific applications. A case study examining various commercial sources of LiFePO4 (LFP) is presented, using Tier 1 of the protocol to identify rapid electrochemical and physicochemical signals that correlate with performance and to provide early go/no-go decisions on LFP materials without the need for long-term cycling data.

25 - ENERGY STORAGE↗

A window on urban sustainability

Sustainable urban development requires the integration of environmental interests in urban planning. Although various methods of environmental assessment have been developed, plan outcomes are often disappointing due to the complex nature of decision-making in urban planning, which takes place in multiple arenas within multiple policy networks involving diverse stakeholders. We argue that the concept of ‘decision windows’ can structure this seemingly chaotic chain of interrelated decisions. First, explicitly considering the dynamics of the decision-making process, we further conceptualized decision windows as moments in an intricate web of substantively connected deliberative processes where issues are reframed within a decision-making arena, and interests may be linked within and across arenas. Adopting this perspective in two case studies, we then explored how decision windows arise, which factors determine their effectiveness and how their occurrence can be influenced so as to arrive at more sustainable solutions. We conclude that the integration of environmental interests in urban planning is highly dependent on the ability of the professionals involved to recognize and manipulate decision windows. Finally, we explore how decision windows may be opened. -- Highlights: • Decision-making about sustainable urban development occurs in networks. • The concept of ‘decision windows’ was further elaborated. • Decision windows help understand how environmental interests enter decision-making. • Decision windows can, to some extent, be influenced.

54 ENVIRONMENTAL SCIENCES↗

Road ecology in environmental impact assessment

Transport infrastructure has a wide array of effects on terrestrial and aquatic ecosystems, and road and railway networks are increasingly being associated with a loss of biodiversity worldwide. Environmental Impact Assessment (EIA) and Strategic Environmental Assessment (SEA) are two legal frameworks that concern physical planning, with the potential to identify, predict, mitigate and/or compensate transport infrastructure effects with negative impacts on biodiversity. The aim of this study was to review the treatment of ecological impacts in environmental assessment of transport infrastructure plans and projects. A literature review on the topic of EIA, SEA, biodiversity and transport infrastructure was conducted, and 17 problem categories on the treatment of biodiversity were formulated by means of a content analysis. A review of environmental impact statements and environmental reports (EIS/ER) produced between 2005 and 2013 in Sweden and the UK was then conducted using the list of problems as a checklist. The results show that the treatment of ecological impacts has improved substantially over the years, but that some impacts remain problematic; the treatment of fragmentation, the absence of quantitative analysis and that the impact assessment study area was in general delimited without consideration for the scales of ecological processes. Actions to improve the treatment of ecological impacts could include improved guidelines for spatial and temporal delimitation, and the establishment of a quantitative framework including tools, methods and threshold values. Additionally, capacity building and further method development of EIA and SEA friendly spatial ecological models can aid in clarifying the costs as well as the benefits in development/biodiversity tradeoffs. - Highlights: • The treatment of ecological impacts in EIA and SEA has improved. • Quantitative methods for ecological impact assessment were rarely used • Fragmentation effects were recognized but not analysed.

