Outline

Overview

Major changes to the way we discover and develop new medicines have taken place in recent years. Sequencing of the human genome has revolutionised drug target identification and therapeutic design. Approaches that combine molecular biology and intensive data analysis are key to the development of effective personalised and precision therapies. New methods in organic synthesis have accelerated how we explore chemical space and parallel developments in nanotechnology are driving innovative drug delivery methods. Improvements in cell, tissue and animal models of human disease are changing how drugs are identified and tested. In this unit, you will explore how these new ideas and technologies are transforming medicinal chemistry. You will learn and apply such techniques to the molecular-level understanding of diseases and the design of effective therapeutics. You will learn the procedures leading to drug registration and regulation. You will participate in enquiry-led practicals that reinforce the concepts of the unit and develop your skills in cutting-edge methods used in modern medicinal chemistry. By studying this unit you will build knowledge and skills that will enable you to play a role in creating therapeutics that will impact lives.

Unit details and rules

Academic unit	Department of Medical Sciences
Credit points	6
Prerequisites ?	[(PCOL2011 or PCOL2021 or MEDS2002) or (BMED2401 and BMED2402) or (BMED2401 and BMED2405)] or (12cp from BCMB2XXX) and [(CHEM2401 or CHEM2521 or CHEM2911 or CHEM2915 or CHEM2921 or CHEM2991)]
Corequisites ?	None
Prohibitions ?	MCHM3901
Assumed knowledge ?	None
Available to study abroad and exchange students	Yes

Teaching staff

Coordinator	Michael Gotsbacher, michael.gotsbacher@sydney.edu.au

Type	Description	Weight	Due	Length
Final exam (Record+)	Final exam Short answer and MCQ	40%	Formal exam period	2 hours
Outcomes assessed:
Presentation	Presentation Presentation in-class or pre-recorded.	10%	Week 04	3 minute duration.
Outcomes assessed:
Small test	Test 1 Canvas quiz	5%	Week 05	1 hour
Outcomes assessed:
Presentation	Group slide presentation Presentation slides	10%	Week 07	10-slide template provided.
Outcomes assessed:
Assignment	In silico Docking Assignment Figure and Legend Preparation of a representative and explanatory figure and figure legend.	10%	Week 08	1 page
Outcomes assessed:
Small test	Test 2 Canvas quiz	5%	Week 10	1 hour
Outcomes assessed:
Assignment	Project report HIRACs, Results, Analysis and Abstract organised in LabArchives.	20%	Week 12	Variable
Outcomes assessed:
= hurdle task ? = group assignment ? = Type B final exam ?

Assessment summary

Test 1 and 2: All in-semester assessments are compulsory, and failure to submit any piece of assessment will result in a grade of ‘AF Absent Fail’ for the unit of study.
Presentation: This involves the presentation of a research finding regarding a widely used therapeutic such as antibiotics, in the style of a short talk to a non-scientific audience.
Group slide presentation: This involves preparation of a presentation slide deck, using the template provided, with material describing the process of evaluation and approval of a drug for prescription in Australia.
Docking Assignment: Preparation of figure and legend illustrating output of in silico docking workshop
Project report: HIRACs, Results, Analysis and Abstract organised in LabArchives according to template provided.
Final exam: No sample papers will be provided.

Detailed information for each assessment can be found on Canvas.

Assessment criteria

The University awards common result grades, set out in the Coursework Policy 2014 (Schedule 1).

As a general guide, a high distinction indicates work of an exceptional standard, a distinction a very high standard, a credit a good standard, and a pass an acceptable standard.