54 ENVIRONMENTAL SCIENCES↗

A critical review of environmental assessment tools for sustainable urban design

Cities are responsible for the depletion of natural resources and agricultural lands, and 70% of global CO{sub 2} emissions. There are significant risks to cities from the impacts of climate change in addition to existing vulnerabilities, primarily because of rapid urbanization. Urban design and development are generally considered as the instrument to shape the future of the city and they determine the pattern of a city's resource usage and resilience to change, from climate or otherwise. Cities are inherently dynamic and require the participation and engagement of their diverse stakeholders for the effective management of change, which enables wider stakeholder involvement and buy-in at various stages of the development process. Sustainability assessment of urban design and development is increasingly being seen as indispensable for informed decision-making. A sustainability assessment tool also acts as a driver for the uptake of sustainable pathways by recognizing excellence through their rating system and by creating a market demand for sustainable products and processes. This research reviews six widely used sustainability assessment tools for urban design and development: BREEAM Communities, LEED-ND, CASBEE-UD, SBTool{sup PT}–UP, Pearl Community Rating System (PCRS) and GSAS/QSAS, to identify, compare and contrast the aim, structure, assessment methodology, scoring, weighting and suitability for application in different geographical contexts. Strengths and weaknesses of each tool are critically discussed. The study highlights the disparity in local and international contexts for global sustainability assessment tools. Despite their similarities in aim on environmental aspects, differences exist in the relative importance and share of mandatory vs optional indicators in both environmental and social dimensions. PCRS and GSAS/QSAS are new incarnations, but have widely varying shares of mandatory indicators, at 45.4% and 11.36% respectively, compared to 30% in BREEAM Community. Considerations of economic and cultural aspects are only marginal in the reviewed sustainability assessment tools. However, the newly developed sustainability assessment tools such as GSAS/QSAS and PCRS diverge from their predecessors in their consideration of cultural aspects. - Highlights: • Reviews six urban sustainability assessment methods: LEED-ND, BREEAM Communities, CASBEE-UD, SBTool{sup PT}-UP, PCRS, GSAS/QSAS. • Reviewed methods are biased more towards the environmental, followed by social and economic dimensions of sustainability. • Water issues are highlighted in the Middle East but natural hazards are emphasized only in CASBEE and BREEAM Communities. • SBTool{sup PT}-UP, the most recent of the groups puts more weight (7.32%) on cultural aspects. • Share of mandatory indicators is highest (45.4%) in the Pearl Community Rating System (PCRS)

54 ENVIRONMENTAL SCIENCES↗

Advancing the practice of health impact assessment in Canada: Obstacles and opportunities

Health Impact Assessment (HIA) is recognized as a useful tool that can identify potential health impacts resulting from projects or policy initiatives. Although HIA has become an established practice in some countries, it is not yet an established practice in Canada. In order to enable broader support for HIA, this study provides a comprehensive review and analysis of the peer-reviewed and gray literature on the state of HIA practice. The results of this review revealed that, although there is an abundance of publications relating to HIA, there remains a lack of transparent, consistent and reproducible approaches and methods throughout the process. Findings indicate a need for further research and development on a number of fronts, including: 1) the nature of HIA triggers; 2) consistent scoping and stakeholder engagement approaches; 3) use of evidence and transparency of decision-making; 4) reproducibility of assessment methods; 5) monitoring and evaluation protocols; and, 6) integration within existing regulatory frameworks. Addressing these issues will aid in advancing the more widespread use of HIA in Canada. - Highlights: • Reviewed current state of practice in the field of HIA • Identified key obstacles and opportunities for HIA advancement • Major issues include lack of consistent approach and methodology. • No national regulatory driver hinders opportunity for widespread use of HIA. • Identified research opportunities vital to developing HIA practice in Canada.

54 ENVIRONMENTAL SCIENCES↗

A new method to assess the sustainability performance of events: Application to the 2014 World Orienteering Championship

Nowadays an increasing attention of public and private agencies to the sustainability performance of events is observed, since it is recognized as a key issue in the context of sustainable development. Assessing the sustainability performance of events involves environmental, social and economic aspects; their impacts are complex and a quantitative assessment is often difficult. This paper presents a new quali-quantitative method developed to measure the sustainability of events, taking into account all its potential impacts. The 2014 World Orienteering Championship, held in Italy, was selected to test the proposed evaluation methodology. The total carbon footprint of the event was 165.34 tCO{sub 2}eq and the avoided emissions were estimated as being 46 tCO{sub 2}eq. The adopted quali-quantitative method resulted to be efficient in assessing the sustainability impacts and can be applied for the evaluation of similar events. - Highlights: • A quali-quantitative method to assess events' sustainability is presented. • All the methodological issues related to the method are explained. • The method is used to evaluate the sustainability of an international sports event. • The method resulted to be valid to assess the event's sustainability level. • The carbon footprint of the event has been calculated.

29 ENERGY PLANNING, POLICY, AND ECONOMY↗

Current legal regime for environmental impact assessment in areas beyond national jurisdiction and its future approaches

In 2004, the United Nations launched an Ad Hoc Open-ended Informal Working Group to study issues relating to the conservation and sustainable use of marine biological diversity in areas beyond national jurisdiction. Since then, the topic of governing marine areas beyond national jurisdiction (ABNJ) has been widely discussed by politicians, policy makers and scholars. As one of management tools to protect marine biodiversity in ABNJ, environmental impact assessment (EIA) has been widely recognized and accepted by the international community, however, the biggest challenge is how to effectively implement the EIA regime in ABNJ. This paper explores the impacts of anthropogenic activities in ABNJ on marine ecosystems, reviews the existing legal regime for EIA in ABNJ and discusses possible measures to strengthen the implementation of EIA in ABNJ. - Highlights: • We identify human activities in ABNJ and their impacts on marine ecosystems. • We analyze the characters and gaps of the existing legal regime for EIA in ABNJ. • We analyze the pros and cons of alternative approaches of EIA in ABNJ.

54 ENVIRONMENTAL SCIENCES↗

Disasters can happen to anybody: The case of Korea

In Korea, there is a pervasive feeling of invincibility to the point that people and organizations do not believe that disasters can strike them. This has impact on the level of preparedness for disasters. This study aims to delve into how Korea has to change its governmental policies/practices with some private partners' efforts to mitigate disaster risks. A case study was utilized as the major methodology by comparing exclusive management with inclusive management. These two approaches have been comparatively analyzed via four variables, namely the central government, the local governments, the incident commander, and other stakeholders. The major finding is that Korea's practices and policies have to evolve from the current exclusive management into future-oriented inclusive management. Moreover, the importance of communication, cooperation, collaboration, and multi-discipline coordination is discussed. Additionally, the problem of reductionism and equal participation among all stakeholders, as well as the resistance from vested interests, are recognized and elaborated for Korea and the international community. - Highlights: • Only a few stakeholders in Korea believe that disaster can happen to anyone. This study aims to delve into how Korea has to change its current practices to mitigate disaster risks. • To compare exclusive management with inclusive management, we have examined four comparative variables, namely the central government's policy, local government's strategy, the incident commander's post, and other stakeholders' efforts. • The major finding is that Korea's practices and policies have to evolve from the current exclusive management into future-oriented inclusive management.

54 ENVIRONMENTAL SCIENCES↗

Bridging the divide between theory and guidance in strategic environmental assessment: A path for Italian regions

Clear and effective legislation is a requisite to bring sustainable development from theory into practice. This paper develops a methodology to investigate how Italian regional legislation disciplines the use of Strategic Environmental Assessment (SEA), the procedure used in the European Union (EU) to pursue sustainable development of policies, plans, and programs (PPPs). Our case study is the Italian regional level, examined to identify eventual flaws and areas for improvement for each regional legislative framework. For this purpose, this study refers to a selection of analytical criteria recurring in the international debate on sustainability assessments. Statistical multi-dimensional analysis is used to identify Italian regions with similar SEA legislation. We recognize four taxonomies, depending on the way regional legislation provides information about i) legislation and guidelines, ii) integration between SEA and PPPs, iii) sustainability goals, iv) technical organization, v) participatory organization, and vi) monitoring. The results suggest that Italian administrators should cooperate to improve legislation at the regional level. Acknowledging the institution-centred nature of SEA, this methodology could drive the EU to better support SEA development in countries with diversified traditions.

29 ENERGY PLANNING, POLICY, AND ECONOMY↗

Social relations: A critical reflection on the notion of social impacts as change

This article seeks to reflect upon the dominant conception of social impacts as the change produced by development projects and programs, and the ways in which those affected perceive and experience them. Identifying change may be a necessary but not sufficient step in acknowledging the complexity of social life. Engaging with critical scholarship produced in the fields of both social impact assessment (SIA) and of the social studies of technical/planned interventions, I discuss how the understanding of social impacts as change responds ultimately to a causal–instrumental logic that, in order to make sense of the complexity of social life, tends to reduce it to a series of variables and matrices. I suggest a complementary dialectical approach focusing on social relations. This approach, allows an alternative means of analysing social impacts concerning the way policies and projects reconfigure conditions and possibilities on a societal level. To accomplish this, and in order to go beyond the sequence of potential impacts (or changes) and their generic indicators, I propose a set of analytical questions that highlight how social relations are structured. Besides, on the assumption that development is both a form of governance and a space of contestation, negotiation, and activism, this approach may contribute to further the potential for reflection and mobilisation that the practice of SIA presents. - Highlights: •Change, which is inherent to social life, is insufficient to determine social impacts. •The critique of causal-instrumental logic provides insights to reflect on social impacts. •Social impacts should rather refer to how interventions reconfigure social relations. •The complex, mutually constitutive nature of social phenomena may thus be recognized. •SIA should go beyond change to the understanding of its socio-political significance.