Result name	Mark range	Description
High distinction	85 - 100	Mastery of topics showing extensive integration and ability to transfer knowledge to novel contexts; treatment of tasks shows an advanced synthesis of ideas; demonstration of initiative, complex understanding and analysis; work is very well presented; all criteria addressed and learning outcomes achieved to an outstanding level
Distinction	75 - 84	Excellent achievement, consistent evidence of deep understanding and application of knowledge in medical science; treatment of tasks shows advanced understanding of topics; demonstration of initiative, complex understanding and analysis; work is well-presented; all criteria addressed and learning outcomes achieved to a superior level
Credit	65 - 74	Confident in explaining medical science processes, with evidence of solid understanding and achievement; occasional lapses indicative of unresolved issues; treatment of tasks shows a good understanding of topic; work is well-presented with a minimum of errors; all criteria addressed and learning outcomes achieved to a high level
Pass	50 - 64	Satisfactory level of engagement with and understanding of topic; some inconsistencies in understanding and knowledge of medical science; work is adequately presented, with some errors or omissions, most criteria addressed and learning outcomes achieved to an adequate level
Fail	0 - 49	Unsatisfactory achievement and engagement with the medical science discipline; inadequate understanding or fundamental misunderstanding of topics; most criteria and learning outcomes not clearly or adequately addressed or achieved; lack of effort/involvement in the unit

For more information see guide to grades.

Late submission

In accordance with University policy, these penalties apply when written work is submitted after 11:59pm on the due date:

Deduction of 5% of the maximum mark for each calendar day after the due date.
After ten calendar days late, a mark of zero will be awarded.

Academic integrity

The Current Student website provides information on academic integrity and the resources available to all students. The University expects students and staff to act ethically and honestly and will treat all allegations of academic integrity breaches seriously.

We use similarity detection software to detect potential instances of plagiarism or other forms of academic integrity breach. If such matches indicate evidence of plagiarism or other forms of academic integrity breaches, your teacher is required to report your work for further investigation.

Use of generative artificial intelligence (AI) and automated writing tools

You may only use generative AI and automated writing tools in assessment tasks if you are permitted to by your unit coordinator. If you do use these tools, you must acknowledge this in your work, either in a footnote or an acknowledgement section. The assessment instructions or unit outline will give guidance of the types of tools that are permitted and how the tools should be used.

Your final submitted work must be your own, original work. You must acknowledge any use of generative AI tools that have been used in the assessment, and any material that forms part of your submission must be appropriately referenced. For guidance on how to acknowledge the use of AI, please refer to the AI in Education Canvas site.

The unapproved use of these tools or unacknowledged use will be considered a breach of the Academic Integrity Policy and penalties may apply.

Studiosity is permitted unless otherwise indicated by the unit coordinator. The use of this service must be acknowledged in your submission as detailed on the Learning Hub’s Canvas page.

Outside assessment tasks, generative AI tools may be used to support your learning. The AI in Education Canvas site contains a number of productive ways that students are using AI to improve their learning.

Learning support

Simple extensions

If you encounter a problem submitting your work on time, you may be able to apply for an extension of five calendar days through a simple extension.  The application process will be different depending on the type of assessment and extensions cannot be granted for some assessment types like exams.

Special consideration

If exceptional circumstances mean you can’t complete an assessment, you need consideration for a longer period of time, or if you have essential commitments which impact your performance in an assessment, you may be eligible for special consideration or special arrangements.

Special consideration applications will not be affected by a simple extension application.

Using AI responsibly

Co-created with students, AI in Education includes lots of helpful examples of how students use generative AI tools to support their learning. It explains how generative AI works, the different tools available and how to use them responsibly and productively.