54 ENVIRONMENTAL SCIENCES↗

Assessing the urban carbon footprint: An overview

All cities present environmental sustainability issues, above all regarding greenhouse gas (GHG) emissions, and specifically carbon dioxide (CO{sub 2}), that directly affect climate change. Consequently, it is very important to quantify and report their Carbon Footprint (CF) for implementing national and international policies/strategies aimed at mitigating and adapting these concerns. The Urban Carbon Footprint (UCF), indeed, has been recognized as the more valuable choice to inform, specifically, decision makers about city environmental sustainability. Several accounting systems and inventory methods have been taken into account to perform UCF, highlighting the complexity of the topic and generating very often confusion among users. In this context, the authors aim to summarize what has been done and what is going on with UCFs, trying to classify them according to some principal dimensions. Thus, they divide UFCs in two main categories namely: “spatial” or “direct”, with a limited amount of data requested, and “economic” or “life cycle based”, more or less data inclusive according to the accounting systems considered. Furthermore, they observe that there is not a “global agreed-upon protocol” yet, neither is there a specific model shared among researchers, even if some steps have been made towards this direction (Relative Carbon Footprint - RCF, Publicly Available Specification – PAS 2070 and Global Protocol for Community scale - GPC). Consequently, it is necessary to complete and standardize, in the short term, the accounting and reporting frameworks, in order to compare different UCFs for adopting shared climate strategies and actions at global level. - Highlights: •Cities present environmental sustainability issues. •GHG emissions - specifically carbon dioxide - directly affect climate change. •UCF is a tool to support policy makers towards city environmental sustainability. •There is not a “global agreed-upon protocol” to perform UFC. •There are still missing points to be considered to provide a sharing model.

29 ENERGY PLANNING, POLICY, AND ECONOMY↗

The role of time and social churn in impact assessment: An engagement-based model

To participate in social impact assessments, members of a community need to understand both the nature and complexity of impacts at the individual and social level. This study considers the role of engagement in developing community understanding of social impacts by documenting and analyzing organizational and community actions and responses in the Adani Carmichael mine case. Findings suggest engagement facilitates the conduct of social churn. We define social churn as a process of collective level discussion, meaning-making, and consensus-building from multiple information inputs in response to equivocality or uncertainty resulting from organizational behavior, out of which is generated an articulation of community level perceptions of that organizational behavior and its impacts at an individual, community, and societal level. Theoretically, the findings of this study challenge traditional linear notions of social impact assessments and offer an alternative engagement-based model. Practically, the model identifies ways in which organizations can recognize and participate in the social processes that both create and represent the differing levels of social reality determining perceptions of those impacts.

54 ENVIRONMENTAL SCIENCES↗

Comparative review of EIA in the Association of Southeast Asian Nations

Environmental sustainability is one of the frameworks for cooperation under the Declaration of ASEAN Concord II, 2015. Environmental Impact Assessment (EIA) has been recognized as a crucial tool. This paper proposes the review of EIA in ASEAN countries in three key areas, namely legal enforcement, implementation approach and EIA effectiveness as the basis for a sustainable approach. The results showed that almost all the countries established their EIAs at the legal level with the complete EIA process; however, the implementation was somewhat different depending on the unique characteristics of the EIA processes. Such unique characteristics can be divided into three groups. The first belongs to the countries that initiated the EIA process before 1990, although they have their own outstanding topography, namely, Thailand, Malaysia, Indonesia and the Philippines. The second group includes the countries that applied the EIA after 1990. The Asian Development Bank has played an active role and their EIA processes have rapidly developed especially EIA monitoring, Strategic Environmental Assessment (SEA) and Transboundary Impact Assessment. The countries in this group are Cambodia, Vietnam, Laos and Myanmar. The last group contains the countries with stringent environmental regulations and is becoming part of environmental laws. They include Singapore and Brunei. The tools to support the achievement of sustainability, such as ecosystem services, biodiversity offsets and transboundary impacts will be of prime importance to the ASEAN EIA in the future.