Weekly schedule

WK	Topic	Learning activity
Week 01	Unit Introduction; History and future of Drug Discovery	Lecture (1 hr)
Week 01	Omics-informed drug discovery	Lecture (1 hr)
Week 02	Introduction to Practical Stream and NMR-based fragment screening.	Practical (3 hr)
	Omics in target and lead identification and drug evaluation	Lecture (1 hr)
	Metabolomics and lipidomics in drug development and evaluation	Lecture (1 hr)
Week 03	Enzyme assay and sample preparation for NMR based fragment screening	Practical (3 hr)
	Expanding the druggable proteome	Lecture (1 hr)
	Data analysis, identification of fragment hits and molecular visualisation.	Practical (3 hr)
	Therapeutic modulation of gene expression	Lecture (1 hr)
Week 04	Communicating drug development stories to a lay audience	Workshop (3 hr)
	2D and 3D cell cultures and organ-on-a-chip	Lecture (1 hr)
	From phage display to therapeutics	Lecture (1 hr)
Week 05	Synthesis of drug discovery lead compound #1	Practical (3 hr)
	Synthesis of drug discovery lead compound #2	Practical (3 hr)
	Hit discovery: high-throughput methods	Lecture (1 hr)
Week 06	Synthesis of drug discovery lead compound #3	Practical (3 hr)
	Macrocycle screening	Lecture (1 hr)
	Synthesis of drug discovery lead compound #4	Practical (3 hr)
	In silico virtual screening	Lecture (1 hr)
Week 07	Enzyme activity assays and determination of lead compound IC50.	Practical (3 hr)
	Hit-to-lead approaches for optimising target interactions 1	Lecture (1 hr)
	Hit-to-lead approaches for optimising target interactions 2	Lecture (1 hr)
Week 08	In silico docking 1	Workshop (3 hr)
	Using Medicinal Chemistry to Solve ADME Challenges 1	Lecture (1 hr)
	In silico docking 2	Workshop (3 hr)
	Using Medicinal Chemistry to Solve ADME Challenges 2	Lecture (1 hr)
Week 09	Lead optimisation and late-stage functionalisation 1	Lecture (1 hr)
Week 10	Lead optimisation and late-stage functionalisation 2	Lecture (1 hr)
Week 10	Tutorial 1	Tutorial (2 hr)
Week 11	Evaluating the use of animals in research	Workshop (3 hr)
	Economic challenges in drug discovery	Lecture (1 hr)
	Formulation - effective delivery methods	Lecture (1 hr)
Week 12	Developing methods of drug delivery	Lecture (1 hr)
Week 12	Clinical Trials for pharmaceuticals and devices	Lecture (1 hr)
Week 13	Preclinical toxicology - is it safe?	Lecture (1 hr)
	Tutorial 2	Tutorial (2 hr)
	What the TGA requires for a submission	Lecture (1 hr)

Attendance and class requirements

Due to the exceptional circumstances caused by the COVID-19 pandemic, attendance requirements for this unit of study have been amended. Where online lectures/tutorials/workshops/virtual laboratories have been scheduled, students should make every effort to attend and participate at the scheduled time. Penalties will not be applied if technical issues, etc. prevent attendance at a specific online class. In that case, students should discuss the problem with the coordinator, and attend another session, if available.

Study commitment

Typically, there is a minimum expectation of 1.5-2 hours of student effort per week per credit point for units of study offered over a full semester. For a 6 credit point unit, this equates to roughly 120-150 hours of student effort in total.

Required readings

All readings for this unit can be accessed through the Library eReserve, available on Canvas.

Patrick, GL, (2016) An Introduction to Medicinal Chemistry 6th ed. Oxford University Press.

Learning outcomes

Learning outcomes are what students know, understand and are able to do on completion of a unit of study. They are aligned with the University's graduate qualities and are assessed as part of the curriculum.

Outcomes
Graduate qualities

At the completion of this unit, you should be able to:

LO1. demonstrate an understanding of major developments in modern drug discovery, ranging from analysis of bioinformatics through combinatorial synthetic methods and fragment-based screening, to formulation, preclinical development, delivery and registration
LO2. apply bioinformatics and in silico methods to drug target identification and drug optimisation
LO3. propose and justify reasonable synthetic approaches towards small organic molecule drug candidates
LO4. understand and apply the principles of scientific measurement during a fragment-based screening project
LO5. find and analyse information and judge its reliability and significance when evaluating the efficacy of drug action
LO6. communicate scientific information appropriately, both orally and through written work
LO7. engage in team and group work to assess the development, approval and registration of new drugs
LO8. demonstrate a sense of responsibility, ethical behaviour, and independence as a learner and as a scientist.

Graduate qualities

The graduate qualities are the qualities and skills that all University of Sydney graduates must demonstrate on successful completion of an award course. As a future Sydney graduate, the set of qualities have been designed to equip you for the contemporary world.