54 ENVIRONMENTAL SCIENCES↗

Environmental impact assessment follow-up for projects in China: Institution and practice

Highlights: • As an essential part of the environmental management system required by the EIA Law, the EIA follow-up was poorly executed. • The effectiveness of the EIA follow-up could be greatly elevated by enhancing monitoring and public participation. • Environmental information disclosure plays the essential role in promoting the EIA follow-up. - Abstract: The Environmental Impact Assessment (EIA) is one of the important means of environmental management worldwide, and the EIA follow-up is one of the crucial measures to ensure the concrete implementation of the EIA. In this research, systematic reviews of EIA follow-up for projects in China were conducted to comprehensively appraise the implementation of the EIA follow-up and to identify the potential to improve the practice of an EIA follow-up. First, the EIA follow-up reports were collected through various sources. In total, there were 74 EIA follow-up reports that were identified and acquired. Second, a reviewing framework, containing 16 different indicators, was developed to systematically document and classify these EIA follow-up reports. Third, these EIA follow-up reports were grouped into several categories according to various indicators and then were analyzed to recognize their key features, including sources of data, analytic tools adopted, spatial-temporal distribution, industrial distribution, triggering causes, content, structure and effectiveness. The results showed that there were considerable disparities in the quality and the rigor of EIA follow-ups conducted. These features, along with some existing deficiencies of EIA follow-up, such as the lack of corresponding monitoring and management, can greatly limit the overall application and effectiveness of EIA follow-up in China. However, a number of good practices were identified. For example, a list of projects subject to mandatory EIA follow-up was promulgated, and the conditions for projects subject to EIA follow-up were explicitly stipulated in regulations. These good practices would be very helpful for the international EIA community to advance the practice of EIA follow-up, to reduce the disparities in the quality and the rigor of EIA follow-up, to improve the overall effectiveness of EIA follow-up and to promote the future implementation and development of EIA follow-up.

54 ENVIRONMENTAL SCIENCES↗

A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals

Boceprevir is an HCV NSP3 inhibitor that was explored as a repurposed drug for COVID-19. It inhibits the SARS-CoV-2 main protease (M Pro ) and contains an α-ketoamide warhead, a P1 β-cyclobutylalanyl moiety, a P2 dimethylcyclopropylproline, a P3 tert-butylglycine, and a P4 N-terminal tert-butylcarbamide. By introducing modifications at all four positions, we synthesized 20 boceprevir-based M Pro inhibitors including PF-07321332 and characterized their M Pro inhibition potency in test tubes (in vitro) and 293T cells (in cellulo). Crystal structures of M Pro bound with 10 inhibitors and cytotoxicity and antiviral potency of 4 inhibitors were characterized as well. Replacing the P1 site with a β-(S-2-oxopyrrolidin-3-yl)-alanyl (Opal) residue and the warhead with an aldehyde leads to high in vitro potency. The original moieties at P2, P3 and the P4 N-terminal cap positions in boceprevir are better than other tested chemical moieties for high in vitro potency. In crystal structures, all inhibitors form a covalent adduct with the M Pro active site cysteine. Here, the P1 Opal residue, P2 dimethylcyclopropylproline and P4 N-terminal tert-butylcarbamide make strong hydrophobic interactions with M Pro , explaining high in vitro potency of inhibitors that contain these moieties. A unique observation was made with an inhibitor that contains a P4 N-terminal isovaleramide. In its M Pro complex structure, the P4 N-terminal isovaleramide is tucked deep in a small pocket of M Pro that originally recognizes a P4 alanine side chain in a substrate. Although all inhibitors show high in vitro potency, they have drastically different in cellulo potency to inhibit ectopically expressed M Pro in human 293T cells. In general, inhibitors with a P4 N-terminal carbamide or amide have low in cellulo potency. This trend is reversed when the P4 N-terminal cap is changed to a carbamate. The installation of a P3 O-tert-butyl-threonine improves in cellulo potency. Three molecules that contain a P4 N-terminal carbamate were advanced to cytotoxicity tests on 293T cells and antiviral potency tests on three SARS-CoV-2 variants. They all have relatively low cytotoxicity and high antiviral potency with EC 50 values around 1 μM. A control compound with a nitrile warhead and a P4 N-terminal amide has undetectable antiviral potency. Based on all observations, we conclude that a P4 N-terminal carbamate in a boceprevir derivative is key for high antiviral potency against SARS-CoV-2.

60 APPLIED LIFE SCIENCES↗