GQ1	Depth of disciplinary expertise Deep disciplinary expertise is the ability to integrate and rigorously apply knowledge, understanding and skills of a recognised discipline defined by scholarly activity, as well as familiarity with evolving practice of the discipline.
GQ2	Critical thinking and problem solving Critical thinking and problem solving are the questioning of ideas, evidence and assumptions in order to propose and evaluate hypotheses or alternative arguments before formulating a conclusion or a solution to an identified problem.
GQ3	Oral and written communication Effective communication, in both oral and written form, is the clear exchange of meaning in a manner that is appropriate to audience and context.
GQ4	Information and digital literacy Information and digital literacy is the ability to locate, interpret, evaluate, manage, adapt, integrate, create and convey information using appropriate resources, tools and strategies.
GQ5	Inventiveness Generating novel ideas and solutions.
GQ6	Cultural competence Cultural Competence is the ability to actively, ethically, respectfully, and successfully engage across and between cultures. In the Australian context, this includes and celebrates Aboriginal and Torres Strait Islander cultures, knowledge systems, and a mature understanding of contemporary issues.
GQ7	Interdisciplinary effectiveness Interdisciplinary effectiveness is the integration and synthesis of multiple viewpoints and practices, working effectively across disciplinary boundaries.
GQ8	Integrated professional, ethical, and personal identity An integrated professional, ethical and personal identity is understanding the interaction between one’s personal and professional selves in an ethical context.
GQ9	Influence Engaging others in a process, idea or vision.

Outcome map

Learning outcomes	Graduate qualities
Learning outcomes

Responding to student feedback

This section outlines changes made to this unit following staff and student reviews.

No changes have been made since this unit was first offered in 2020.

Additional information

Work, health and safety

We are governed by the Work Health and Safety Act 2011, Work Health and Safety Regulation 2011 and Codes of Practice. Penalties for non-compliance have increased. Everyone has a responsibility for health and safety at work. The University’s Work Health and Safety policy explains the responsibilities and expectations of workers and others, and the procedures for managing WHS risks associated with University activities.

General Laboratory Safety Rules

No eating or drinking is allowed in any laboratory under any circumstances
A laboratory coat and closed-toe shoes are mandatory
Follow safety instructions in your manual and posted in laboratories
In case of fire, follow instructions posted outside the laboratory door
First aid kits, eye wash and fire extinguishers are located in or immediately outside each laboratory
As a precautionary measure, it is recommended that you have a current tetanus immunisation. This can be obtained from University Health Service: unihealth.usyd.edu.au/

Disclaimer

The University reserves the right to amend units of study or no longer offer certain units, including where there are low enrolment numbers.

To help you understand common terms that we use at the University, we offer an online glossary.

Current students

Overview

Overview

Unit details and rules

Teaching staff

Assessment

Assessment

Assessment summary

Assessment criteria

Late submission

Academic integrity

Learning support

Learning support

Simple extensions

Special consideration

Using AI responsibly

Weekly schedule

Weekly schedule

Attendance and class requirements

Study commitment

Required readings

Learning outcomes

Learning outcomes

Graduate qualities

Outcome map

Responding to student feedback

Responding to student feedback

Additional information

Additional information

Work, health and safety

Disclaimer

On this page

Useful links

Media

Student links

About us

Connect

Current students

MCHM3001: From Molecules to Therapeutics

Semester 1, 2022 [Normal day] - Camperdown/Darlington, Sydney

Overview

Overview

Unit details and rules

Teaching staff

Assessment

Assessment

Assessment summary

Assessment criteria

Late submission

Academic integrity

Learning support

Learning support

Simple extensions

Special consideration

Using AI responsibly

Weekly schedule

Weekly schedule

Attendance and class requirements

Study commitment

Required readings

Learning outcomes

Learning outcomes

Graduate qualities

Outcome map

Responding to student feedback

Responding to student feedback

Additional information

Additional information

Work, health and safety

Disclaimer

On this page

Useful links

Media

Student links

About us

Connect